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1-8. (Cancelled) 9. A prosthesis for reducing the incidence of herniation at an incision or other opening in connective tissue through which access has been made to treat an anatomical area spaced from such connective tissue incision or other opening, the incision or other opening in the connective tissue having a length and a depth and defining first and second edges, said prosthesis comprising: a first biocompatible, implantable sheet that is integratable with the connective tissue, said first sheet having a length and a height, said length of said first sheet corresponding to a length of the incision or opening in the connective tissue, and said height of said first sheet corresponding to the depth of the incision or opening in the connective tissue; a second biocompatible, implantable sheet that is integratable with the connective tissue, said second sheet having a length and a width, said length of said second sheet corresponding to a length of the incision or opening, and said width of said second sheet sufficient to overlap at least one of the first and second edges; wherein said second sheet extends substantially transversely to said first sheet. 10. The prosthesis of claim 9, wherein said width of said second sheet is sufficient to overlap both the first and second edges. 11. The prosthesis of claim 9, wherein said first and second sheets are tissue infiltratable. 12. The prosthesis of claim 9, wherein said first and second sheets form a T-shape. 13. The prosthesis of claim 9, wherein said first and second sheets form a V-shape. 14. The prosthesis of claim 9, wherein said second sheet includes a first sheet segment and a second sheet segment that is spaced from the first sheet segment. 15. The prosthesis of claim 9, wherein said second sheet includes a pair of diverging sheets. 16. The prosthesis of claim 9, wherein said first sheet includes a pair of diverging sheets. 17. The prosthesis of claim 9, further including a third biocompatible, implantable sheet that is integratable with the connective tissue, said third sheet having a length and a width, said length of said third sheet corresponding to the length of the incision or opening, and said width of said third sheet sufficient to overlap the first and second edges, said third sheet extending substantially transversely to said first sheet. 18. The prosthesis of claim 17, wherein said third sheet is tissue infiltratable. 19. The prosthesis of claim 17, wherein said first, second and third sheets form an I-shape. 20. The prosthesis of claim 17, wherein said first, second and third sheets form an X-shape. 21. The prosthesis of claim 17, wherein said third sheet includes a pair of diverging sheets. 22. The prosthesis of claim 17, wherein said second sheet extends along a first end of said first sheet and said third sheet extends along a second end of said first sheet. 23. The prosthesis of claim 22, wherein said first end is opposite said second end. 24. The prosthesis of claim 9, wherein said second sheet is perpendicular to said first sheet. 25. The prosthesis of claim 17, wherein said third sheet is perpendicular to said first sheet. 26. The prosthesis of claim 17, wherein said second sheet and said third sheet are perpendicular to said first sheet. 27. The prosthesis of claim 9, wherein each of said first and second sheets is planar. 28. The prosthesis of claim 17, wherein each of said first, second and third sheets is planar. 29. The prosthesis of claim 9, wherein at least one of said first and second sheets is formed of resorbable material. 30. The prosthesis of claim 29, wherein both of said first and second sheets are formed of resorbable material. 31. The prosthesis of claim 17, wherein each of said first, second and third sheets is formed of resorbable material. 32. The prosthesis of claim 9, wherein said first and second sheets have substantially a same thickness. 33. The prosthesis of claim 17, wherein said first, second and third sheets have substantially a same thickness. 34. The prosthesis of claim 9, wherein said prosthesis, after implantation at the incision or other opening, stimulates greater formation of connective tissue at the incision or other opening than if the first and second edges were merely approximated together by suturing without inclusion of said prosthesis. 35. The prosthesis of claim 9, wherein the anatomical area is a hernia. 36. The prosthesis of claim 9, wherein the connective tissue is beneath dermis and subcutaneous fat. 37. The prosthesis of claim 9, wherein the connective tissue is located in an abdominal wall. 38. The prosthesis of claim 9, wherein the connective tissue is an aponeurosis. 39. The prosthesis of claim 9, wherein said second sheet is constructed and arranged to be positioned beneath the first and second edges of the incision or other opening in the connective tissue. 40. The prosthesis of claim 9, wherein said second sheet is constructed and arranged to be positioned above the first and second edges of the incision or other opening in the connective tissue. 41. A method of reducing the incidence of herniation at an incision or other opening in connective tissue that is accessed to treat an anatomical area spaced from such connective tissue incision or other opening, the incision or other opening in the connective tissue defining a first edge and a second edge, and having a length and a depth, said method comprising: locating, in the incision or other opening in the connective tissue, a prophylactic, tissue integratable, prosthesis for reducing the incidence of herniation; and approximating together the first and second edges of the incision or other opening in the connective tissue. 42. The method of claim 41, wherein the prosthesis has a length corresponding to the length of the connective tissue incision or other opening and a height corresponding to the depth of the connective tissue incision or other opening. 43. The method of claim 41, wherein the prosthesis includes a flat portion and during said locating step, the flat portion is inserted between the first and second edges. 44. The method of claim 41, wherein the prosthesis is constructed and arranged to stimulate greater formation of connective tissue at the incision or other opening in the connective tissue than if the edges of the incision or other opening were merely approximated together by suturing without inclusion of the prosthesis. 45. The method of claim 41, wherein the prosthesis includes a tissue infiltratable material. 46. The method of claim 45, wherein the tissue infiltratable material is a sheet. 47. The method of claim 41, wherein said approximating step includes suturing together the first and second edges of the incision or other opening. 48. The method of claim 47, wherein a suture is passed through the prosthesis during said step of suturing together the first and second edges. 49. The method of claim 41, wherein the prosthesis includes a first biocompatible, implantable sheet that is integratable with the connective tissue, and a second biocompatible, implantable sheet that is integratable with the connective tissue; and said locating step includes positioning the first sheet of the prosthesis between first and second edges of the incision or other opening in the connective tissue and positioning the second sheet of the prosthesis so that it overlaps at least one of the first and second edges of the incision or other opening in the connective tissue. 50. The method of claim 49, wherein the second sheet overlaps both the first and second edges. 51. The method of claim 49, wherein the first and second sheets are tissue infiltratable. 52. The method of claim 49, wherein the first and second sheets form a T-shape. 53. The method of claim 49, wherein the first and second sheets form a V-shape. 54. The method of claim 49, wherein the second sheet of the prosthesis includes a pair of diverging sheets. 55. The method of claim 49, wherein the first sheet of the prosthesis includes a pair of diverging sheets. 56. The method of claim 49, wherein the prosthesis further includes a third biocompatible, implantable sheet that is integratable with the connective tissue. 57. The method of claim 56, wherein the third sheet is tissue infiltratable. 58. The method of claim 57, wherein the third sheet of the prosthesis includes a pair of diverging sheets. 59. The method of claim 56, wherein the first, second and third sheets form an I-shape. 60. The method of claim 56, wherein the first, second and third sheets form an X-shape. 61. The method of claim 56, wherein the second sheet of the prosthesis extends along a first end of the first sheet of the prosthesis, and the third sheet of the prosthesis extends along a second end of the first sheet of the prosthesis. 62. The method of claim 49, wherein the second sheet of the prosthesis extends transversely to the first sheet of the prosthesis. 63. The method of claim 56, wherein the third sheet of the prosthesis extends transversely to the first sheet of the prosthesis. 64. The method of claim 56, wherein each of the second sheet and the third sheet of the prosthesis extend transversely to the first sheet of the prosthesis. 65. The method of claim 49, wherein at least one of the first and second sheets is resorbable. 66. The method of claim 49, wherein both of the first and second sheets are resorbable. 67. The method of claim 56, wherein each of the first, second and third sheets are resorbable. 68. The method of claim 49, wherein the first and second sheets have substantially a same thickness. 69. The method of claim 56, wherein the first, second and third sheets have substantially a same thickness. 70. The method of claim 49, wherein each of the first and second sheets is planar. 71. The method of claim 56, wherein each of the first, second and third sheets is planar. 72. The method of claim 41, wherein the anatomical area is a hernia. 73. The method of claim 41, wherein the connective tissue is beneath dermis and subcutaneous fat. 74. The method of claim 41, wherein the connective tissue is located in an abdominal wall. 75. The method of claim 49, wherein the first sheet has a length and a height, the length of the first sheet corresponding to the length of the incision or other opening in the connective tissue, and the height of the first sheet corresponding to the depth of the incision or other opening in the connective tissue. 76. The method of claim 49, wherein the second sheet has a length and a width, the length of the second sheet corresponding to the length of the incision or other opening in the connective tissue, and the width of the second sheet being sufficient to overlap the first and second edges of the incision or other opening in the connective tissue. 77. The method of claim 49, wherein there is a space between the first and second edges of the incision or other opening in the connective tissue prior to said approximating step, and wherein the width of the second sheet is sufficient to overlap the spaced apart first and second edges of the incision or other opening in the connective tissue. 78. The method of claim 56, wherein the third sheet has a length and a width, the length of the third sheet corresponding to the length of the incision or other opening in the connective tissue, and the width of the third sheet being sufficient to overlap the first and second edges of the incision or other opening in the connective tissue. 79. The method of claim 41, further including, before said locating step, the step of treating, through the incision or opening, the anatomical area. 80. The method of claim 79, wherein said treating step includes repairing a hernia. 81. The method of claim 41, further comprising the step of selectively modifying the size or shape of the prosthesis to fit the incision or other opening in the connective tissue of a specific patient. 82. The method of claim 41, wherein the connective tissue is an aponeurosis. 83. The method of claim 56, wherein the second sheet overlaps a top or front surface of the first and second edges of the incision or other opening in the connective tissue, and the third sheet overlaps a bottom or rear surface of the first and second edges of the incision or other opening in the connective tissue. 84. The prosthesis of claim 49, wherein positioning the second sheet of the prosthesis includes positioning the second sheet of the prosthesis beneath the first and second edges of the incision or other opening in the connective tissue. 85. The prosthesis of claim 49, wherein positioning the second sheet of the prosthesis includes positioning the second sheet of the prosthesis above the first and second edges of the incision or other opening in the connective tissue. |
<SOH> FIELD OF INVENTION <EOH>This invention is a prosthesis that can be implanted in surgical closures of the abdominal wall, characterized by tissue integration and stimulation of the connective tissue response in the center of wound scarring, increasing its resistance and thus preventing hernias from forming in the incision, to be used primarily in the field of abdominal surgery. |
<SOH> SUMMARY OF INVENTION <EOH>In order to increase the resistance of scars on the abdominal wall and reduce the likelihood of incisional hernias, a wall prosthesis that can be implanted in the center of a wound to reinforce abdominal wall closure has been designed, and is the subject of the present invention. In effect, the invention is tantamount to a new concept in wall prostheses that has not been used until now. This new prosthesis has been conceived for direct use at the center of connective scarring of the abdominal wall, in whose cavity is anchored the connective tissue of each side of the wound, in addition to stimulating formation of the same, which in turn increases the wound's resistance to traction, in terms of both time, as said resistance is achieved more quickly, and final results, as the final resistance achieved is superior. To these ends, the proposed prosthesis is made from synthetic material and arranged in a geometric shape in the form of sheets that converge in dihedral angles. The sheets or planes are made in porous form, using braided or perforated wire or any other method, with large pores that allow fibroblasts and collagenous fibers to proliferate, completely engulfing the prosthesis in their cavity. One of the planes is introduced into the center of scarring between the two aponeurotic surfaces to be joined, where it functions as a guide for placement and stimulation of connective tissue proliferation. The other plane or planes of the prosthesis, perpendicular to the first one, overlap the aponeurotic edges of the section, either above the two sides, beneath them, or in both positions, where they are enclosed by the connective tissue, which they then stimulate as they proliferate. The resulting proliferation of tissue surrounding the prosthesis, in and around the center of scarring, provides stress resistance greater than that obtained in standard closures performed with sutures without the use of the prosthesis, in terms of both final results and promptness of healing, greatly reducing the likelihood of hernia due to badly healed wounds. Because of its novel placement at the center of scarring of the aponeurotic layer of the wound and the form in which it works, the wall prosthesis that can be implanted in the center of a wound to reinforce abdominal wall closure constitutes an advance in the state of the technique. |
Selective metal removal process for metallized retro-reflective and holographic films and radio frequency devices made therewith |
A method for selectively removing metal from a metallized substrate (e.g., a metallized polymer film) and the formation of devices thereby are provided. Th method involves selectively exposing the metallized surface to a demetallizing (i.e., an oxidizing) chemical solution. The metallized layer can be selectively exposed to the demetallizing solution using a flexographic printing process wherein printing rollers are used to transfer the demetallizing solution to the metallized surface. An identification device including, for example, a holographic, retro-reflective, or other metallized material and a radio-frequency transponder are also provided. The radio-frequency transponder includes an RF chip and an antenna in electrical communication with the chip. The identification device including the holographic image allows both electronic identification through the reading or identification data stored in the chip and optical identification via the holographic image. |
1. An identification device, comprising: a base layer; a radio-frequency (RF) transponder comprising an RF chip and an antenna disposed on the base layer, wherein the antenna is in electrical communication with the chip; and a discontinuous metallized region; wherein the discontinuous metallized region enables the RF transponder is to transmit and receive information at radio frequencies. 2. The device of claim 1, wherein the discontinuous metallized region comprises an image. 3. The device of claim 2, wherein the image is a holographic image. 4. The device of claim 1, wherein the discontinuous metallized region comprises a retro-reflective layer. 5. The device of claim 1, wherein the discontinuous metallized region comprises a holographic image and wherein the holographic image and the antenna form a single metal layer. 6. The device of claim 1, wherein the base layer has at least one side, and wherein the antenna and the discontinuous metallized region are located on the same side of the base layer. 7. The device of claim 1, wherein the base layer has at least a first side and a second side, the first side being opposite the second side, and wherein the antenna and the discontinuous metallized region are located on opposite sides of the base layer. 8. The device of claim 1, wherein the base layer has at least a first side and a second side, the first side being opposite the second side, and wherein a first part of the antenna and the discontinuous metallized region are located on the first side, and a second part of the antenna is located on the second side of the base layer, and wherein the first part of the antenna is electrically connected to the second part of the antenna. 9. The device of claim 1, wherein the device comprises an upper metal layer positioned above the base layer and a lower metal layer positioned below the base layer, wherein a first part of the antenna is formed on the upper metal layer and a second part of the antenna is formed on the lower metal layer, the device further comprising a through contact connecting the first part of the antenna to the second part of the antenna. 10. The device of claim 1, wherein the discontinuous metallized region is in electrical communication with the antenna. 11. The device of claim 10, wherein the discontinuous metallized region comprises an electronic commutation element. 12. The device of claim 10, wherein the discontinuous metallized region comprises a capacitor. 13. The device of claim 1, wherein the discontinuous metallized region comprises a plurality of electrically isolated holographic regions. 14. The device of claim 1, wherein the base layer is an electrically conductive layer. 15. The device of claim 14, wherein an isolation layer is formed on the base layer. 16. The device of claim 15, wherein the radio frequency (RF) chip is mounted on the isolation layer. 17. The device of claim 15, wherein the base layer includes a depressed region, and wherein the isolation layer is formed in the depressed region. 18. The device of claim 1, wherein the base layer has at least one side, and wherein the antenna and the discontinuous metallized region are formed on the same side of the base layer in discrete, non-overlapping areas. 19. The device of claim 1, wherein the antenna comprises a conductive wire inlaid in a polymer layer. 20. The device of claim 1, wherein the device is selected from the group consisting of a decal, a license plate, and an identification card. 21. The device of claim 1, wherein the discontinuous metallized region comprises a square grid pattern. 22. The device of claim 21, wherein the squares in the square grid pattern have a length of about 5 mm or less. 23. The device of claim 21, wherein the squares in the square grid pattern have a length of about 3 mm or less. 24. A method of forming a pattern in a metallized region, the method comprising: transferring a metal etching solution to portions of an exposed surface of the metallized region using a printing process; allowing the etching solution to react with the metallized region to selectively demetallize the surface; and washing the selectively demetallized surface. 25. The method of claim 24, wherein the printing process is selected from the group consisting of a flexographic printing process, an offset printing process and a screen printing process. 26. The method of claim 24, wherein the metal etching solution is an aqueous solution of sodium hydroxide. 27. The method of claim 26, wherein the metal etching solution further comprises ethylene glycol. 28. A method of making an identification device comprising a base layer and a plurality of metallized regions disposed thereon, the method comprising: forming an antenna in a first metallized region; and forming a holographic image in a second metallized region; wherein the antenna is formed by a method comprising: transferring a metal etching solution to portions of an exposed surface of the metallized layer using a printing process; allowing the etching solution to react with the metal to selectively demetallize the surface; and washing the selectively demetallized surface. 29. The method of claim 28, wherein the first and second metallized regions form a single metal layer. 30. A method of making a radio-frequency (RF) identification device comprising: forming an antenna on a base layer; and mounting an radio frequency (RF) chip on the base layer in electrical communication with the antenna to form an RF transponder; wherein the antenna is formed by selective de-metallization of a continuous metallized layer or by partial deposition of a discontinuous metallized layer. 31. The method of claim 30, wherein the antenna is formed by partial deposition of a discontinuous metallized layer by a method selected from the group consisting of chemical deposition, electrical deposition, sputtering and vapor coating. 32. The method of claim 30, further comprising: forming a discontinuous metallized region on the base layer, wherein the discontinuous metallized region comprises a retro-reflective material or a holographic material. 33. The method of claim 32, wherein the discontinuous metallized region and the antenna are formed simultaneously. 34. The method of claim 30, wherein the antenna is formed by selective de-metallization of a continuous metallized layer, and wherein selective demetallization comprises: transferring a metal etching solution to portions of an exposed surface of the continuous metallized layer using a printing process; allowing the etching solution to react with the metal; and washing the exposed surface of the metallized layer. 35. A method of making an identification device comprising a base layer and a metallized retro-reflective layer, the method comprising: forming a discontinuous retro-reflective layer on the base layer, forming an antenna on the base layer, and mounting a radio frequency (RF) chip on the base layer; wherein the chip the and the antenna are in electrical communication to form an RF transponder, and wherein the discontinuous retro-reflective layer retains retro-reflective properties while allowing the RF transponder to transmit and receive information at radio frequencies. 36. The method of claim 35, wherein the base layer has at least one side, and wherein the antenna and the retro-reflective layer are formed on the same side of the base layer in discrete, non-overlapping regions. 37. The method of claim 35, wherein forming an antenna comprises: forming an inlaid antenna by embedding a conductive wire in a polymer layer; and affixing the inlaid antenna to the base layer. 38. The method of claim 37, wherein the inlaid antenna is affixed to a demetallized region of the retro-reflective layer 39. The method of claim 37, wherein the inlaid antenna is provided with an adhesive layer and wherein affixing an antenna further comprises: adhesively bonding the antenna to the device through the adhesive layer. 40. The method of claim 38, wherein the adhesive is selected from a group consisting of an auto-adhesive and a pressure sensitive adhesive. 41. The method of claim 37, wherein the polymer layer comprises polyvinyl chloride (PVC) or polyethylene terephthalate (PET). 42. The method of claim 36, wherein the radio frequency (RF) chip is mounted on the same side of the base layer as the antenna and retro-reflective layer. 43. The method of claim 35, further comprising: forming a depressed region in the base layer, and forming an isolation layer in the depressed region; wherein the radio frequency (RF) chip is mounted on the isolation layer. 44. The method of claim 43, wherein the antenna is formed on top of the depressed region. 45. The method of claim 43, wherein the isolation layer comprises a ferrite composite. 46. The method of claim 35, further comprising: over-printing a design on the surface of the retro-reflective material. 47. The method of claim 35, wherein forming a discontinuous retro-reflective layer comprises: transferring a metal etching solution to portions of an exposed surface of a continuous metallized retro-reflective layer using a printing process; allowing the etching solution to react with the metal of the retro-reflective layer; and washing the exposed surface of the metallized retro-reflective layer. 48. The method of claim 47, wherein the metal etching solution is transferred to the exposed surface of the metallized retro-reflective layer as a plurality of lines arranged in a square pattern. 49. The method of claim 48, wherein the lines are spaced apart about 5 mm or less. 50. The method of claim 48, wherein the lines are spaced apart about 3 mm or less. 51. The method of claim 35, wherein the base layer comprises a polymeric material and wherein forming an antenna comprises: forming an inlaid antenna by embedding a conductive wire in the base layer. 52. The method of claim 51, wherein a demetallized portion of the retro-reflective layer is applied over the antenna layer. 53. The device of claim 1, wherein the discontinuous metallized layer is directly disposed on at least one surface of the base layer. 54. The device of claim 1, wherein the discontinuous metallized layer comprises at least one metal selected from the group consisting of aluminum, aluminum alloys, nickel, silver and copper. 55. The device of claim 1, wherein the discontinuous metallized layer is formed by a process selected from a group consisting of a chemical deposition, electrical deposition, sputtering and vapor coating. 56. The device of claim 1, wherein the antenna is formed by selective demetallization of a continuous metallized layer or by partial deposition of a discontinuous metallized layer. 57. The device of claim 56, wherein the antenna is formed by partial deposition of a discontinuous metallized layer by a method selected from a group consisting of chemical deposition, electrical deposition, sputtering and vapor coating. 58. The device of claim 1, wherein the antenna comprises at least one metal selected from a group consisting of aluminum, aluminum alloy, nickel, silver and copper. 59. The device of claim 58, wherein the antenna comprises an amorphous metal. 60. The device of claim 1, wherein the thickness of the antenna is between about 0.5 and 3 microns. 61. The device of claim 1, wherein the thickness of the base layer is between about 5 and 3,000 microns. 62. An identification device, comprising: a base layer; and a radio-frequency (RF) transponder comprising an RF chip and an antenna disposed on the base layer, wherein the antenna is in electrical communication with the chip; wherein the antenna is formed by selective de-metallization of a continuous metallized layer or by partial deposition of a discontinuous metallized layer. 63. The device of claim 62, wherein the antenna comprises at least one metal selected from a group consisting of aluminum, aluminum alloy, nickel, silver and copper. 64. The device of claim 62, wherein the antenna comprises an amorphous metal. 65. The device of claim 62, wherein the thickness of the antenna is between about 0.5 and 3 microns. 66. The device of claim 62, wherein the thickness of the base layer is between about 5 and 3,000 microns. |
<SOH> BACKGROUND OF THE INVENTION <EOH>1. Field of the Invention The present invention relates generally to a process for selectively removing metallic material from a metallized film and, in particular, to the removal of metallic material from a metallized polymeric film using a printing method such as flexographic printing. The film can be a reflective film (e.g., a retro-reflective film) or a holographic film that can be used, for example, in an identification device comprising a radio frequency (RF) transponder. 2. Background of the Technology Retro-reflective materials can reflect and re-emit incident light in a direction that is parallel to that of the source of the incident light. In other words, retro-reflective materials reflect light directly back toward the source of the light Such materials and devices are widely used in the areas of nighttime transportation and safety. For example, retro-reflective materials are used to identify highway lanes and road signs using the light emitted from vehicle headlights. Retro-reflective materials are also used for the production of car plates, decals and distinctives for all kinds of vehicles and for truck containers, tractors and other applications. Retro-reflective materials have a bright effect under direct light without disturbing human sight Holographic materials have also been used for identification purposes. Since holograms are all but impossible to counterfeit, they are being increasingly used on all types of identification, including driver's licenses, credit cards, bus passes, etc., to increase security. Both retro-reflective and holographic materials typically contain a very high level of metal such as aluminum. Holograms, for example, are typically stamped from metal foils. It is known that metal blocks the transmission and reception of radio frequency (RF) signals because the RF signal is absorbed or distorted by the metal content in the material. As a result, the signal cannot be received by an antenna blocked by metal. Such a blocked signal cannot be used, for example, to activate a connected device. This same blocking effect can occur whether the device is positioned on top of or underneath the metallic material because the distortion and absorption of the RF signal will be affected in either case. Thus, there is a problem in the prior art with regard to using retro-reflective and holographic materials, as well as other materials containing metals, on the surface of devices for receiving RF signals. It would be desirable to incorporate an RF transponder into an identification device comprising a retro-reflective material, a holographic image, or other material containing a metal. The RF transponder could be used for electronic identification. |
<SOH> SUMMARY OF THE INVENTION <EOH>According to a first aspect of the invention, an identification device is provided that includes retro-reflective or holographic materials, or other materials containing metal, and a usable antenna for receiving radio frequency (RF) signals. The identification device comprises: a base layer, an RF transponder comprising a mounted RF chip and an antenna disposed on the base layer, and a metallized region. The metallized region can comprise a holographic image or a ret reflective layer. The antenna is in electrical communication with the chip. According to this aspect of the invention, the metallized region is discontinuous, such that the RF transponder can transmit and receive information at radio frequencies. According to a second aspect of the invention, a method of forming a pattern in a metallized layer is provided. The method comprises: transferring a metal etching solution to portions of an exposed surface of the metallized layer using a printing process; allowing the etching solution to react with the metallized layer to selectively demetallize the surface; and washing the selectively demetallized surface. According to a third aspect of the invention, a method of making an identification device comprising a base layer and at least one metal region disposed thereon is provided. The method comprises: selectively demetallizing a first metal region of the device; forming a holographic image in the first metal region; forming an antenna on the base layer; and mounting an RF chip on the base layer in electrical communication with the antenna to form an RF transponder. According to this aspect of the invention, the selective demetallization of the first metal region allows the RF transponder to transmit and receive information. According to a fourth aspect of the invention, a method of making an identification device comprising a base layer and a metallized retro-reflective layer is provided. The method comprises: forming an antenna on a base layer; and mounting a radio frequency (RF) chip on the base layer in electrical communication with the antenna to form an RF transponder. According to this aspect of the invention, the antenna is formed by selective de-metallization of a continuous metallized layer or by partial deposition of a discontinuous metallized layer. According to a fifth aspect of the invention, an identification device is provided. The device includes a base layer and a radio-frequency (RF) transponder comprising an RF chip and an antenna disposed on the base layer wherein the antenna is in electrical communication with the chip. According to this aspect of the invention, the antenna is formed by selective de-metallization of a continuous metallized layer or by partial deposition of a discontinuous metallized layer. Additional advantages and novel features of the invention will be set forth in part in the description that follows, and in part will become more apparent to those skilled in the art upon examination of the following or upon learning by practice of the invention. |
Quinazolinone derivative |
An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH═ or nitrogen atom; and R represents a C1-C4 alkyl group and so on], or pharmaceutically acceptable salts thereof, has a selective antagonism for the M3 muscarinic receptor and depressant action on the frequency of rhythmic bladder contractions, and it is useful for the treatment of pollakiuria and urinary incontinence. |
1. An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents a group of the formula —CH═ or nitrogen atom; and R represents a fluorine atom, C1-C4 alkyl group, C1-C4 alkoxy group, trifluoromethoxy group or 2,2,2-trifluoroethoxy group], or pharmaceutically acceptable salt thereof. 2. The optically active form of the quinazolinone derivatives described in claim 1, which is (+) form, or pharmaceutically acceptable salt thereof. 3. The optically active form of the quinazolinone derivatives described in claim 1 or 2, wherein Y is a phenyl group and E is a group of the formula —CH═, or pharmaceutically acceptable salt thereof. 4. The optically active form of the quinazolinone derivatives described in claim 1 or 2, wherein Y is a C2-C7 alkyl group and E is a nitrogen atom, or pharmaceutically acceptable salt thereof. 5. The optically active form of the quinazolinone derivatives described in claim 1 or 2, wherein Y is a C3-C7 alkyl group, or pharmaceutically acceptable salt thereof. 6. (+)-3-{1-[3-(2,2,2-trifluoroethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4dihydro-2(1H)-quinazolinone or pharmaceutically acceptable salt thereof. 7. (+)-3-[1-(3-trifluoromethoxybenzyl)piperidin-4-yl]-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or pharmaceutically acceptable salt thereof. 8. (+)-4-isopropyl-3-{1-[(6-methyl-2-pyridinyl)methyl]piperidin-4-yl}-3,4dihydro-2(1H)-quinazolinone or pharmaceutically acceptable salt thereof. 9. (+)-3-[1-(3-trifluoromethoxybenzyl)piperidin-4-yl]-4-phenyl-3,4dihydro-2(1H)-quinazolinone fumarate. 10. A medicament comprising the compound described in any of claims 1 or 6-9 or pharmaceutically acceptable salt thereof. 11. A remedy for treating pollakiuria or urinary incontinence comprising the compound described in any of claims 1 or 6-9 or pharmaceutically acceptable salt thereof as an active ingredient. 12. Use of the compound described in any of claims 1 or 6-9 or pharmaceutically acceptable salt thereof for manufacturing a remedy for treating pollakiuria or urinary incontinence. 13. A method for treating pollakiuria or urinary incontinence which comprises administrating an effective amount of the compound described in any of claims 1 or 6-9 or pharmaceutically acceptable salt thereof to a patient in need. 14. The optically active form of the quinazolinone derivatives described in claim 3, wherein Y is a C3-C7 alkyl group, or pharmaceutically acceptable salt thereof. 15. The optically active form of the quinazolinone derivatives described in claim 4, wherein Y is a C3-C7 alkyl group, or pharmaceutically acceptable salt thereof. |
<SOH> BACKGROUND ART <EOH>Oxybutinin is used as a medicament having an antagonistic action on muscarinic receptors for the treatment of pollakiuria and urinary incontinence, while the medicament is known to be inevitably associated with side effects due to its antagonistic action on muscarinic receptors. There are at least three known subtypes of muscarinic receptors which are the sites of action of anticholinergic drugs, and it has been shown that the M1 receptor is mainly localized in the brain, the M2 receptor in the heart, and the M3 receptor in smooth muscle and the glandular tissue, respectively. Accordingly, when a compound having an antagonistic action on muscarinic receptors is used as a remedy for the treatment of pollakiuria and urinary incontinence, it is considered preferable that the selectivity for the M3 receptor is higher than that for the M1 and M2 receptors, and compounds with a variety of chemical structures, that is selective for the M3 receptor, have been reported. However, dry mouth and mydriasis which are generally-known side effects of anticholinergic drugs result from the antagonistic action on the M3-receptor, and thus it is difficult to eliminate these side effects merely by enhancing the selectivity for the M3 receptor. On the other hand, research and development of non-cholinergic remedies for the treatment of pollakiuria and urinary incontinence, such as α-receptor regulator, potassium channel opener and central muscular relaxtation action, are proceeding, but no medicament having a satisfactory effect has been obtained. Accordingly, it is desired to obtain a compound that has another useful action for the treatment of pollakiuria and urinary incontinence in addition to the antagonistic action on the muscarinic receptor as the compound which can be widely used for the treatment of pollakiuria and urinary incontinence and which can reduce the side effects of anticholinergic medicaments, due to having a plurality of actions. On the other hand, quinazolinone derivatives have been reported as the compound having a selective antagonism for the M3 muscarinic receptor in WO 00/23436. |
Food processing device |
The present invention provides a combination weighing apparatus (1) capable of eliminating the need for memo paper for messages and reminders. A memory (22) of a control unit (20), which comprehensively controls the operation of the combination weighing apparatus (1), is provided with a memo information storage unit (22b) that stores memo information. In addition, the control unit (20) is provided with a retrieval control unit (21a) that retrieves memo information stored in the memo information storage unit (22b), and a display control unit (21b) for displaying the memo information retrieved by the retrieval control unit (21a). Furthermore, a touch screen (30), which is a memo information input means for inputting memo information, is connected, capable of sending and receiving signals, to the control unit (20). |
1. A foodstuffs processing apparatus that performs prescribed processing related to foodstuffs, comprising: foodstuffs processing means for performing a prescribed food processing operation; operation inputting means for inputting operation related to said operation of said foodstuffs processing means; memo information input means for inputting memo information; memo information storage means that stores the memo information inputted through said memo information input means; memo information retrieval means that retrieves said memo information stored in said memo information storage means; and memo information display means that displays said memo information retrieved by said memo information retrieval means. 2. The foodstuffs processing apparatus as recited in claim 1, wherein said memo information input means allows input in a character code input function and a handwriting input function. 3. The foodstuffs processing apparatus as recited in claim 1, wherein said memo information storage means associates and stores as said memo information at least one of the time, error symptoms, error cause, error handling status, and apparatus state after error handling. 4. The foodstuffs processing apparatus as recited in claim 3, wherein said memo information storage means associates and stores said memo information and post-error-handling operation enable/disable information; said foodstuff processing apparatus further comprises: an operation restricting means that restricts operation if operation disabled information is stored. 5. The foodstuffs processing apparatus as recited in claim 1 wherein, said memo information storage means associates and stores said memo information and an operation level that specifies a range in which operations of said foodstuffs processing means can be input in said operation inputting means; and said memo information retrieval means retrieves memo information corresponding to said operation level. 6. The foodstuffs processing apparatus as recited in claim 1, wherein said memo information storage means associates and stores said memo information and a preset number that specifies a foodstuffs item to be processed by said foodstuffs processing means; and said memo information retrieval means retrieves memo information corresponding to said preset number. 7. The foodstuffs processing apparatus as recited in claim 1, wherein said memo information storage means associates and stores said memo information and an identifier that specifies to whom said memo information is directed; and said memo information retrieval means retrieves said memo information corresponding to said identifier. |
<SOH> FIELD OF THE INVENTION <EOH>The present invention relates to an apparatus for foodstuffs processing, such as weighing, packaging, and inspecting. |
Aminoisoxazole derivatives active as kinase inhibitors |
Compounds (I) which are aminoisoxazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders. |
1. A method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of an aminoisoxazole derivative represented by formula (I): wherein R is an optionally substituted 5 or 6 membered heteroaryl group with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur, optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; X is a divalent group selected from —N(R3)— or —O—; Y is a divalent group selected from —CH(R3)—, —CO—, —CONH— or —SO2—, or Y may also be a single bond when R2 is a hydrogen atom or a C3-C6cycloalkyl group; R1 is a hydrogen atom or a group, optionally further substituted, selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl or aryl C1-C6 alkyl, 5 or 6 membered heterocyclyl or heterocyclyl C1-C6 alkyl having from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; the said cycloalkyl, aryl or heterocyclyl groups being optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; R2 and R3 have, each independently, the meanings above reported for R1 or represent an optionally substituted straight or branched C2-C6 alkenyl or alkynyl group; and the pharmaceutically acceptable salts thereof. 2. The method of claim 1 wherein the disease caused by and/or associated with an altered protein kinase activity is a cell proliferative disorder selected from the group consisting of cancer, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders. 3. The method of claim 2 wherein the cancer is selected from carcinoma, squamous cell carcinoma, hematopoietic tumors of lymphoid or myeloid lineage, tumors of mesenchymal origin, tumors of the central and peripheral nervous system, melanoma, seminoma, teratocarcinoma, osteosarcoma, xeroderma pigmentosum, keratoxanthoma, thyroid follicular cancer and Kaposi's sarcoma. 4. The method of claim 1 wherein the cell proliferative disorder is selected from benign prostate hyperplasia, familial adenomatosis, polyposis, neuro-fibromatosis, psoriasis, vascular smooth cell proliferation associated with atherosclerosis, pulmonary fibrosis, arthritis glomerulonephritis and post-surgical stenosis and restenosis. 5. The method of claim 1 which provides tumor angiogenesis and metastasis inhibition. 6. The method of claim 1 further comprising subjecting the mammal in need thereof to a radiation therapy or chemotherapy regimen in combination with at least one cytostatic or cytotoxic agent. 7. The method of claim 1 wherein the mammal in need thereof is a human. 8. The method of claim 1 wherein, within the compounds of formula (I), Y is a single bond, R2 is a hydrogen atom, and R, R1 and X are as above defined. 9. The method of claim 1 wherein, within the compounds of formula (I), Y is a —CO— group and R, R1, R2 and X are as above defined. 10. The method of claim 1 wherein, within the compounds of formula (I), Y is a —CONH— group and R, R1, R2 and X are as above defined. 11. The method of claim 1 wherein, within the compounds of formula (I), Y is a —SO2— group and R, R1, R2 and X are as above defined. 12. A method for inhibiting protein kinase activity which comprises contacting the said kinase with an effective amount of a compound as defined in claim 1. 13. An aminoisoxazole derivative represented by formula (I) wherein R is an optionally substituted 5 or 6 membered heteroaryl group with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur, optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; X is a divalent group selected from —N(R3)— or —O—; Y is a divalent group selected from —CH(R3)—, —CO—, —CONH— or —SO2—, or Y may also be a single bond when R2 is a hydrogen atom or a C3-C6 cycloalkyl group; R1 is a hydrogen atom or a group, optionally further substituted, selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl or aryl C1-C6 alkyl, 5 or 6 membered heterocyclyl or heterocyclyl C1-C6 alkyl having from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; the said cycloalkyl, aryl or heterocyclyl groups being optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; R2 and R3 have, each independently, the meanings above reported for R1 or represent an optionally substituted straight or branched C2-C6 alkenyl or alkynyl group; and the pharmaceutically acceptable salts thereof; provided that: a) R is other than nitrofuryl; and b) 5-amino-3-(2-aminofuryl-5-yl)-4-methoxycarbonyl-isoxazole and 5-amino-4-ethoxycarbonyl-3-(indol-3-yl)-isoxazole, optionally further substituted at the indole moiety, being excluded. 14. A compound of formula (I) according to claim 13 wherein Y is a single bond, R2 is a hydrogen atom, and R, R1 and X are as defined in claim 13. 15. The compound of claim 14 wherein X is a —N(R3)— group and R3 is as defined in claim 13. 16. A compound of formula (I) according to claim 13 wherein Y is a —CO— group and R, R1, R2 and X are as defined in claim 13. 17. The compound of claim 16 wherein X is —N(R3)— and R1 and R3 are both hydrogen atoms. 18. A compound of formula (I) according to claim 13 wherein Y is a —CONH— group and R, R1, R2 and X are as above defined. 19. The compound of claim 18 wherein X is —N(R3)— and R1 and R3 are both hydrogen atoms. 20. A compound of formula (I) according to claim 13 wherein Y is a —SO2— group and R, R1, R2 and X are as above defined. 21. The compound of claim 20 wherein X is —N(R3)— and R1 and R3 are both hydrogen atoms. 22. A compound of formula (I) according to claim 13 wherein any heteroaryl or heterocyclyl group has 1 or 2 heteroatoms selected among nitrogen, oxygen or sulfur. 23. A compound of formula (I) as defined in claim 13, optionally in the form of a pharmaceutically acceptable salt, selected from: 1) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 2) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 3) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 4) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 5) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 6) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 7) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 8) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 9) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid butylamide; 10) 5-acetylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 11) methyl 5-amino-3-(2-pyridinyl)-4-isoxazolecarboxylate; 12) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 13) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 14) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid benzylamide; 15) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 16) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 17) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 18) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 19) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 20) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid benzylamide; 21) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 22) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 23) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 24) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 25) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 26) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid benzylamide; 27) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 28) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 29) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 30) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 31) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 32) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid benzylamide; 33) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 34) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 35) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 36) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 37) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 38) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid benzylamide; 39) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 40) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 41) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 42) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 43) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 44) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid benzylamide; 45) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 46) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 47) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 48) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 49) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 50) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 51) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 52) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid benzhydryl-amide; 53) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (2,4-difluoro-phenyl)-amide; 54) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (4-chloro-phenyl)-amide; 55) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid benzylamide; 56) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (5,6,7,8-tetrahydro-naphthalen-1-yl)-amide; 57) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (4-fluoro-phenyl)-amide; 58) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid benzhydryl-amide; 59) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 60) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid p-tolylamide; 61) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 62) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 63) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 64) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 65) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 66) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid p-tolylamide; 67) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 68) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 69) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 70) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 71) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 72) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid p-tolylamide; 73) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 74) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 75) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 76) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 77) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 78) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid p-tolylamide; 79) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 80) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 81) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 82) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 83) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 84) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid p-tolylamide; 85) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 86) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 87) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 88) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 89) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 90) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid p-tolylamide; 91) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 92) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 93) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 94) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 95) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 96) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid p-tolylamide; 97) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 98) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 99) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid indan-5-ylamide; 100) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 101) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid naphthalen-1-ylamide; 102) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid p-tolylamide; 103) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (3-benzyloxy-phenyl)-amide; 104) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid 2,4-dimethoxy-benzylamide; 105) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid indan-5-ylamide; 106) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (3,5-dimethoxy-phenyl)-amide; 107) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 108) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3,4,5-trimethoxy-phenyl)-amide; 109) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (2-methoxy-5-trifluoromethyl-phenyl)-amide; 110) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 111) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 112) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 113) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (3,4,5-trimethoxy-phenyl)-amide; 114) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 115) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 116) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 117) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3,4,5-trimethoxy-phenyl)-amide; 118) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2-methoxy-5-trifluoromethyl-phenyl)-amide; 119) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 120) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 121) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 122) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 123) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 124) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 125) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3,4,5-trimethoxy-phenyl)-amide; 126) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (2-methoxy-5-trifluoromethyl-phenyl)-amide; 127) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 128) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 129) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 130) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 131) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 132) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 133) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2-methoxy-5-trifluoromethyl-phenyl)-amide; 134) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 135) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 136) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (3,4,5-trimethoxy-phenyl)-amide; 137) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid quinolin-8-ylamide; 138) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (4-tert-butyl-phenyl)-amide; 139) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 140) 3-[(5-amino-3-pyridin-4-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 141) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 142) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 143) 3-[(5-amino-3-thiophen-2-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 144) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 145) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-dimethylamino-phenyl)-amide; 146) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 147) 3-[(5-amino-3-thiophen-3-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 148) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 149) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-dimethylamino-phenyl)-amide; 150) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 151) 3-[(5-amino-3-thiazol-2-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 152) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 153) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-dimethylamino-phenyl)-amide; 154) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 155) 3-[(5-amino-3-pyridin-2-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 156) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 157) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (4-dimethylamino-phenyl)-amide; 158) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 159) 3-[(5-amino-3-pyridin-3-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 160) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 161) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 162) 3-{[5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carbonyl]-amino}-benzoic acid ethyl ester; 163) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 164) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (4-dimethylamino-phenyl)-amide; 165) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (2-benzyl-phenyl)-amide; 166) 3-[(5-amino-3-quinolin-2-yl-isoxazole-4-carbonyl)-amino]-benzoic acid ethyl ester; 167) 5-amino-3-quinolin-2-yl-isoxazole-4-carboxylic acid (4-trifluoromethoxy-phenyl)-amide; 168) 5-amino-3-pyridin-2-yl-isoxazole-4-phenyl carboxamide; 169) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 170) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (pyridin-4-ylmethyl)-amide; 171) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 172) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)-amide; 173) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)-amide; 174) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 175) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 176) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 177) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 178) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 179) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (pyridin-4-ylmethyl)-amide; 180) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid phenylamide; 181) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid phenylamide; 182) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3-methoxy-propyl)-amide; 183) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 184) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid phenylamide; 185) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 186) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3-phenoxy-phenyl)-amide; 187) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 188) 4-{[5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carbonyl]-amino}-piperidine-1-carboxylic acid ethyl ester; 189) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide; 190) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid phenylamide; 191) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid 2-methoxy-benzylamide; 192) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid 4-chloro-benzylamide; 193) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid 2-methoxy-benzylamide; 194) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid 4-fluoro-benzylamide; 195) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3,4-dimethyl-phenyl)-amide; 196) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (2-dimethylamino-ethyl)-amide; 197) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 198) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 199) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-methoxy-propyl)-amide; 200) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 201) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 202) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 203) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-butoxy-phenyl)-amide; 204) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (4-butoxy-phenyl)-amide; 205) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (1-ethyl-propyl)-amide; 206) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3,4-dimethyl-phenyl)-amide; 207) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-fluoro-2-methyl-phenyl)-amide; 208) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid [4-(acetyl-methyl-amino)-phenyl]-amide; 209) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid 2-methoxy-benzylamide; 210) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid [2-(4-methoxy-phenyl)-ethyl]-amide; 211) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3-methoxy-propyl)-amide; 212) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid 4-chloro-benzylamide; 213) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid [2-(4-methoxy-phenyl)-ethyl]-amide; 214) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-phenoxy-phenyl)-amide; 215) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (pyridin-4-ylmethyl)-amide; 216) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)-amide; 217) 5-amino-3-pyridin-3-yl-isoxazole-4-carboxylic acid phenylamide; 218) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (2-methylsulfanyl-phenyl)-amide; 219) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (3-chloro-4-methyl-phenyl)-amide; 220) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-chloro-4-methyl-phenyl)-amide; 221) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 222) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 223) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (3-trifluoromethyl-phenyl)-amide; 224) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (3-methoxy-propyl)-amide; 225) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid cyclopropylamide; 226) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-trifluoromethyl-phenyl)-amide; 227) 4-[(5-amino-3-thiophen-3-yl-isoxazole-4-carbonyl)-amino]-piperidine-1-carboxylic acid ethyl ester; 228) 4-[(5-amino-3-pyridin-2-yl-isoxazole-4-carbonyl)-amino]-piperidine-1-carboxylic acid ethyl ester; 229) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)-amide; 230) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid [2-(4-methoxy-phenyl)-ethyl]-amide; 231) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (furan-2-ylmethyl)-amide; 232) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (furan-2-ylmethyl)-amide; 233) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (furan-2-ylmethyl)-amide; 234) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 235) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 236) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 237) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (9H-fluoren-2-yl)-amide; 238) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3-trifluoromethyl-phenyl)-amide; 239) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid 4-fluoro-benzylamide; 240) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-butoxy-phenyl)-amide; 241) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-difluoromethoxy-phenyl)-amide; 242) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid [4-(toluene-4-sulfonylamino)-phenyl]-amide; 243) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (2-methylsulfanyl-phenyl)-amide; 244) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid phenylamide; 245) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (1-ethyl-propyl)-amide; 246) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 247) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid [4-(toluene-4-sulfonylamino)-phenyl]-amide; 248) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide; 249) 5-amino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid (3-chloro-4-methyl-phenyl)-amide; 250) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide; 251) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (2-dimethylamino-ethyl)-amide; 252) 5-amino-3-thiazol-2-yl-isoxazole-4-carboxylic acid (3-trifluoromethyl-phenyl)-amide; 253) 5-amino-3-thiophen-2-yl-isoxazole-4-carboxylic acid (pyridin-4-ylmethyl)-amide; 254) 5-amino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-morpholin-4-yl-phenyl)-amide; 255) 5-amino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (3-methoxy-phenyl)-amide; 256) 5-amino-3-pyridin-4-yl-isoxazole-4-carboxylic acid (4-butoxy-phenyl)-amide; 257) 5-benzoylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid phenylamide; 258) 5-phenylacetylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid butylamide; 259) 5-(4-methyl-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 260) 5-(4-chloro-butyrylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 261) 5-(4-tert-butyl-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 262) 5-pentanoylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 263) 5-(4-methyl-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 264) 5-(4-chloro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 265) 5-pentanoylamino-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 266) 5-(3-phenyl-propionylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 267) 5-(4-tert-butyl-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 268) 5-pentanoylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 269) 5-(3-phenyl-propionylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 270) 5-(4-methyl-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 271) 5-(4-tert-butyl-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 272) 5-pentanoylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 273) 5-(3-phenyl-propionylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 274) 5-(4-chloro-butyrylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 275) 5-(4-tert-butyl-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 276) 5-(4-chloro-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 277) 5-(3-phenyl-propionylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 278) 5-(4-methyl-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 279) 5-(4-tert-butyl-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 280) 5-(4-chloro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 281) 5-pentanoylamino-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 282) 5-(4-tert-butyl-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 283) 5-(4-chloro-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 284) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-pentanoylamino-isoxazole-4-carboxylic acid amide; 285) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(3-phenyl-propionylamino)-isoxazole-4-carboxylic acid amide; 286) 5-(4-chloro-butyrylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 287) 5-pentanoylamino-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 288) 5-(3-phenyl-propionylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 289) 5-(3-fluoro-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 290) 5-(3-methoxy-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 291) 3-pyridin-2-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 292) 5-(3-fluoro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 293) 5-(2-methoxy-acetylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 294) 5-benzoylamino-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 295) 5-(3-methoxy-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 296) 3-pyridin-4-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 297) 5-(3-bromo-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 298) 5-(3-fluoro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 299) 5-(2-methoxy-acetylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 300) 5-benzoylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 301) 5-(3-methoxy-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 302) 3-thiophen-2-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 303) 5-(2-methoxy-acetylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 304) 5-benzoylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 305) 5-(3-methoxy-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 306) 3-thiophen-3-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 307) 5-(2-methoxy-acetylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 308) 5-benzoylamino-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 309) 5-(3-methoxy-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 310) 3-thiazol-2-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 311) 5-(3-bromo-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 312) 5-(2-methoxy-acetylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 313) 5-(3-methoxy-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 314) 3-pyridin-3-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 315) 5-(3-bromo-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 316) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(3-fluoro-benzoylamino)-isoxazole-4-carboxylic acid amide; 317) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(2-methoxy-acetylamino)-isoxazole-4-carboxylic acid amide; 318) 5-(3-bromo-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 319) 3-quinolin-2-yl-5-(4-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 320) 5-(cyclopropanecarbonyl-amino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 321) 5-(2-phenoxy-acetylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 322) 5-(2-chloro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 323) 5-(cyclopropanecarbonyl-amino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 324) 5-(3-methyl-but-2-enoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 325) 5-(2,4-difluoro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 326) 5-[2-(3-methoxy-phenyl)-acetylamino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 327) 5-(2-phenoxy-acetylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 328) 5-(2-chloro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 329) 5-(cyclopropanecarbonyl-amino)-3-thiopheh-2-yl-isoxazole-4-carboxylic acid amide; 330) 5-(3-methyl-but-2-enoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 331) 5-(2,4-difluoro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 332) 5-[2-(3-methoxy-phenyl)-acetylamino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 333) 5-(2-chloro-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 334) 5-(cyclopropanecarbonyl-amino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 335) 5-(3-methyl-but-2-enoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 336) 5-(2,4-difluoro-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 337) 5-(2-phenoxy-acetylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 338) 5-(cyclopropanecarbonyl-amino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 339) 5-(3-methyl-but-2-enoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 340) 5-(2,4-difluoro-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 341) 5-(2-phenoxy-acetylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 342) 5-(2-chloro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 343) 5-(cyclopropanecarbonyl-amino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 344) 5-(2,4-difluoro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 345) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(2-phenoxy-acetylamino)-isoxazole-4-carboxylic acid amide; 346) 5-(2-chloro-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 347) 5-(cyclopropanecarbonyl-amino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 348) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(3-methyl-but-2-enoylamino)-isoxazole-4-carboxylic acid amide; 349) 5-(2,4-difluoro-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 350) 5-(cyclopropanecarbonyl-amino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 351) 5-(4-fluoro-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 352) 3-pyridin-2-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 353) 5-(2-methyl-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 354) 5-(4-ethyl-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 355) 5-[(naphthalene-1-carbonyl)-amino]-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 356) 5-(4-fluoro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 357) 3-pyridin-4-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 358) 5-(2-methyl-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 359) 3-pyridin-4-yl-5-(3-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 360) 5-(4-ethyl-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 361) 5-[(naphthalene-1-carbonyl)-amino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 362) 5-(4-fluoro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 363) 3-thiophen-2-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 364) 5-(2-methyl-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 365) 3-thiophen-2-yl-5-(3-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 366) 5-(4-ethyl-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 367) 5-[(naphthalene-1-carbonyl)-amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 368) 5-(4-fluoro-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 369) 3-thiophen-3-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 370) 5-(2-methyl-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 371) 3-thiophen-3-yl-5-(3-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 372) 5-(4-ethyl-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 373) 5-[(naphthalene-1-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 374) 5-(4-fluoro-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 375) 3-thiazol-2-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 376) 5-(2-methyl-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 377) 3-thiazol-2-yl-5-(3-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 378) 5-(4-ethyl-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 379) 5-(4-fluoro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 380) 3-pyridin-3-yl-5-(4-trifluoromethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 381) 3-pyridin-3-yl-5-(3-trifluoromethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 382) 5-(2-methyl-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 383) 5-(4-ethyl-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 384) 5-[(naphthalene-1-carbonyl)-amino]-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 385) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(4-fluoro-benzoylamino)-isoxazole-4-carboxylic acid amide; 386) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(2-methyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 387) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(4-ethyl-benzoylamino)-isoxazole-4-carboxylic acid amide; 388) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-[(naphthalene-1-carbonyl)-amino]-isoxazole-4-carboxylic acid amide; 389) 5-(2-fluoro-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 390) 5-(3-methyl-benzoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 391) 5-[2-(4-fluoro-phenyl)-acetylamino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 392) 5-(3,5-difluoro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 393) 5-(3-chloro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 394) 5-(2-fluoro-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 395) 5-(3-methyl-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 396) 5-(3,5-difluoro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 397) 5-(3-chloro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 398) 5-(3,5-difluoro-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 399) 5-(3-methyl-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 400) 5-(3-chloro-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 401) 5-(3-chloro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 402) 5-(2-fluoro-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 403) 5-(3-methyl-benzoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 404) 5-(3-chloro-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 405) 5-butyrylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 406) 5-[(E)-(3-phenyl-acryloyl)amino]-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 407) 5-(3,3-dimethyl-butyrylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 408) 5-(2-chloro-2-phenyl-acetylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 409) 5-butyrylamino-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 410) 5-[(biphenyl-4-carbonyl)-amino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 411) 5-(4-chloromethyl-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 412) 3-pyridin-4-yl-5-(3,4,5-trimethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 413) 5-[(E)-(3-phenyl-acryloyl)amino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 414) 5-(3,3-dimethyl-butyrylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 415) 5-(2-chloro-2-phenyl-acetylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 416) 5-(4-nitro-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 417) 5-butyrylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 418) 5-[(biphenyl-4-carbonyl)-amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 419) 5-(4-chloromethyl-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 420) 3-thiophen-2-yl-5-(3,4,5-trimethoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 421) 5-[(E)-(3-phenyl-acryloyl)amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 422) 5-(3,3-dimethyl-butyrylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 423) 5-(2-chloro-2-phenyl-acetylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 424) 5-butyrylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 425) 5-(3,3-dimethyl-butyrylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 426) 5-(4-chloromethyl-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 427) 5-(3,3-dimethyl-butyrylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 428) 5-(3,3-dimethyl-butyrylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 429) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-[(E)-(3-phenyl-acryloyl)amino]-isoxazole-4-carboxylic acid amide; 430) 5-butyrylamino-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 431) 5-(3,3-dimethyl-butyrylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 432) 5-butyrylamino-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 433) 5-(3,3-dimethyl-butyrylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 434) 5-[(furan-2-carbonyl)-amino]-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 435) 5-[(naphthalene-2-carbonyl)-amino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 436) 5-(4-methoxy-benzoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 437) 5-[(furan-2-carbonyl)-amino]-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 438) 5-(3-cyclopentyl-propionylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 439) 5-[(naphthalene-2-carbonyl)-amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 440) 5-(4-methoxy-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 441) 5-(2-benzyloxy-acetylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 442) 5-(2,4-dimethoxy-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 443) 5-[(furan-2-carbonyl)-amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 444) 5-(3-cyclopentyl-propionylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 445) 5-(4-bromo-benzoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 446) 5-[(naphthalene-2-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 447) 5-(4-methoxy-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 448) 5-(2,4-dimethoxy-benzoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 449) 5-[(furan-2-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 450) 5-(3-cyclopentyl-propionylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 451) 5-(4-methoxy-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 452) 5-(2,4-dimethoxy-benzoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 453) 5-[(furan-2-carbonyl)-amino]-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 454) 5-(3-cyclopentyl-propionylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 455) 5-[(furan-2-carbonyl)-amino]-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 456) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(4-methoxy-benzoylamino)-isoxazole-4-carboxylic acid amide; 457) 5-(2,4-dimethoxy-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 458) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-[(furan-2-carbonyl)-amino]-isoxazole-4-carboxylic acid amide; 459) 5-(3-cyclopentyl-propionylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 460) 5-(3,4-dimethoxy-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 461) 5-(4-bromo-benzoylamino)-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 462) 5-(3-cyclopentyl-propionylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 463) 5-(2-ethyl-butyrylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 464) 5-(2-propyl-pentanoylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 465) 5-(3-methyl-butyrylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 466) 5-[(benzo[1,3]dioxole-5-carbonyl)-amino·-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 467) 5-(2-ethyl-butyrylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 468) 5-(2-propyl-pentanoylamino)-3-pyridin-4-yl-isoxazole-4-carboxylic acid amide; 469) 5-(3-methyl-butyrylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 470) 5-[(benzo[1,3]dioxole-5-carbonyl)-amino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 471) 5-(2-ethyl-butyrylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 472) 5-(2-propyl-pentanoylamino)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 473) 5-[2-(3,4-dimethoxy-phenyl)-acetylamino]-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 474) 5-(3-methyl-butyrylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 475) 5-[(benzo[1,3]dioxole-5-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 476) 5-(2-ethyl-butyrylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 477) 5-(2-propyl-pentanoylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 478) 5-(3-methyl-butyrylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 479) 5-[(benzo[1,3]dioxole-5-carbonyl)-amino]-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 480) 5-(2-ethyl-butyrylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 481) 5-(2-propyl-pentanoylamino)-3-thiazol-2-yl-isoxazole-4-carboxylic acid amide; 482) 5-(2-ethyl-butyrylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 483) 5-(2-propyl-pentanoylamino)-3-pyridin-3-yl-isoxazole-4-carboxylic acid amide; 484) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(3-methyl-butyrylamino)-isoxazole-4-carboxylic acid amide; 485) 5-[(benzo[1,3]dioxole-5-carbonyl)-amino]-3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-isoxazole-4-carboxylic acid amide; 486) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(2-ethyl-butyrylamino)-isoxazole-4-carboxylic acid amide; 487) 3-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-5-(2-propyl-pentanoylamino)-isoxazole-4-carboxylic acid amide; 488) 5-(3-methyl-butyrylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 489) 5-(2-ethyl-butyrylamino)-3-quinolin-2-yl-isoxazole-4-carboxylic acid amide; 490) 5-Phenylacetylamino-3-thiophen-2-yl-isoxazole-4-carboxylic acid butylamide; 491) 5-Phenylacetylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 492) 5-Butyrylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 493) 5-[(Furan-2-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 494) 5-Benzoylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 495) 5-Phenylacetylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 496) 5-Butyrylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 497) 5-[(Furan-2-carbonyl)-amino]-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 498) 5-Benzoylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 499) 5-Phenylacetylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 500) 5-Butyrylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 501) 5-[(Furan-2-carbonyl)-amino]-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 502) 5-Benzoylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 503) 5-Phenylacetylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 504) 5-Butyrylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 505) 5-[(Furan-2-carbonyl)-amino]-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 506) 5-Benzoylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 507) 5-(4-Acetylamino-benzenesulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid phenylamide; 508) 5-(4-Acetylamino-benzenesulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 509) 5-(Butane-1-sulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 510) 3-Pyridin-2-yl-5-(toluene-4-sulfonylamino)-isoxazole-4-carboxylic acid amide; 511) 5-(2,5-Dichloro-thiophene-3-sulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 512) 5-(Butane-1-sulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid acetylamide; 513) 3-Pyridin-2-yl-5-(toluene-4-sulfonylamino)-isoxazole-4-carboxylic acid benzylamide; 514) 5-(2,5-Dichloro-thiophene-3-sulfonylamino)-3-pyridin-2-yl-isoxazole-4-carboxylic acid phenylamide; 515) 5-Methanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 516) 5-Benzenesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 517) 5-Phenylmethanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 518) 5-(Thiophene-2-sulfonylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid amide; 519) 5-Benzenesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 520) 5-Phenylmethanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 521) 3-Pyridin-2-yl-5-(thiophene-2-sulfonylamino)-isoxazole-4-carboxylic acid amide; 522) 5-Methanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid amide; 523) 5-Methanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 524) 5-Benzenesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 525) 5-Phenylmethanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 526) 5-(Thiophene-2-sulfonylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 527) 5-Methanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 528) 5-Benzenesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 529) 5-Phenylmethanesulfonylamino-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 530) 5-(Thiophene-2-sulfonylamino)-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 531) 5-Benzenesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 532) 5-Phenylmethanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 533) 3-Pyridin-2-yl-5-(thiophene-2-sulfonylamino)-isoxazole-4-carboxylic acid butylamide; 534) 5-Methanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 535) 5-Methanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 536) 5-Benzenesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 537) 5-Phenylmethanesulfonylamino-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 538) 3-Pyridin-2-yl-5-(thiophene-2-sulfonylamino)-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 539) Phenyl 5-amino-3-(2-pyridinyl)-4-isoxazolecarboxylate 540) Cyclohexyl 5-amino-3-(2-pyridinyl)-4-isoxazolecarboxylate 541) 5-Benzothiophenyl 5-amino-3-(2-pyridinyl)-4-isoxazolecarboxylate; 542) Phenyl 5-acetylamino-3-(2-pyridinyl)-4-isoxazolecarboxylate; 543) Ciclohexyl 5-benzoylamino-3-(2-pyridinyl)-4-isoxazolecarboxylate; 544) 5-Benzothiophenyl 5-(2,4-dimethoxybenzoylamino)-3-(2-pyridinyl)-4-isoxazolecarboxylate; 545) 5-(3-Phenyl-ureido)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 546) 5-(3-Isopropyl-ureido)-3-thiophen-2-yl-isoxazole-4-carboxylic acid amide; 547) 5-(3-Phenyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 548) 5-(3-Benzyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 549) 5-(3-Isopropyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 550) 5-(3-Pyridin-3-yl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid butylamide; 551) 5-(3-Phenyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 552) 5-(3-Benzyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 553) 5-(3-Isopropyl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 554) 5-(3-Pyridin-3-yl-ureido)-3-thiophen-3-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 555) 5-(3-Phenyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 556) 5-(3-Benzyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 557) 5-(3-Isopropyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid butylamide; 558) 3-Pyridin-2-yl-5-(3-pyridin-3-yl-ureido)-isoxazole-4-carboxylic acid butylamide; 559) 5-(3-Phenyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 560) 5-(3-Benzyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 561) 5-(3-Isopropyl-ureido)-3-pyridin-2-yl-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 562) 3-Pyridin-2-yl-5-(3-pyridin-3-yl-ureido)-isoxazole-4-carboxylic acid (4-methoxy-phenyl)-amide; 563) 5-amino-N-benzyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 564) 5-amino-N-(2-furylmethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 565) 5-amino-N-(2-phenylethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 566) 5-amino-N-cyclohexyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 567) 5-amino-N-(4-methoxybenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 568) 5-amino-N-hexyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 569) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 570) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 571) 5-amino-N-cyclopentyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 572) 5-amino-N-(1,5-dimethylhexyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 573) 5-amino-N-isopentyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 574) 5-amino-N-(2-ethylhexyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 575) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(4-phenylbutyl)isoxazole-4-carboxamide; 576) 5-amino-N-(2-methylcyclohexyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 577) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 578) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 579) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(3-phenylpropyl)isoxazole-4-carboxamide; 580) 5-amino-N-isobutyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 581) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 582) 5-amino-N-(2-methoxybenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 583) 5-amino-N-(2-fluorobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 584) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 585) 5-amino-N-(3,4-difluorobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 586) 5-amino-N-(3-chlorobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 587) 5-amino-N-(2-chlorobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 588) 5-amino-N-(3-methylbenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 589) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 590) 5-amino-N-(cyclopropylmethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 591) 5-amino-N-cycloheptyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 592) 5-amino-N-[2-(4-methoxyphenyl)ethyl]-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 593) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 594) 5-amino-N-(1,2-dimethylpropyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 595) 5-amino-N-(3,3-diphenylpropyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 596) 5-amino-N-(1,2-diphenylethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 597) 5-amino-N-(2,4-dimethoxybenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 598) 5-amino-N-[3-(dibutylamino)propyl]-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 599) 5-amino-N-butyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 600) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 601) 5-amino-N-(1-methylhexyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 602) 5-amino-N-(2-methoxy-1-methylethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 603) 5-amino-N-(1-methylbutyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 604) 5-amino-N-(3-fluorobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 605) 5-amino-N-(4-methylbenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 606) 5-amino-N-(1,3-dimethylbutyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 607) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 608) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 609) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 610) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-pentylisoxazole-4-carboxamide; 611) 5-amino-N-(cyclohexylmethyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 612) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 613) 5-amino-N-(1-ethylpropyl)-3-(5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 614) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-(1-phenylethyl)isoxazole-4-carboxamide; 615) 5-amino-N-(2-methylbenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 616) 5-amino-N-cyclobutyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 617) 5-amino-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}-N-octylisoxazole-4-carboxamide; 618) 5-amino-N-(2-bromobenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 619) 5-amino-N-(1-methylheptyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 620) 5-amino-N-heptyl-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 621) 5-amino-N-(tert-butyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 622) 5-amino-N-(3,4-dimethoxybenzyl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 623) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 624) 5-amino-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-3-{5-[3-(trifluoromethyl)phenyl]-2-furyl}isoxazole-4-carboxamide; 625) 5-amino-N-benzyl-3-(5-bromothien-2-yl)isoxazole-4-carboxamide; 626) 5-amino-3-(5-bromothien-2-yl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 627) 5-amino-3-(5-bromothien-2-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 628) 5-amino-3-(5-bromothien-2-yl)-N-(sec-butyl)isoxazole-4-carboxamide; 629) 5-amino-3-(5-bromothien-2-yl).-N-cyclohexylisoxazole-4-carboxamide; 630) 5-amino-3-(5-bromothien-2-yl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 631) 5-amino-3-(5-bromothien-2-yl)-N-isopropylisoxazole-4-carboxamide; 632) 5-amino-3-(5-bromothien-2-yl)-N-hexylisoxazole-4-carboxamide; 633) N-allyl-5-amino-3-(5-bromothien-2-yl)isoxazole-4-carboxamide; 634) 5-amino-3-(5-bromothien-2-yl)-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 635) 5-amino-3-(5-bromothien-2-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 636) 5-amino-3-(5-bromothien-2-yl)-N-cyclopentylisoxazole-4-carboxamide; 637) 5-amino-3-(5-bromothien-2-yl)-N-(1,5-dimethylhexyl)isoxazole-4-carboxamide; 638) 5-amino-3-(5-bromothien-2-yl)-N-isopentylisoxazole-4-carboxamide; 639) 5-amino-3-(5-bromothien-2-yl)-N-(2-ethylhexyl)isoxazole-4-carboxamide; 640) 5-amino-3-(5-bromothien-2-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 641) 5-amino-3-(5-bromothien-2-yl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 642) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(5-bromothien-2-yl)isoxazole-4-carboxamide; 643) 5-amino-3-(5-bromothien-2-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 644) 5-amino-3-(5-bromothien-2-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 645) 5-amino-3-(5-bromothien-2-yl)-N-isobutylisoxazole-4-carboxamide; 646) 5-amino-3-(5-bromothien-2-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 647) 5-amino-3-(5-bromothien-2-yl)-N-(2-methoxybenzyl)isoxazole-4-carboxamide; 648) 5-amino-3-(5-bromothien-2-yl)-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 649) 5-amino-3-(5-bromothien-2-yl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 650) 5-amino-3-(5-bromothien-2-yl)-N-(3,4-difluorobenzyl)isoxazole-4-carboxamide; 651) 5-amino-3-(5-bromothien-2-yl)-N-(3-chlorobenzyl)isoxazole-4-carboxamide; 652) 5-amino-3-(5-bromothien-2-yl)-N-(2-chlorobenzyl)isoxazole-4-carboxamide; 653) 5-amino-3-(5-bromothien-2-yl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 654) 5-amino-3-(5-bromothien-2-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 655) 5-amino-3-(5-bromothien-2-yl)-N-(cyclopropylmethyl)isoxazole-4-carboxamide; 656) 5-amino-3-(5-bromothien-2-yl)-N-cycloheptylisoxazole-4-carboxamide; 657) 5-amino-3-(5-bromothien-2-yl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 658) 5-amino-3-(5-bromothien-2-yl)-N-(2-cyclohex-1-en-1-ylethyl)isoxazole-4-carboxamide; 659) 5-amino-3-(5-bromothien-2-yl)-N-prop-2-ynylisoxazole-4-carboxamide; 660) 5-amino-3-(5-bromothien-2-yl)-N-(1,2-dimethylpropyl)isoxazole-4-carboxamide; 661) 5-amino-3-(5-bromothien-2-yl)-N-(3,3-diphenylpropyl)isoxazole-4-carboxamide; 662) 5-amino-3-(5-bromothien-2-yl)-N-(1,2-diphenylethyl)isoxazole-4-carboxamide; 663) 5-amino-3-(5-bromothien-2-yl)-N-[3-(dibutylamino)propyl]isoxazole-4-carboxamide; 664) 5-amino-3-(5-bromothien-2-yl)-N-butylisoxazole-4-carboxamide; 665) 5-amino-3-(5-bromothien-2-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 666) 5-amino-3-(5-bromothien-2-yl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 667) 5-amino-3-(5-bromothien-2-yl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 668) 5-amino-3-(5-bromothien-2-yl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 669) 5-amino-3-(5-bromothien-2-yl)-N-(4-tert-butylcyclohexyl)isoxazole-4-carboxamide; 670) 5-amino-3-(5-bromothien-2-yl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 671) 5-amino-3-(5-bromothien-2-yl)-N-(3-fluorobenzyl)isoxazole-4-carboxamide; 672) 5-amino-3-(5-bromothien-2-yl)-N-(4-methylbenzyl)isoxazole-4-carboxamide; 673) 5-amino-3-(5-bromothien-2-yl)-N-(1,3-dimethylbutyl)isoxazole-4-carboxamide; 674) 5-amino-3-(5-bromothien-2-yl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 675) 5-amino-3-(5-bromothien-2-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 676) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-bromothien-2-yl)isoxazole-4-carboxamide; 677) 5-amino-3-(5-bromothien-2-yl)-N-pentylisoxazole-4-carboxamide; 678) 5-amino-3-(5-bromothien-2-yl)-N-(cyclohexylmethyl)isoxazole-4-carboxamide; 679) ethyl 4-({[5-amino-3-(5-bromothien-2-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 680) 5-amino-3-(5-bromothien-2-yl)-N-[2-(3-chlorophenyl)ethyl]isoxazole-4-carboxamide; 681) 5-amino-3-(5-bromothien-2-yl)-N-(1-ethylpropyl)isoxazole-4-carboxamide; 682) 5-amino-3-(5-bromothien-2-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 683) 5-amino-3-(5-bromothien-2-yl)-N-propylisoxazole-4-carboxamide; 684) 5-amino-3-(5-bromothien-2-yl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 685) 5-amino-3-(5-bromothien-2-yl)-N-cyclobutylisoxazole-4-carboxamide; 686) 5-amino-3-(5-bromothien-2-yl)-N-(3-methoxypropyl)isoxazole-4-carboxamide; 687) 5-amino-3-(5-bromothien-2-yl)-N-octylisoxazole-4-carboxamide; 688) 5-amino-N-(2-bromobenzyl)-3-(5-bromothien-2-yl)isoxazole-4-carboxamide; 689) 5-amino-3-(5-bromothien-2-yl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 690) 5-amino-3-(5-bromothien-2-yl)-N-heptylisoxazole-4-carboxamide; 691) 5-amino-3-(5-bromothien-2-yl)-N-(tert-butyl)isoxazole-4-carboxamide; 692) 5-amino-3-(5-bromothien-2-yl)-N-(2,3-dihydro-1H-inden-1-yl)isoxazole-4-carboxamide; 693) 5-amino-3-(5-bromothien-2-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 694) 5-amino-N-benzyl-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 695) 5-amino-3-(5-chlorothien-2-yl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 696) 5-amino-3-(5-chlorothien-2-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 697) 5-amino-N-(sec-butyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 698) 5-amino-3-(5-chlorothien-2-yl)-N-cyclohexylisoxazole-4-carboxamide; 699) 5-amino-3-(5-chlorothien-2-yl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 700) 5-amino-3-(5-chlorothien-2-yl)-N-isopropylisoxazole-4-carboxamide; 701) 5-amino-3-(5-chlorothien-2-yl)-N-hexylisoxazole-4-carboxamide; 702) N-allyl-5-amino-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 703) 5-amino-3-(5-chlorothien-2-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 704) 5-amino-3-(5-chlorothien-2-yl)-N-cyclopentylisoxazole-4-carboxamide; 705) 5-amino-3-(5-chlorothien-2-yl)-N-isopentylisoxazole-4-carboxamide; 706) 5-amino-3-(5-chlorothien-2-yl)-N-(2-ethylhexyl)isoxazole-4-carboxamide; 707) 5-amino-3-(5-chlorothien-2-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 708) 5-amino-3-(5-chlorothien-2-yl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 709) 5-amino-3-(5-chlorothien-2-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 710) 5-amino-3-(5-chlorothien-2-yl)-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 711) 5-amino-3-(5-chlorothien-2-yl)-N-(3,4-difluorobenzyl)isoxazole-4-carboxamide; 712) 5-amino-N-(3-chlorobenzyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 713) 5-amino-N-(2-chlorobenzyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 714) 5-amino-3-(5-chlorothien-2-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 715) 5-amino-3-(5-chlorothien-2-yl)-N-(cyclopropylmethyl)isoxazole-4-carboxamide; 716) 5-amino-3-(5-chlorothien-2-yl)-N-cycloheptylisoxazole-4-carboxamide; 717) 5-amino-3-(5-chlorothien-2-yl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 718) 5-amino-3-(5-chlorothien-2-yl)-N-(2-cyclohex-1-en-1-ylethyl)isoxazole-4-carboxamide; 719) 5-amino-3-(5-chlorothien-2-yl)-N-(3,3-diphenylpropyl)isoxazole-4-carboxamide; 720) 5-amino-3-(5-chlorothien-2-yl)-N-(1,2-diphenylethyl)isoxazole-4-carboxamide; 721) 5-amino-3-(5-chlorothien-2-yl)-N-[3-(dibutylamino)propyl]isoxazole-4-carboxamide; 722) 5-amino-N-butyl-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 723) 5-amino-3-(5-chlorothien-2-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 724) 5-amino-3-(5-chlorothien-2-yl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 725) 5-amino-3-(5-chlorothien-2-yl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 726) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 727) 5-amino-3-(5-chlorothien-2-yl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 728) 5-amino-3-(5-chlorothien-2-yl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 729) 5-amino-3-(5-chlorothien-2-yl)-N-(3-fluorobenzyl)isoxazole-4-carboxamide; 730) 5-amino-3-(5-chlorothien-2-yl)-N-(1,3-dimethylbutyl)isoxazole-4-carboxamide; 731) 5-amino-3-(5-chlorothien-2-yl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 732) 5-amino-3-(5-chlorothien-2-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 733) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 734) 5-amino-3-(5-chlorothien-2-yl)-N-pentylisoxazole-4-carboxamide; 735) 5-amino-3-(5-chlorothien-2-yl)-N-(cyclohexylmethyl)isoxazole-4-carboxamide; 736) ethyl 4-({[5-amino-3-(5-chlorothien-2-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 737) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 738) 5-amino-3-(5-chlorothien-2-yl)-N-(1-ethylpropyl)isoxazole-4-carboxamide; 739) 5-amino-3-(5-chlorothien-2-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 740) 5-amino-3-(5-chlorothien-2-yl)-N-propylisoxazole-4-carboxamide; 741) 5-amino-3-(5-chlorothien-2-yl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 742) 5-amino-3-(5-chlorothien-2-yl)-N-cyclobutylisoxazole-4-carboxamide; 743) 5-amino-3-(5-chlorothien-2-yl)-N-(3-methoxypropyl)isoxazole-4-carboxamide; 744) 5-amino-N-(2-bromobenzyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 745) 5-amino-3-(5-chlorothien-2-yl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 746) 5-amino-3-(5-chlorothien-2-yl)-N-heptylisoxazole-4-carboxamide; 747) 5-amino-N-(tert-butyl)-3-(5-chlorothien-2-yl)isoxazole-4-carboxamide; 748) 5-amino-3-(5-chlorothien-2-yl)-N-(3,4-dimethoxybenzyl)isoxazole-4-carboxamide; 749) 5-amino-3-(5-chlorothien-2-yl)-N-(2,3-dihydro-1H-inden-1-yl)isoxazole-4-carboxamide; 750) 5-amino-3-(5-chlorothien-2-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 751) 5-amino-N-benzyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 752) 5-amino-N-(2-furylmethyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 753) 5-amino-3-(5-methylthien-2-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 754) 5-amino-N-(sec-butyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 755) 5-amino-N-cyclohexyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 756) 5-amino-N-(4-methoxybenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 757) 5-amino-N-isopropyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 758) 5-amino-N-hexyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 759) N-allyl-5-amino-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 760) 5-amino-3-(5-methylthien-2-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 761) 5-amino-N-cyclopentyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 762) 5-amino-N-(1,5-dimethylhexyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 763) 5-amino-N-isopentyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 764) 5-amino-N-(2-ethylhexyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 765) 5-amino-3-(5-methylthien-2-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 766) 5-amino-N-(2-methylcyclohexyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 767) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 768) 5-amino-3-(5-methylthien-2-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 769) 5-amino-3-(5-methylthien-2-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 770) 5-amino-N-isobutyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 771) 5-amino-3-(5-methylthien-2-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 772) 5-amino-N-(2-methoxybenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 773) 5-amino-N-(2-fluorobenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 774) 5-amino-N-(3,4-difluorobenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 775) 5-amino-N-(3-chlorobenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 776) 5-amino-N-cycloheptyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 777) 5-amino-N-(1,2-dimethylpropyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 778) 5-amino-N-(3,3-diphenylpropyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 779) 5-amino-N-(1,2-diphenylethyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 780) 5-amino-N-(2,4-dimethoxybenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 781) 5-amino-N-[3-(dibutylamino)propyl]-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 782) 5-amino-N-butyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 783) 5-amino-3-(5-methylthien-2-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 784) 5-amino-N-[(5-methyl-2-furyl)methyl]-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 785) 5-amino-N-(1-methylhexyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 786) 5-amino-N-(2-methoxy-1-methylethyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 787) 5-amino-N-(4-tert-butylcyclohexyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 788) 5-amino-N-(1-methylbutyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 789) 5-amino-N-(3-fluorobenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 790) 5-amino-N-(4-methylbenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 791) 5-amino-N-(1-methyl-3-phenylpropyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 792) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 793) 5-amino-3-(5-methylthien-2-yl)-N-pentylisoxazole-4-carboxamide; 794) 5-amino-N-(cyclohexylmethyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 795) 5-amino-3-(5-methylthien-2-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 796) 5-amino-3-(5-methylthien-2-yl)-N-propylisoxazole-4-carboxamide; 797) 5-amino-N-(2-methylbenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 798) 5-amino-N-cyclobutyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 799) 5-amino-N-(3-methoxypropyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 800) 5-amino-3-(5-methylthien-2-yl)-N-octylisoxazole-4-carboxamide; 801) 5-amino-N-(1-methylheptyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 802) 5-amino-N-heptyl-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 803) 5-amino-N-(tert-butyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 804) 5-amino-N-(3,4-dimethoxybenzyl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 805) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(5-methylthien-2-yl)isoxazole-4-carboxamide; 806) 5-amino-3-(5-methylthien-2-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 807) 5-amino-N-benzyl-3-(3-methylthien-2yl)isoxazole-4-carboxamide; 808) 5-amino-N-(2-furylmethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 809) 5-amino-3-(3-methylthien-2-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 810) 5-amino-N-(sec-butyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 811) 5-amino-N-cyclohexyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 812) 5-amino-N-(4-methoxybenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 813) 5-amino-N-isopropyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 814) 5-amino-N-hexyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 815) N-allyl-5-amino-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 816) 5-amino-3-(3-methylthien-2-yl)-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 817) 5-amino-N-cyclopentyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 818) 5-amino-N-(1,5-dimethylhexyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 819) 5-amino-N-isopentyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 820) 5-amino-N-(2-ethylhexyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 821) 5-amino-3-(3-methylthien-2-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 822) 5-amino-N-(2-methylcyclohexyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 823) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 824) 5-amino-3-(3-methylthien-2-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 825) 5-amino-3-(3-methylthien-2-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 826) 5-amino-N-isobutyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 827) 5-amino-3-(3-methylthien-2-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 828) 5-amino-N-(2-methoxybenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 829) 5-amino-N-(2-fluorobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 830) 5-amino-3-(3-methylthien-2-yl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 831) 5-amino-N-(3,4-difluorobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 832) 5-amino-N-(3-chlorobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 833) 5-amino-N-(2-chlorobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 834) 5-amino-N-(3-methylbenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 835) 5-amino-3-(3-methylthien-2-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 836) 5-amino-N-(cyclopropylmethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 837) 5-amino-N-cycloheptyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 838) 5-amino-N-[2-(4-methoxyphenyl)ethyl]-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 839) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 840) 5-amino-N-(1,2-dimethylpropyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 841) 5-amino-N-(3,3-diphenylpropyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 842) 5-amino-N-(2,4-dimethoxybenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 843) 5-amino-N-[3-(dibutylamino)propyl]-3 (3-methylthien-2-yl)isoxazole-4-carboxamide; 844) 5-amino-N-butyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 845) 5-amino-3-(3-methylthien-2-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 846) 5-amino-N-[(5-methyl-2-furyl)methyl]-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 847) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 848) 5-amino-N-(2-methoxy-1-methylethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 849) 5-amino-N-(4-tert-butylcyclohexyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 850) 5-amino-N-(1-methylbutyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 851) 5-amino-N-(3-fluorobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 852) 5-amino-N-(4-methylbenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 853) 5-amino-N-(1,3-dimethylbutyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 854) 5-amino-N-(1-methyl-3-phenylpropyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 855) 5-amino-3-(3-methylthien-2-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 856) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 857) 5-amino-3-(3-methylthien-2-yl)-N-pentylisoxazole-4-carboxamide; 858) 5-amino-N-(cyclohexylmethyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 859) ethyl 4-({[5-amino-3-(3-methylthien-2-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 860) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 861) 5-amino-N-(1-ethylpropyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 862) 5-amino-3-(3-methylthien-2-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 863) 5-amino-N-(2-methylbenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 864) 5-amino-N-cyclobutyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 865) 5-amino-N-benzhydryl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 866) 5-amino-3-(3-methylthien-2-yl)-N-octylisoxazole-4-carboxamide; 867) 5-amino-N-(2-bromobenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 868) 5-amino-N-(1-methylheptyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 869) 5-amino-N-heptyl-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 870) 5-amino-N-(tert-butyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 871) 5-amino-N-(3,4-dimethoxybenzyl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 872) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(3-methylthien-2-yl)isoxazole-4-carboxamide; 873) 5-amino-3-(3-methylthien-2-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 874) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-furylmethyl)isoxazole-4-carboxamide; 875) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-phenylethyl)isoxazole-4-carboxamide; 876) 5-amino-N-(sec-butyl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 877) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-cyclohexylisoxazole-4-carboxamide; 878) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 879) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-isopropylisoxazole-4-carboxamide; 880) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-hexylisoxazole-4-carboxamide; 881) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 882) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-cyclopentylisoxazole-4-carboxamide; 883) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1,5-dimethylhexyl)isoxazole-4-carboxamide; 884) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-isopentylisoxazole-4-carboxamide; 885) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-ethylhexyl)isoxazole-4-carboxamide; 886) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(4-phenylbutyl)isoxazole-4-carboxamide; 887) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 888) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 889) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 890) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(3-phenylpropyl)isoxazole-4-carboxamide; 891) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-isobutylisoxazole-4-carboxamide; 892) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 893) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-methoxybenzyl)isoxazole-4-carboxamide; 894) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 895) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 896) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(3,4-difluorobenzyl)isoxazole-4-carboxamide; 897) 5-amino-N-(3-chlorobenzyl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 898) 5-amino-N-(2-chlorobenzyl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 899) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(3-methylbenzyl)isoxazole-4-carboxamide; 900) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 901) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(cyclopropylmethyl)isoxazole-4-carboxamide; 902) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-cycloheptylisoxazole-4-carboxamide; 903) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 904) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-cyclohex-1-en-1-ylethyl)isoxazole-4-carboxamide; 905) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1,2-dimethylpropyl)isoxazole-4-carboxamide; 906) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(3,3-diphenylpropyl)isoxazole-4-carboxamide; 907) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1,2-diphenylethyl)isoxazole-4-carboxamide; 908) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2,4-dimethoxybenzyl)isoxazole-4-carboxamide; 909) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[3-(dibutylamino)propyl]isoxazole-4-carboxamide; 910) 5-amino-N-butyl-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 911) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 912) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 913) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-methylhexyl)isoxazole-4-carboxamide; 914) 5-amino-N-(1-benzylpiperidin-4-yl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 915) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1,3-dimethylbutyl)isoxazole-4-carboxamide; 916) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 917) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 918) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-pentylisoxazole-4-carboxamide; 919) ethyl 4-[({5-amino-3-[5-(3-chlorophenyl)-2-furyl]isoxazol-4-yl}carbonyl)amino]piperidine-1-carboxylate; 920) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 921) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-ethylpropyl)isoxazole-4-carboxamide; 922) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-phenylethyl)isoxazole-4-carboxamide; 923) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2-methylbenzyl)isoxazole-4-carboxamide; 924) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-cyclobutylisoxazole-4-carboxamide; 925) 5-amino-N-benzhydryl-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 926) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-octylisoxazole-4-carboxamide; 927) 5-amino-N-(2-bromobenzyl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 928) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1-methylheptyl)isoxazole-4-carboxamide; 929) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-heptylisoxazole-4-carboxamide; 930) 5-amino-N-(tert-butyl)-3-[5-(3-chlorophenyl)-2-furyl]isoxazole-4-carboxamide; 931) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(3,4-dimethoxybenzyl)isoxazole-4-carboxamide; 932) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(2,3-dihydro-1H-inden-1-yl)isoxazole-4-carboxamide; 933) 5-amino-3-[5-(3-chlorophenyl)-2-furyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 934) 5-amino-N-benzyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 935) 5-amino-N-(2-furylmethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 936) 5-amino-3-(5-methyl-2-furyl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 937) 5-amino-N-(sec-butyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 938) 5-amino-N-cyclohexyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 939) 5-amino-N-(4-methoxybenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 940) 5-amino-N-hexyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 941) 5-amino-3-(5-methyl-2-furyl)-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 942) 5-amino-3-(5-methyl-2-furyl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 943) 5-amino-N-cyclopentyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 944) 5-amino-N-(1,5-dimethylhexyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 945) 5-amino-N-isopentyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 946) 5-amino-N-(2-ethylhexyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 947) 5-amino-3-(5-methyl-2-furyl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 948) 5-amino-N-(2-methylcyclohexyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 949) 5-amino-3-(5-methyl-2-furyl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 950) 5-amino-3-(5-methyl-2-furyl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 951) 5-amino-N-isobutyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 952) 5-amino-3-(5-methyl-2-furyl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 953) 5-amino-N-(2-methoxybenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 954) 5-amino-N-(2-fluorobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 955) 5-amino-3-(5-methyl-2-furyl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 956) 5-amino-N-(3,4-difluorobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 957) 5-amino-N-(3-chlorobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 958) 5-amino-N-(2-chlorobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 959) 5-amino-N-(3-methylbenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 960) 5-amino-3-(5-methyl-2-furyl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 961) 5-amino-N-(cyclopropylmethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 962) 5-amino-N-cycloheptyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 963) 5-amino-N-[2-(4-methoxyphenyl)ethyl]-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 964) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 965) 5-amino-N-(1,2-dimethylpropyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 966) 5-amino-N-(3,3-diphenylpropyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 967) 5-amino-N-(1,2-diphenylethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 968) 5-amino-N-(2,4-dimethoxybenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 969) 5-amino-N-[3-(dibutylamino)propyl]-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 970) 5-amino-N-butyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 971) 5-amino-3-(5-methyl-2-furyl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 972) 5-amino-3-(5-methyl-2-furyl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 973) 5-amino-3-(5-methyl-2-furyl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 974) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 975) 5-amino-N-(2-methoxy-1-methylethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 976) 5-amino-N-(1-methylbutyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 977) 5-amino-N-(3-fluorobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 978) 5-amino-N-(4-methylbenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 979) 5-amino-N-(1,3-dimethylbutyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 980) 5-amino-3-(5-methyl-2-furyl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 981) 5-amino-3-(5-methyl-2-furyl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 982) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 983) 5-amino-3-(5-methyl-2-furyl)-N-pentylisoxazole-4-carboxamide; 984) 5-amino-N-(cyclohexylmethyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 985) ethyl 4-({[5-amino-3-(5-methyl-2-furyl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 986) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 987) 5-amino-N-(1-ethylpropyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 988) 5-amino-3-(5-methyl-2-furyl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 989) 5-amino-N-(2-methylbenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 990) 5-amino-N-cyclobutyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 991) 5-amino-N-benzhydryl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 992) 5-amino-3-(5-methyl-2-furyl)-N-octylisoxazole-4-carboxamide; 993) 5-amino-N-(2-bromobenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 994) 5-amino-3-(5-methyl-2-furyl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 995) 5-amino-N-heptyl-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 996) 5-amino-N-(tert-butyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 997) 5-amino-N-(3,4-dimethoxybenzyl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 998) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(5-methyl-2-furyl)isoxazole-4-carboxamide; 999) 5-amino-3-(5-methyl-2-furyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1000) 5-amino-N-benzyl-3-(2-furyl)isoxazole-4-carboxamide; 1001) 5-amino-3-(2-furyl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 1002) 5-amino-3-(2-furyl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 1003) 5-amino-N-(sec-butyl)-3-(2-furyl)isoxazole-4-carboxamide; 1004) 5-amino-3-(2-furyl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 1005) 5-amino-3-(2-furyl)-N-hexylisoxazole-4-carboxamide; 1006) 5-amino-3-(2-furyl)-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 1007) 5-amino-3-(2-furyl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 1008) 5-amino-N-cyclopentyl-3-(2-furyl)isoxazole-4-carboxamide; 1009) 5-amino-N-(1,5-dimethylhexyl)-3-(2-furyl)isoxazole-4-carboxamide; 1010) 5-amino-3-(2-furyl)-N-isopentylisoxazole-4-carboxamide; 1011) 5-amino-N-(2-ethylhexyl)-3-(2-furyl)isoxazole-4-carboxamide; 1012) 5-amino-3-(2-furyl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 1013) 5-amino-3-(2-furyl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 1014) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(2-furyl)isoxazole-4-carboxamide; 1015) 5-amino-3-(2-furyl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1016) 5-amino-3-(2-furyl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 1017) 5-amino-3-(2-furyl)-N-isobutylisoxazole-4-carboxamide; 1018) 5-amino-3-(2-furyl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1019) 5-amino-3-(2-furyl)-N-(2-methoxybenzyl)isoxazole-4-carboxamide; 1020) 5-amino-N-(2-fluorobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1021) 5-amino-3-(2-furyl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1022) 5-amino-N-(3,4-difluorobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1023) 5-amino-N-(3-chlorobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1024) 5-amino-N-(2-chlorobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1025) 5-amino-3-(2-furyl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 1026) 5-amino-3-(2-furyl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 1027) 5-amino-N-(cyclopropylmethyl)-3-(2-furyl)isoxazole-4-carboxamide; 1028) 5-amino-N-cycloheptyl-3-(2-furyl)isoxazole-4-carboxamide; 1029) 5-amino-3-(2-furyl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 1030) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-(2-furyl)isoxazole-4-carboxamide; 1031) 5-amino-N-(1,2-dimethylpropyl)-3-(2-furyl)isoxazole-4-carboxamide; 1032) 5-amino-N-(3,3-diphenylpropyl)-3-(2-furyl)isoxazole-4-carboxamide; 1033) 5-amino-N-(1,2-diphenylethyl)-3-(2-furyl)isoxazole-4-carboxamide; 1034) 5-amino-N-(2,4-dimethoxybenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1035) 5-amino-N-[3-(dibutylamino)propyl]-3-(2-furyl)isoxazole-4-carboxamide; 1036) 5-amino-N-butyl-3-(2-furyl)isoxazole-4-carboxamide; 1037) 5-amino-3-(2-furyl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1038) 5-amino-3-(2-furyl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 1039) 5-amino-3-(2-furyl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 1040) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(2-furyl)isoxazole-4-carboxamide; 1041) 5-amino-3-(2-furyl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 1042) 5-amino-N-(4-tert-butylcyclohexyl)-3-(2-furyl)isoxazole-4-carboxamide; 1043) 5-amino-3-(2-furyl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 1044) 5-amino-N-(3-fluorobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1045) 5-amino-3-(2-furyl)-N-(4-methylbenzyl)isoxazole-4-carboxamide; 1046) 5-amino-N-(1,3-dimethylbutyl)-3-(2-furyl)isoxazole-4-carboxamide; 1047) 5-amino-3-(2-furyl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 1048) 5-amino-3-(2-furyl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 1049) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(2-furyl)isoxazole-4-carboxamide; 1050) 5-amino-3-(2-furyl)-N-pentylisoxazole-4-carboxamide; 1051) 5-amino-N-(cyclohexylmethyl)-3-(2-furyl)isoxazole-4-carboxamide; 1052) ethyl 4-({[5-amino-3-(2-furyl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 1053) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(2-furyl)isoxazole-4-carboxamide; 1054) 5-amino-N-(1-ethylpropyl)-3-(2-furyl)isoxazole-4-carboxamide; 1055) 5-amino-3-(2-furyl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 1056) 5-amino-3-(2-furyl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 1057) 5-amino-N-cyclobutyl-3-(2-furyl)isoxazole-4-carboxamide; 1058) 5-amino-N-benzhydryl-3-(2-furyl)isoxazole-4-carboxamide; 1059) 5-amino-3-(2-furyl)-N-octylisoxazole-4-carboxamide; 1060) 5-amino-N-(2-bromobenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1061) 5-amino-3-(2-furyl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 1062) 5-amino-3-(2-furyl)-N-heptylisoxazole-4-carboxamide; 1063) 5-amino-N-(tert-butyl)-3-(2-furyl)isoxazole-4-carboxamide; 1064) 5-amino-N-(3,4-dimethoxybenzyl)-3-(2-furyl)isoxazole-4-carboxamide; 1065) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(2-furyl)isoxazole-4-carboxamide; 1066) 5-amino-3-(2-furyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1067) 5-amino-3-(1-benzofuran-3-yl)-N-benzylisoxazole-4-carboxamide; 1068) 5-amino-3-(1-benzofuran-3-yl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 1069) 5-amino-3-(1-benzofuran-3-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 1070) 5-amino-3-(1-benzofuran-3-yl)-N-(sec-butyl)isoxazole-4-carboxamide; 1071) 5-amino-3-(1-benzofuran-3-yl)-N-cyclohexylisoxazole-4-carboxamide; 1072) 5-amino-3-(1-benzofuran-3-yl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 1073) 5-amino-3-(1-benzofuran-3-yl)-N-hexylisoxazole-4-carboxamide; 1074) 5-amino-3-(1-benzofuran-3-yl)-N-(tetrahydrofuran-2-ylmethyl)isoxazole-4-carboxamide; 1075) 5-amino-3-(1-benzofuran-3-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 1076) 5-amino-3-(1-benzofuran-3-yl)-N-cyclopentylisoxazole-4-carboxamide; 1077) 5-amino-3-(1-benzofuran-3-yl)-N-(1,5-dimethylhexyl)isoxazole-4-carboxamide; 1078) 5-amino-3-(1-benzofuran-3-yl)-N-isopentylisoxazole-4-carboxamide; 1079) 5-amino-3-(1-benzofuran-3-yl)-N-(2-ethylhexyl)isoxazole-4-carboxamide; 1080) 5-amino-3-(1-benzofuran-3-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 1081) 5-amino-3-(1-benzofuran-3-yl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 1082) 5-amino-3-(1-benzofuran-3-yl)-N-[3,5-bis(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1083) 5-amino-3-(1-benzofuran-3-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1084) 5-amino-3-(1-benzofuran-3-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 1085) 5-amino-3-(1-benzofuran-3-yl)-N-isobutylisoxazole-4-carboxamide; 1086) 5-amino-3-(1-benzofuran-3-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1087) 5-amino-3-(1-benzofuran-3-yl)-N-(2-methoxybenzyl)isoxazole-4-carboxamide; 1088) 5-amino-3-(1-benzofuran-3-yl)-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 1089) 5-amino-3-(1-benzofuran-3-yl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1090) 5-amino-3-(1-benzofuran-3-yl)-N-(3,4-difluorobenzyl)isoxazole-4-carboxamide; 1091) 5-amino-3-(1-benzofuran-3-yl)-N-(3-chlorobenzyl)isoxazole-4-carboxamide; 1092) 5-amino-3-(1-benzofuran-3-yl)-N-(2-chlorobenzyl)isoxazole-4-carboxamide; 1093) 5-amino-3-(1-benzofuran-3-yl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 1094) 5-amino-3-(1-benzofuran-3-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 1095) 5-amino-3-(1-benzofuran-3-yl)-N-(cyclopropylmethyl)isoxazole-4-carboxamide; 1096) 5-amino-3-(1-benzofuran-3-yl)-N-cycloheptylisoxazole-4-carboxamide; 1097) 5-amino-3-(1-benzofuran-3-yl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 1098) 5-amino-3-(1-benzofuran-3-yl)-N-(2-cyclohex-1-en-1-ylethyl)isoxazole-4-carboxamide; 1099) 5-amino-3-(1-benzofuran-3-yl)-N-(1,2-dimethylpropyl)isoxazole-4-carboxamide; 1100) 5-amino-3-(1-benzofuran-3-yl)-N-(3,3-diphenylpropyl)isoxazole-4-carboxamide; 1101) 5-amino-3-(1-benzofuran-3-yl)-N-(1,2-diphenylethyl)isoxazole-4-carboxamide; 1102) 5-amino-3-(1-benzofuran-3-yl)-N-(2,4-dimethoxybenzyl)isoxazole-4-carboxamide; 1103) 5-amino-3-(1-benzofuran-3-yl)-N-[3-(dibutylamino)propyl]isoxazole-4-carboxamide; 1104) 5-amino-3-(1-benzofuran-3-yl)-N-butylisoxazole-4-carboxamide; 1105) 5-amino-3-(1-benzofuran-3-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1106) 5-amino-3-(1-benzofuran-3-yl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 1107) 5-amino-3-(1-benzofuran-3-yl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 1108) 5-amino-3-(1-benzofuran-3-yl)-N-(1-benzylpiperidin-4-yl)isoxazole-4-carboxamide; 1109) 5-amino-3-(1-benzofuran-3-yl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 1110) 5-amino-3-(1-benzofuran-3-yl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 1111) 5-amino-3-(1-benzofuran-3-yl)-N-(3-fluorobenzyl)isoxazole-4-carboxamide; 1112) 5-amino-3-(1-benzofuran-3-yl)-N-(1,3-dimethylbutyl)isoxazole-4-carboxamide; 1113) 5-amino-3-(1-benzofuran-3-yl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 1114) 5-amino-3-(1-benzofuran-3-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 1115) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(1-benzofuran-3-yl)isoxazole-4-carboxamide; 1116) 5-amino-3-(1-benzofuran-3-yl)-N-pentylisoxazole-4-carboxamide; 1117) 5-amino-3-(1-benzofuran-3-yl)-N-(cyclohexylmethyl)isoxazole-4-carboxamide; 1118) ethyl 4-({[5-amino-3-(1-benzofuran-3-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 1119) 5-amino-3-(1-benzofuran-3-yl)-N-[2-(3-chlorophenyl)ethyl]isoxazole-4-carboxamide; 1120) 5-amino-3-(1-benzofuran-3-yl)-N-(1-ethylpropyl)isoxazole-4-carboxamide; 1121) 5-amino-3-(1-benzofuran-3-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 1122) 5-amino-3-(1-benzofuran-3-yl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 1123) 5-amino-3-(1-benzofuran-3-yl)-N-cyclobutylisoxazole-4-carboxamide; 1124) 5-amino-N-benzhydryl-3-(1-benzofuran-3-yl)isoxazole-4-carboxamide; 1125) 5-amino-3-(1-benzofuran-3-yl)-N-octylisoxazole-4-carboxamide; 1126) 5-amino-3-(1-benzofuran-3-yl)-N-(2-bromobenzyl)isoxazole-4-carboxamide; 1127) 5-amino-3-(1-benzofuran-3-yl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 1128) 5-amino-3-(1-benzofuran-3-yl)-N-heptylisoxazole-4-carboxamide; 1129) 5-amino-3-(1-benzofuran-3-yl)-N-(tert-butyl)isoxazole-4-carboxamide; 1130) 5-amino-3-(1-benzofuran-3-yl)-N-(3,4-dimethoxybenzyl)isoxazole-4-carboxamide; 1131) 5-amino-3-(1-benzofuran-3-yl)-N-(2,3-dihydro-1H-inden-1-yl)isoxazole-4-carboxamide; 1132) 5-amino-3-(1-benzofuran-3-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1133) 5-amino-N-benzyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1134) 5-amino-3-(5-ethylthien-2-yl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 1135) 5-amino-3-(5-ethylthien-2-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 1136) 5-amino-N-(sec-butyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1137) 5-amino-N-cyclohexyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1138) 5-amino-3-(5-ethylthien-2-yl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 1139) 5-amino-3-(5-ethylthien-2-yl)-N-hexylisoxazole-4-carboxamide; 1140) 5-amino-3-(5-ethylthien-2-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 1141) 5-amino-N-cyclopentyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1142) 5-amino-N-(1,5-dimethylhexyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1143) 5-amino-3-(5-ethylthien-2-yl)-N-isopentylisoxazole-4-carboxamide; 1144) 5-amino-N-(2-ethylhexyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1145) 5-amino-3-(5-ethylthien-2-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 1146) 5-amino-3-(5-ethylthien-2-yl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 1147) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1148) 5-amino-3-(5-ethylthien-2-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1149) 5-amino-3-(5-ethylthien-2-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 1150) 5-amino-3-(5-ethylthien-2-yl)-N-isobutylisoxazole-4-carboxamide; 1151) 5-amino-3-(5-ethylthien-2-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1152) 5-amino-3-(5-ethylthien-2-yl)-N-(2-methoxybenzyl)isoxazole-4-carboxamide; 1153) 5-amino-3-(5-ethylthien-2-yl)-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 1154) 5-amino-N-(3,4-difluorobenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1155) 5-amino-N-(3-chlorobenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1156) 5-amino-N-(2-chlorobenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1157) 5-amino-3-(5-ethylthien-2-yl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 1158) 5-amino-3-(5-ethylthien-2-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 1159) 5-amino-N-(cyclopropylmethyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1160) 5-amino-N-cycloheptyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1161) 5-amino-3-(5-ethylthien-2-yl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 1162) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1163) 5-amino-N-(1,2-dimethylpropyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1164) 5-amino-N-(3,3-diphenylpropyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1165) 5-amino-N-(1,2-diphenylethyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1166) 5-amino-N-(2,4-dimethoxybenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1167) 5-amino-N-[3-(dibutylamino)propyl]-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1168) 5-amino-N-butyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1169) 5-amino-3-(5-ethylthien-2-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1170) 5-amino-3-(5-ethylthien-2-yl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 1171) 5-amino-3-(5-ethylthien-2-yl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 1172) 5-amino-3-(5-ethylthien-2-yl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 1173) 5-amino-N-(4-tert-butylcyclohexyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1174) 5-amino-3-(5-ethylthien-2-yl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 1175) 5-amino-3-(5-ethylthien-2-yl)-N-(3-fluorobenzyl)isoxazole-4-carboxamide; 1176) 5-amino-3-(5-ethylthien-2-yl)-N-(4-methylbenzyl)isoxazole-4-carboxamide; 1177) 5-amino-N-(1,3-dimethylbutyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1178) 5-amino-3-(5-ethylthien-2-yl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 1179) 5-amino-3-(5-ethylthien-2-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 1180) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1181) 5-amino-3-(5-ethylthien-2-yl)-N-pentylisoxazole-4-carboxamide; 1182) 5-amino-N-(cyclohexylmethyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1183) ethyl 4-({[5-amino-3-(5-ethylthien-2-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 1184) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1185) 5-amino-N-(1-ethylpropyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1186) 5-amino-3-(5-ethylthien-2-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 1187) 5-amino-3-(5-ethylthien-2-yl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 1188) 5-amino-N-cyclobutyl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1189) 5-amino-N-benzhydryl-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1190) 5-amino-3-(5-ethylthien-2-yl)-N-octylisoxazole-4-carboxamide; 1191) 5-amino-N-(2-bromobenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1192) 5-amino-3-(5-ethylthien-2-yl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 1193) 5-amino-3-(5-ethylthien-2-yl)-N-heptylisoxazole-4-carboxamide; 1194) 5-amino-N-(tert-butyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1195) 5-amino-N-(3,4-dimethoxybenzyl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1196) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(5-ethylthien-2-yl)isoxazole-4-carboxamide; 1197) 5-amino-3-(5-ethylthien-2-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1198) 5-amino-N-benzyl-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1199) 5-amino-3-(5-chloro-2-furyl)-N-(2-furylmethyl)isoxazole-4-carboxamide; 1200) 5-amino-3-(5-chloro-2-furyl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 1201) 5-amino-N-(sec-butyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1202) 5-amino-3-(5-chloro-2-furyl)-N-cyclohexylisoxazole-4-carboxamide; 1203) 5-amino-3-(5-chloro-2-furyl)-N-(4-methoxybenzyl)isoxazole-4-carboxamide; 1204) 5-amino-3-(5-chloro-2-furyl)-N-hexylisoxazole-4-carboxamide; 1205) 5-amino-3-(5-chloro-2-furyl)-N-cyclopentylisoxazole-4-carboxamide; 1206) 5-amino-3-(5-chloro-2-furyl)-N-(1,5-dimethylhexyl)isoxazole-4-carboxamide; 1207) 5-amino-3-(5-chloro-2-furyl)-N-isopentylisoxazole-4-carboxamide; 1208) 5-amino-3-(5-chloro-2-furyl)-N-(2-ethylhexyl)isoxazole-4-carboxamide; 1209) 5-amino-3-(5-chloro-2-furyl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 1210) 5-amino-3-(5-chloro-2-furyl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 1211) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1212) 5-amino-3-(5-chloro-2-furyl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1213) 5-amino-3-(5-chloro-2-furyl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 1214) 5-amino-3-(5-chloro-2-furyl)-N-isobutylisoxazole-4-carboxamide; 1215) 5-amino-3-(5-chloro-2-furyl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1216) 5-amino-3-(5-chloro-2-furyl)-N-(2-methoxybenzyl)isoxazole-4-carboxamide 1217) 5-amino-3-(5-chloro-2-furyl)-N-(2-fluorobenzyl)isoxazole-4-carboxamide; 1218) 5-amino-3-(5-chloro-2-furyl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1219) 5-amino-3-(5-chloro-2-furyl)-N-(3,4-difluorobenzyl)isoxazole-4-carboxamide; 1220) 5-amino-N-(3-chlorobenzyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1221) 5-amino-N-(2-chlorobenzyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1222) 5-amino-3-(5-chloro-2-furyl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 1223) 5-amino-3-(5-chloro-2-furyl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 1224) 5-amino-3-(5-chloro-2-furyl)-N-(cyclopropylmethyl)isoxazole-4-carboxamide; 1225) 5-amino-3-(5-chloro-2-furyl)-N-cycloheptylisoxazole-4-carboxamide; 1226) 5-amino-3-(5-chloro-2-furyl)-N-[2-(4-methoxyphenyl)ethyl]isoxazole-4-carboxamide; 1227) 5-amino-3-(5-chloro-2-furyl)-N-(2-cyclohex-1-en-1-ylethyl)isoxazole-4-carboxamide; 1228) 5-amino-3-(5-chloro-2-furyl)-N-(1,2-dimethylpropyl)isoxazole-4-carboxamide; 1229) 5-amino-3-(5-chloro-2-furyl)-N-(3,3-diphenylpropyl)isoxazole-4-carboxamide; 1230) 5-amino-3-(5-chloro-2-furyl)-N-(1,2-diphenylethyl)isoxazole-4-carboxamide; 1231) 5-amino-3-(5-chloro-2-furyl)-N-(2,4-dimethoxybenzyl)isoxazole-4-carboxamide; 1232) 5-amino-3-(5-chloro-2-furyl)-N-[3-(dibutylamino)propyl]isoxazole-4-carboxamide; 1233) 5-amino-N-butyl-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1234) 5-amino-3-(5-chloro-2-furyl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1235) 5-amino-3-(5-chloro-2-furyl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 1236) 5-amino-3-(5-chloro-2-furyl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 1237) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1238) 5-amino-3-(5-chloro-2-furyl)-N-(2-methoxy-1-methylethyl)isoxazole-4-carboxamide; 1239) 5-amino-N-(4-tert-butylcyclohexyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1240) 5-amino-3-(5-chloro-2-furyl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 1241) 5-amino-3-(5-chloro-2-furyl)-N-(3-fluorobenzyl)isoxazole-4-carboxamide; 1242) 5-amino-3-(5-chloro-2-furyl)-N-(4-methylbenzyl)isoxazole-4-carboxamide; 1243) 5-amino-3-(5-chloro-2-furyl)-N-(1,3-dimethylbutyl)isoxazole-4-carboxamide; 1244) 5-amino-3-(5-chloro-2-furyl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 1245) 5-amino-3-(5-chloro-2-furyl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 1246) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1247) 5-amino-3-(5-chloro-2-furyl)-N-pentylisoxazole-4-carboxamide; 1248) 5-amino-3-(5-chloro-2-furyl)-N-(cyclohexylmethyl)isoxazole-4-carboxamide; 1249) ethyl 4-({[5-amino-3-(5-chloro-2-furyl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 1250) 5-amino-3-(5-chloro-2-furyl)-N-[2-(3-chlorophenyl)ethyl]isoxazole-4-carboxamide; 1251) 5-amino-3-(5-chloro-2-furyl)-N-(1-ethylpropyl)isoxazole-4-carboxamide; 1252) 5-amino-3-(5-chloro-2-furyl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 1253) 5-amino-3-(5-chloro-2-furyl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 1254) 5-amino-3-(5-chloro-2-furyl)-N-cyclobutylisoxazole-4-carboxamide; 1255) 5-amino-N-benzhydryl-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1256) 5-amino-3-(5-chloro-2-furyl)-N-octylisoxazole-4-carboxamide; 1257) 5-amino-N-(2-bromobenzyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1258) 5-amino-3-(5-chloro-2-furyl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 1259) 5-amino-3-(5-chloro-2-furyl)-N-heptylisoxazole-4-carboxamide; 1260) 5-amino-N-(tert-butyl)-3-(5-chloro-2-furyl)isoxazole-4-carboxamide; 1261) 5-amino-3-(5-chloro-2-furyl)-N-(3,4-dimethoxybenzyl)isoxazole-4-carboxamide; 1262) 5-amino-3-(5-chloro-2-furyl)-N-(2,3-dihydro-1H-inden-1-yl)isoxazole-4-carboxamide; 1263) 5-amino-3-(5-chloro-2-furyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1264) 5-amino-N-benzyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1265) 5-amino-N-(2-furylmethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1266) 5-amino-3-(6-methoxypyridin-3-yl)-N-(2-phenylethyl)isoxazole-4-carboxamide; 1267) 5-amino-N-(sec-butyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1268) 5-amino-N-cyclohexyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1269) 5-amino-N-(4-methoxybenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1270) 5-amino-N-hexyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1271) 5-amino-3-(6-methoxypyridin-3-yl)-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 1272) 5-amino-N-cyclopentyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1273) 5-amino-N-(1,5-dimethylhexyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1274) 5-amino-N-isopentyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1275) 5-amino-N-(2-ethylhexyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1276) 5-amino-3-(6-methoxypyridin-3-yl)-N-(4-phenylbutyl)isoxazole-4-carboxamide; 1277) 5-amino-3-(6-methoxypyridin-3-yl)-N-(2-methylcyclohexyl)isoxazole-4-carboxamide; 1278) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1279) 5-amino-3-(6-methoxypyridin-3-yl)-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1280) 5-amino-3-(6-methoxypyridin-3-yl)-N-(3-phenylpropyl)isoxazole-4-carboxamide; 1281) 5-amino-N-isobutyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1282) 5-amino-3-(6-methoxypyridin-3-yl)-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1283) 5-amino-N-(2-methoxybenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1284) 5-amino-N-(2-fluorobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1285) 5-amino-3-(6-methoxypyridin-3-yl)-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1286) 5-amino-N-(3,4-difluorobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1287) 5-amino-N-(3-chlorobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1288) 5-amino-N-(2-chlorobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1289) 5-amino-3-(6-methoxypyridin-3-yl)-N-(3-methylbenzyl)isoxazole-4-carboxamide; 1290) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-naphthylmethyl)isoxazole-4-carboxamide; 1291) 5-amino-N-(cyclopropylmethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1292) 5-amino-N-cycloheptyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1293) 5-amino-N-[2-(4-methoxyphenyl)ethyl]-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1294) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1295) 5-amino-N-(1,2-dimethylpropyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1296) 5-amino-N-(3,3-diphenylpropyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1297) 5-amino-N-(1,2-diphenylethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1298) 5-amino-N-(2,4-dimethoxybenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1299) 5-amino-N-[3-(dibutylamino)propyl]-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1300) 5-amino-N-butyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1301) 5-amino-3-(6-methoxypyridin-3-yl)-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1302) 5-amino-3-(6-methoxypyridin-3-yl)-N-[(5-methyl-2-furyl)methyl]isoxazole-4-carboxamide; 1303) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-methylhexyl)isoxazole-4-carboxamide; 1304) 5-amino-N-(1-benzylpiperidin-4-yl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1305) 5-amino-N-(2-methoxy-1-methylethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1306) 5-amino-N-(4-tert-butylcyclohexyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1307) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-methylbutyl)isoxazole-4-carboxamide; 1308) 5-amino-N-(3-fluorobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1309) 5-amino-3-(6-methoxypyridin-3-yl)-N-(4-methylbenzyl)isoxazole-4-carboxamide; 1310) 5-amino-N-(1,3-dimethylbutyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1311) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-methyl-3-phenylpropyl)isoxazole-4-carboxamide; 1312) 5-amino-3-(6-methoxypyridin-3-yl)-N-[3-(methylthio)propyl]isoxazole-4-carboxamide; 1313) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1314) 5-amino-3-(6-methoxypyridin-3-yl)-N-pentylisoxazole-4-carboxamide; 1315) 5-amino-N-(cyclohexylmethyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1316) ethyl 4-({[5-amino-3-(6-methoxypyridin-3-yl)isoxazol-4-yl]carbonyl}amino)piperidine-1-carboxylate; 1317) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1318) 5-amino-N-(1-ethylpropyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1319) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-phenylethyl)isoxazole-4-carboxamide; 1320) 5-amino-3-(6-methoxypyridin-3-yl)-N-(2-methylbenzyl)isoxazole-4-carboxamide; 1321) 5-amino-N-cyclobutyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1322) 5-amino-N-benzhydryl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1323) 5-amino-3-(6-methoxypyridin-3-yl)-N-octylisoxazole-4-carboxamide; 1324) 5-amino-N-(2-bromobenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1325) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1-methylheptyl)isoxazole-4-carboxamide; 1326) 5-amino-N-heptyl-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1327) 5-amino-N-(tert-butyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1328) 5-amino-N-(3,4-dimethoxybenzyl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1329) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-(6-methoxypyridin-3-yl)isoxazole-4-carboxamide; 1330) 5-amino-3-(6-methoxypyridin-3-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide; 1331) 5-amino-N-benzyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1332) 5-amino-N-(2-furylmethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1333) 5-amino-N-(2-phenylethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1334) 5-amino-N-cyclohexyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1335) 5-amino-N-(4-methoxybenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1336) 5-amino-N-hexyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1337) 5-amino-3-pyridin-3-yl-N-(thien-2-ylmethyl)isoxazole-4-carboxamide; 1338) 5-amino-N-cyclopentyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1339) 5-amino-N-(1,5-dimethylhexyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1340) 5-amino-N-isopentyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1341) 5-amino-N-(2-ethylhexyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1342) 5-amino-N-(4-phenylbutyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1343) 5-amino-N-(2-methylcyclohexyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1344) 5-amino-N-[3,5-bis(trifluoromethyl)benzyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1345) 5-amino-3-pyridin-3-yl-N-[3-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1346) 5-amino-N-(3-phenylpropyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1347) 5-amino-N-isobutyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1348) 5-amino-3-pyridin-3-yl-N-[2-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1349) 5-amino-N-(2-methoxybenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1350) 5-amino-N-(2-fluorobenzyl)-3-pyridin3-ylisoxazole-4-carboxamide; 1351) 5-amino-3-pyridin-3-yl-N-[4-(trifluoromethyl)benzyl]isoxazole-4-carboxamide; 1352) 5-amino-N-(3,4-difluorobenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1353) 5-amino-N-(3-chlorobenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1354) 5-amino-N-(2-chlorobenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1355) 5-amino-N-(3-methylbenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1356) 5-amino-N-(1-naphthylmethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1357) 5-amino-N-(cyclopropylmethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1358) 5-amino-N-cycloheptyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1359) 5-amino-N-[2-(4-methoxyphenyl)ethyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1360) 5-amino-N-(2-cyclohex-1-en-1-ylethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1361) 5-amino-N-(1,2-dimethylpropyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1362) 5-amino-N-(3,3-diphenylpropyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1363) 5-amino-N-(1,2-diphenylethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1364) 5-amino-N-(2,4-dimethoxybenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1365) 5-amino-N-[3-(dibutylamino)propyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1366) 5-amino-N-butyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1367) 5-amino-3-pyridin-3-yl-N-[4-(trifluoromethoxy)benzyl]isoxazole-4-carboxamide; 1368) 5-amino-N-[(5-methyl-2-furyl)methyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1369) 5-amino-N-(1-methylhexyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1370) 5-amino-N-(1-methylbutyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1371) 5-amino-N-(3-fluorobenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1372) 5-amino-N-(4-methylbenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1373) 5-amino-N-(1,3-dimethylbutyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1374) 5-amino-N-(1-methyl-3-phenylpropyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1375) 5-amino-N-[3-(methylthio)propyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1376) 5-amino-N-(1,3-benzodioxol-5-ylmethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1377) 5-amino-N-pentyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1378) 5-amino-N-(cyclohexylmethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1379) ethyl 4-{[(5-amino-3-pyridin-3-ylisoxazol-4-yl)carbonyl]amino}piperidine-1-carboxylate; 1380) 5-amino-N-[2-(3-chlorophenyl)ethyl]-3-pyridin-3-ylisoxazole-4-carboxamide; 1381) 5-amino-N-(1-ethylpropyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1382) 5-amino-N-(1-phenylethyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1383) 5-amino-N-(2-methylbenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1384) 5-amino-N-cyclobutyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1385) 5-amino-N-benzhydryl-3-pyridin-3-ylisoxazole-4-carboxamide; 1386) 5-amino-N-octyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1387) 5-amino-N-(2-bromobenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1388) 5-amino-N-(1-methylheptyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1389) 5-amino-N-heptyl-3-pyridin-3-ylisoxazole-4-carboxamide; 1390) 5-amino-N-(tert-butyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1391) 5-amino-N-(3,4-dimethoxybenzyl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1392) 5-amino-N-(2,3-dihydro-1H-inden-1-yl)-3-pyridin-3-ylisoxazole-4-carboxamide; 1393) 5-amino-3-pyridin-3-yl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)isoxazole-4-carboxamide. 24. A process for preparing the compounds of formula (I) and the pharmaceutically acceptable salts, as defined in claim 13, which process comprises: a) reacting a compound of formula (II) with a compound of formula (III) wherein R, R1 and X are as above defined and Z represents a halogen atom or a suitable leaving group, so as to obtain a compound of formula (I) and, optionally, reacting the compound of formula (I) according to any one of the alternative steps b) below b.1) with a compound of formula (IV), (V) or (VI) R2—COW (IV), R2—SO2W′ (V), R2—NCO (VI) wherein R2 is as above defined, W is hydroxy or a suitable leaving group and W′ is a suitable leaving group, so as to obtain the compounds of formula (I) wherein Y is —CO—, —SO2— or —CONH—, respectively, and R, R1, R2 and X are as above defined; b.2) with a suitable aldehyde or ketone derivative of formula (VII) R2—CO—R3 (VII) wherein R2 and R3 are as above defined, under reductive conditions, so as to obtain a compound of formula (I) wherein Y is a group —CH(R3)— and R, R1, R2, R3 and X are as above defined; b.3) with a suitable acylating agent in the presence of ammonia, so as to obtain a compound of formula (I) wherein Y is —CONH—, R2 is hydrogen and R, R1 and X are as above defined; and, optionally c) converting the thus obtained compound of formula (I) into another compound of formula (I) and/or into a pharmaceutically acceptable salt thereof. 25. The process of claim 24 wherein, within the compound of formula (IV) or (V) in step b.1), W is hydroxy or a chlorine or bromine atom and W′ is a chlorine or bromine atom. 26. The process of claim 24 wherein, within step b.2), reductive conditions occur in the presence of sodium borohydride, sodium cyanoborohydride or sodium triacetoxyborohydride. 27. The process of claim 24 wherein, in step b.3), the acylating agent is selected from triphosgene or trichloromethyl chloroformate. 28. A process under solid phase synthesis (SPS) conditions for preparing the compounds of formula (I) and the pharmaceutically acceptable salts, as defined in claim 13, which process comprises: a′) reacting cyanoacetic acid with a suitable polystyrenic resin of formula (X) or (XI) Resin-W (X), Resin-NHR1 (XI) wherein R1 is as above defined and W is hydroxy or a suitable leaving group, so as to obtain the compounds of formula (XII) or (XIII), respectively wherein R1 is as above reported; b′) reacting any one of the compounds of formula (XII) or (XIII) with a compound of formula (II) wherein R and Z are as above defined, so as to obtain a compound of formula (XIV) or (XV) c′) cleaving the resin from the compounds of formula (XIV) or (XV) under acidic or basic conditions, so as to obtain a compound of formula (I) wherein X is a group —O— and R1 is hydrogen, or X is a group —N(R3)— wherein R3 is hydrogen and R1 is as above defined, respectively; or, alternatively, reacting the above compounds of formula (XIV) or (XV) according to any one of the alternative steps d′) below d.1′) with a compound of formula (IV), (V) or (VI) R2—COW (IV), R2—SO2W′ (V), R2—NCO (VI) wherein R2 is as above defined, W is hydroxy or a suitable leaving group and W′ is a suitable leaving group, so as to obtain the compounds of formula (XVI) or (XVII) wherein Y is —CO—, —SO2— or —CONH—, respectively, and R, R1 and R2 are as above defined; d.2′) with a suitable aldehyde or ketone derivative of formula (VII) R2—CO—R3 (VII) wherein R2 and R3 are as above defined, under reductive conditions, so as to obtain the compounds of the above formula (XVI) or (XVII) wherein Y is a group —CH(R3)— and R, R1, R2 and R3 are as above defined; d.3′) with a suitable acylating agent in the presence of ammonia, so as to obtain a compound of the above formula (XVI) or (XVII) wherein Y is —CONH—, R2 is hydrogen and R and R1 are as above defined; e′) cleaving the resin from the compounds of formula (XVI) or (XVII) under acidic or basic conditions, so as to obtain a compound of formula (I) wherein X is a group —O— and R1 is hydrogen, or X is a group —N(R3)— wherein R3 is hydrogen and R1 is as above defined, respectively; and, optionally, f′) converting the thus obtained compound of formula (I) into another compound of formula (I) and/or into a pharmaceutically acceptable salt thereof. 29. A library of two or more compounds of formula (I) wherein R is an optionally substituted 5 or 6 membered heteroaryl group with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur, optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; X is a divalent group selected from —N(R3)— or —O—; Y is a divalent group selected from —CH(R3)—, —CO—, —CONH— or —SO2—, or Y may also be a single bond when R2 is a hydrogen atom or a C3-C6 cycloalkyl group; R1 is a hydrogen atom or a group, optionally further substituted, selected from straight or branched C1-C6 alkyl, C3-C6 cycloalkyl, aryl or aryl C1-C6 alkyl, 5 or 6 membered heterocyclyl or heterocyclyl C1-C6 alkyl having from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; the said cycloalkyl, aryl or heterocyclyl groups being optionally further condensed with a 5 to 7 membered aromatic or non-aromatic carbocycle or heterocycle with from 1 to 3 heteroatoms selected among nitrogen, oxygen or sulfur; R2 and R3 have, each independently, the meanings above reported for R1 or represent an optionally substituted straight or branched C2-C6 alkenyl or alkynyl group; and the pharmaceutically acceptable salts thereof. 30. Any specific compound of formula (I), as defined in claim 13, which is obtainable, for instance through a combinatorial chemistry technique as per the process of claim 28, by reacting each of the derivatives of formula (II), as set forth in table I, with any one of the derivatives of formula (XIII) which are obtainable from the amines of formula (IX), as set forth in table II, and by subsequently reacting any one of the obtained derivatives of formula (XV) with any one of the derivatives of formula (IV), as set forth in table III. 31. Any specific compound of formula (I), as defined in claim 13, which is obtainable, for instance through a combinatorial chemistry technique as per the process of claim 28, by reacting each of the derivatives of formula (II), as set forth in table I, with any one of the derivatives of formula (XIII) which are obtainable from the amines of formula (IX), as set forth in table II, and by subsequently reacting any one of the obtained derivatives of formula (XV) with any one of the derivatives of formula (V), as set forth in table IV. 32. Any specific compound of formula (I), as defined in claim 13, which is obtainable, for instance through a combinatorial chemistry technique as per the process of claim 28, by reacting each of the derivatives of formula (II), as set forth in table I, with any one of the derivatives of formula (XIII) which are obtainable from the amines of formula (IX), as set forth in table II, and by subsequently reacting any one of the obtained derivatives of formula (XV) with any one of the derivatives of formula (VI), as set forth in table V. 33. A pharmaceutical composition comprising an effective amount of an aminoisoxazole of formula (I) as defined in claim 13 and, at least, one pharmaceutically acceptable excipient, carrier or diluent. 34. A pharmaceutical composition according to claim 33 further comprising one or more chemotherapeutic agents, as a combined preparation for simultaneous, separate or sequential use in anticancer therapy. 35. A product or kit comprising a compound of claim 13 or a pharmaceutical composition thereof as defined in claim 34, and one or more chemotherapeutic agents, as a combined preparation for simultaneous, separate or sequential use in anticancer therapy. 36. A compound of formula (I) or a pharmaceutically acceptable salt thereof, as defined in claim 13, for use as a medicament. 37. Use of a compound of formula (I) or a pharmaceutically acceptable salt thereof, as defined in claim 13, in the manufacture of a medicament for treating diseases caused by and/or associated with an altered protein kinase activity. 38. Use according to claim 37 for treating tumors. |
Ionic and non-ionic radiograhic contrast agents for use in combined x-ray and nuclear magnetic resonance diagnostics |
The invention discloses the use of ionic and non-ionic radiographic contrast agents for combined X-ray and nuclear magnetic resonance (MRI) diagnostics. |
1. The use of a iodinated contrast agent comprising at least one amido function for the preparation of a diagnostic formulation for obtaining in vivo or in vitro images with magnetization transfer MRI techniques, wherein the iodinated contrast agents comprising at least one amido function are iodinated aromatic compounds having a triiodinated aromatic ring bearing at the remaining positions straight or branched, functionally substituted organic residues or compounds comprising at least two triiodinated aromatic residues mutually covalently linked at one of the positions, either directly or through a straight or branched, functionally substituted organic residue, said aromatic ring being further substituted at the remaining positions by straight or branched, functionally substituted organic residues and in which the organic residues and the triiodinated aromatic ring are linked by amido functions. 2. The use as claimed in claim 1 wherein magnetization transfer is coupled to “gradient or field echo” or “spin echo and fast spin echo” sequences. 3. The use as claimed in claims 1 or 2 wherein the iodinated contrast agents are compounds of formula (I): in which: A, D, E, which can be the same or different, are groups of formula —CON(R)R1, —COOH, —CONH2 or —N(R)—COR2 or CH2N(R)—COR2; R is H or R1, with the proviso that the substituent R is H in at least one group of the compound; R1 is a straight or branched (C1-C6)alkyl residue, optionally substituted with 1-5 hydroxy and/or alkoxy and/or hydroxy-alkoxy groups, or with a NH—CO—R1 or —CO—N(R)R1 group, or R1 is a carbohydrate residue; R2 is a straight or branched (C1-C6)alkyl residue, optionally substituted with 1-5 hydroxy and/or alkoxy and/or hydroxyalkoxy groups and optionally interrupted by an oxo group. 4. The use as claimed in any one of claims 1 to 3 wherein the iodinated contrast agents are compounds of formula (II): in which: A, D and E are as defined above; B and B′, which can be the same or different, are selected from —CO—N(R)—, —N(R)—CO— or —N(COR3)— groups, in which R is H or a residue of a straight or branched (C1-C6)alkyl group, optionally substituted with 1-5 hydroxy and/or alkoxy and/or hydroxyalkoxy groups; R3 is a (C1-C3)alkyl residue, optionally substituted with 1-2 hydroxy or alkoxy or hydroxyalkoxy groups; X is a covalent bond or a straight or branched (C1-C8)alkylene chain, optionally substituted with 1-6 hydroxy and/or —CO—NHR groups, and optionally interrupted by —O—, —S—, —N—, —N(R)—CO groups; in case both groups B and X are absent, the two aromatic compounds are directly linked with a covalent bond with the proviso that the substituent R is H in at least one group of the compound. 5. The use as claimed in any one of claims 1 to 3 wherein the iodinated contrast agents are compounds of formula (III): in which R4, R5, which can be the same or different, are H or a straight or branched (C1-C3)alkyl group, which can optionally be substituted with 1-2 hydroxy and/or alkoxy and/or hydroxyalkoxy groups; R6 is a straight or branched (C1-C4)alkyl group containing one or more hydroxy, alkoxy or acyloxy groups. 6. The use as claimed in any one of claims 1 to 3 wherein the iodinated contrast agents are compounds of formula (IV): in which: A′ is a OH or —NHR1 group; R1 is a straight or branched (C1-C6)alkyl group, optionally substituted with 1-5 hydroxy and/or alkoxy and/or hydroxyalkoxy groups, or by a —NH—CO—R1 or —CO—NHR1 group, or R1 is a carbohydrate residue; B″ and B′″, which can be the same or different, are H or R1, as defined above; R7 and R8, which can be the same or different, are H, an acyl —COR1 group, an alkyl group, a mono or polyhydroxyalkyl group or a carbohydrate residue; with the proviso that at least one of the groups B″, B′″, R7 or R8 is H. 7. The use as claimed in any one of claims 1 to 6 wherein the contrast agents are selected from Iopamidol, Iofratol, Ioprormide, Metrizamide, Iogulamide, loglunide, Iobitridol, Iodamide, Sodium diatrizoate and other diatrizoic acid salts, and combinations thereof. 8. The use as claimed in any one of claims 1 to 7 wherein MRI images are acquired before, during and after irradiation in the used radiofrequency field. 9. The use as claimed in claim 8 for radiographic and magnetic resonance imaging in myclographic, urographic, cerebral or peripheral angiographic, cardiographic, coronary arteriographic or aortograpbic, artrographic intravascular imaging investigations. 10. The use as claimed in claim 9 wherein the radiological investigation is carried out in vivo or in vitro before or after the magnetization transfer magnetic resonance investigation. 11. The use as claimed in any one of claims 1 to 10 wherein the diagnostic composition consists of a liposome suspension of the iodinated contrast agents together with suitable excipients. 12. The use as claimed in any one of claims 1 to 11 wherein the saturation transfer to water depends on the pH of the solution or on the concerned body district. 13. The use as claimed in any one of claims 1 to 12, wherein the saturation transfer to water depends on the temperature of the solution or on the concerned body district. |
Chemo-enzymatic synthesis of sialylated oligosaccharides |
In vitro/cell-free process of preparing a sialylated oligosaccharides are described. The sialylated oligosaccharides include gangliosides. The oligosaccharides linked to various moieties including sphingoids and ceramides. Novel compounds that comprise sphingoid groups are disclosed. The compounds include sialylated oligosaccharides including gangliosides as well as various sphingoids and ceramides. |
1. An in vitro, cell-free, enzymatic method for preparing a compound having the formula: in which X1 is a member selected from substituted or unsubstituted alkyl, a detectable label and a targeting moiety; X is a member selected from: wherein m is an integer from 0 to 20; Q is a member selected from: n, o and s are integers independently selected from 0 to 20; said method comprising: (a) contacting with a trans-sialidase and a Sia donor, a substrate having the structure: under conditions appropriate for said trans-sialidase to transfer a Sia moiety from said donor to said substrate, thereby forming said compound. 2. The method according to claim 1, further comprising: (b) contacting the compound formed in step (a) with a GalNAc-transferase and a GalNAC donor under conditions appropriate for said GalNAc-transferase to transfer a GalNAc moiety from said donor to said compound formed in step (a). 3. The method according to claim 2, further comprising: (c) contacting the compound formed in step (b) with a Gal-transferase and a Gal donor under conditions appropriate for said Gal-transferase to transfer a Gal moiety from said donor to said compound formed in step (b). 4. The method according to claim 3, further comprising: (d) contacting the compound formed in step (c) with a trans-sialidase and a Sia donor under conditions appropriate for said trans-sialidase to transfer a Sia moiety from said donor to said compound formed in step (c). 5. The method according to claim 4, further comprising: (e) contacting the compound formed in step (d) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (d). 6. The method according to claim 3, further comprising: (d) contacting the compound formed in step (c) with a Fuc-transferase and a Fuc donor under conditions appropriate for said Fuc-transferase to transfer a Fuc moiety from said donor to said compound formed in step (c). 7. The method of claim 1, further comprising: (b) contacting the compound formed in step (a) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (a). 8. The method of claim 7, further comprising: (c) contacting the compound formed in step (b) with a GalNAc-transferase and a GalNAc donor under conditions appropriate for said GalNAc-transferase to transfer a GalNAc moiety from said donor to said compound formed in step (b). 9. The method of claim 8, further comprising: (d) contacting the compound formed in step (c) with a Gal-transferase and a Gal donor under conditions appropriate for said Gal-transferase to transfer a Gal moiety from said donor to said compound formed in step (c). 10. The method of claim 9, further comprising: (e) contacting the compound formed in step (d) with a trans-sialidase and a Sia donor under conditions appropriate for said trans-sialidase transfer a Sia moiety from said donor to said compound formed in step (d). 11. The method of claim 10, further comprising: (f) contacting the compound formed in step (e) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (e). 12. The method of claim 7, further comprising: (c) contacting the compound formed in step (b) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (b). 13. The method of claim 12, further comprising: (d) contacting the compound formed in step (c) with a GalNAc-transferase and a GalNAc donor under conditions appropriate for said GalNAc-transferase to transfer a GalNAc moiety from said donor to said compound formed in step (c). 14. The method of claim 13, further comprising: (e) contacting the compound formed in step (d) with a Gal-transferase and a Gal donor under conditions appropriate for said Gal-transferase to transfer a Gal moiety from said donor to said compound formed in step (d). 15. The method of claim 14, further comprising: (f) contacting the compound formed in step (e) with a trans-sialidase and a Sia donor under conditions appropriate for said trans-sialidase to transfer a Sia moiety from said donor to said compound formed in step (e). 16. The method of claim 1, further comprising: (g) prior to step (a), contacting a substrate having the formula: Q-Glc-X1 with a Gal-transferase and a Gal donor under conditions appropriate for said Gal-transferase to transfer a Gal moiety from said donor to said substrate 17. The method of claim 1, further comprising: (g) prior to step (a), contacting a substrate having the formula: Q-Gal-Glc-X1 with a GalNAc-transferase and a GalNAc donor under conditions appropriate for said GalNAc-transferase to transfer a GalNAc moiety from said donor to said substrate. 18. The method according claim 17, further comprising: (h) contacting the compound formed in step (g) with a Gal-transferase and a Gal donor under conditions appropriate for said Gal-transferase to transfer a Gal moiety from said donor to said compound formed in step (g). 19. The method of claim 18, further comprising: (i) following step (a), contacting the compound formed in step (a) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (a). 20. The method of claim 19, further comprising: (j) repeating step (i) a selected number of times, thereby forming a poly(sialic acid) substituent on said compound. 21. The method of claim 1, further comprising: (k) contacting the compound formed in step (a) with a Sia-transferase and a Sia donor under conditions appropriate for said Sia-transferase to transfer a Sia moiety from said donor to said compound formed in step (a). 22. The method of claim 21, further comprising: (l) repeating step (k) a selected number of times, thereby forming a poly(sialic acid) substituent on said compound. 23. The method of claim 1, wherein X1 is: in which Z is selected from O, S and NR5; R1 and R2 are members independently selected from NHR4, SR4, OR4, OCOR4, OC(O)NHR4, NHC(O)OR4, OS(O)2OR4, C(O)R4, NHC(O)R4, detectable labels, and targeting moieties in which R4 and R5 are members independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, detectable labels and targeting moieties; and R3 is substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl groups. 24. The method according to claim 23, wherein R1 is a member selected from NH2, OH and SH, said method further comprising acylating R1. 25. The method of claim 23, wherein X1 is: wherein R6 is a member selected from H, C(O)R7, detectable labels, and targeting moieties in which R7 is a member selected from substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, detectable labels and targeting moieties. 26. The method according to claim 25, wherein said compound is a member selected from GM2, GM1, GD1a. GT1a, Fuc-GM1, GD3, GD2, GD1b, GT1b, GQ1b, GM1b, GD1α, GT1β, GQ1B, GT3, GT2, GT1c, GQ1c, globosindes, and polysialylated lactose. 27. A compound having the formula: in which Z is selected from O, S and NR5; R1 and R2 are members independently selected from NHR4, SR4, OR4, OCOR4, OC(O)NHR4, NHC(O)OR4, OS(O)2OR4, C(O)R4, NHC(O)R4, detectable labels, and targeting moieties in which R4 and R5 are members independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, detectable labels and targeting moieties; Sac is a member selected from mono- and oligo-saccharide; and R3 is substituted or unsubstituted alkyl having at least two degrees of unsaturation and substituted or unsubstituted heteroalkyl groups. 28. The compound according to claim 27 wherein R3 is unsubstituted alkyl having two double bonds, and Sac is other than glucosyl. 29. The compound according to claim 27, wherein R3 includes at least one triple bond. 30. The compound according to claim 27, wherein said compound is a member selected from d18:2 and d18:1:1. 31. A pharmaceutical formulation comprising a compound according to claim 27 in admixture with a pharmaceutically acceptable excipient. |
<SOH> BACKGROUND OF THE INVENTION <EOH>1. Field of the Invention This invention pertains to the field of methods for preparing oligosaccharides that include one or more sialyl groups. 2. Background Gangliosides are a class of glycosphingolipids that have a structure containing a carbohydrate moiety linked to a ceramide. The carbohydrate moiety includes at least one monosaccharide and a sialic acid moiety. The sialic acid moiety is composed of one or more sialic acid groups (N-acetyl or N-glycolyl neuraminic acid). Gangliosides are classified according to the number of monosaccharides in the sugar moiety and the number of sialic acid groups present in the structure. Gangliosides are known as mono-, di-, tri- or poly-sialogangliosides, depending upon the number of sialic acid residues. Abbreviations employed to identify these molecules include “GM1”, “GD3”, “GT1”, etc., with the “G” standing for ganglioside, “M”, “D” or “T”, etc. referring to the number of sialic acid residues, and the number or number plus letter (e.g., “GT1a”), referring to the elution order in a TLC assay observed for the molecule. See, Lehninger, Biochemistry, pg. 294-296 (Worth Publishers, 1981); Wiegandt, Glycolipids: New Comprehensive Biochemistry (Neuberger et al., ed., Elsevier, 1985), pp. 199-260. For example, the international symbol GM 1a designates one of the more common gangliosides, which has been extensively studied. The “M” in the symbol indicates that the ganglioside is a monosialoganglioside and “1” defines its position in a TLC elution profile. The subscripts “a”, “b” or “c” also indicate the positions in a TLC assay of the particular ganglioside. The terminal saccharide is the saccharide, which is located at the end of the carbohydrate moiety, which is opposite to the end that is attached to the ceramide moiety. Hundreds of glycosphingolipids (GSLs) are derived from glucosylceramide (GlcCer), which is enzymatically formed from ceramide and UDP-glucose. The enzyme involved in GlcCer formation is UDP-glucose:N-acylsphingosine glucosyltransferase (GlcCer synthase). The rate of GlcCer formation under physiological conditions may depend on the tissue level of UDP-glucose, which in turn depends on the level of glucose in a particular tissue (Zador, I. Z. et al., J. Clin. Invest. 91: 797-803 (1993)). In vitro assays based on endogenous ceramide yield lower synthetic rates than mixtures containing added ceramide, suggesting that tissue levels of ceramide are also normally rate-limiting (Brenkert, A. et al., Brain Res. 36: 183-193 (1972)). The level of GSLs controls a variety of cell functions, such as growth, differentiation, adhesion between cells or between cells and matrix proteins, binding of microorganisms and viruses to cells, and metastasis of tumor cells. In addition, the GlcCer precursor, ceramide, may cause differentiation or inhibition of cell growth (Bielawska, A. et al., FEBS Letters 307: 211-214 (1992)) and be involved in the functioning of vitamin D 3 , tumor necrosis factor-α, interleukins, and apoptosis (programmed cell death). The sphingols (sphingoid bases), precursors of ceramide, and products of ceramide catabolism, have also been shown to influence many cell systems, possibly by inhibiting protein kinase C (PKC). Gangliosides are known to be functionally important in the nervous system and it has been claimed that gangliosides are useful in the therapy of peripheral nervous system disorders. Numerous gangliosides and derivatives thereof have been used to treat a wide variety of nervous system disorders including Parkinson's disease (Ganglioside GM 1 is currently being used in phase II clinical development for the treatment of Parkinson's Disease (FIDIA, Italy)), and cerebral ischemic strokes (see, U.S. Pat. Nos. 4,940,694; 4,937,232; and 4,716,223). Gangliosides have also been used to affect the activity of phagocytes (U.S. Pat. No. 4,831,021) and to treat gastrointestinal disease-producing organisms (U.S. Pat. No. 4,762,822). The gangliosides GM 2 and GD 2, purified from animal brain, have been conjugated to keyhole limpet hemacyanin (KLH) and mixed with adjuvant QS21, and used to elicit immune responses to these gangliosides, as the basis of a cancer vaccine in phase II and III trials (Progenics, Tarrytown, N.Y.). Ganglioside GM 3 is being investigated for use as an anti-cancer agent (WO 98/52577; Nole et al., Exp. Neurology 168: 300-9 (2001)). )). Glycolipids are also of interest in the treatment of inflammatory bowel disease. See, Tubaro et al., Naunyx - Schmiedebergg's Arch. Pharmacol. 348: 670-678 (1993). Gangliosides are generally isolated via purification from tissue, particularly from animal brain (G LYCOLIPID M ETHODOLOGY, Lloyd A. Witting Ed., American Oil Chemists Society, Champaign, III. 187-214 (1976); U.S. Pat. Nos. 5,844,104; 5,532,141; Sonnino et al., J. Lipid Res. 33: 1221-1226 (1992); Sonnino et al., Ind. J. Biochem. Biophys., 25: 144-149 (1988); Svennerholm, Adv. Exp. Med. Biol. 125: 533-44 (1980)). Gangliosides have been isolated from bovine buttermilk (Ren et al., J. Bio. Chem. 267: 12632-12638 (1992); Takamizawa et al., J. Bio. Chem. 261: 5625-5630(1986)). Even under optimum conditions, the yields of pure gangliosides, e.g., GM2 and GM3, are vanishingly small. Moreover, purification from mammalian tissue carries with it the risk of transmitting contaminants such as viruses, prion particles, and so forth. Alternate methodologies for securing ganglioside specific antibodies are thus highly desirable. Due to the importance of gangliosides, efforts have been expended to develop methods of synthesizing pure gangliosides in high yields. Methods of chemically synthesizing gangliosides are described in Hasegawa et al., J. Carbohydrate Chemistry, 11(6): 699-714 (1992) and Sugimoto et al., Carbohydrate Research, 156: C1-C5 (1986). U.S. Pat. No. 4,918,170 discloses the synthesis of GM3 and GM4. Schmidt et al. describe the chemical synthesis of GM3 (U.S. Pat. No. 5,977,329). The references describe multi-step synthetic procedures using laborious protection-activation-coupling-deprotection strategies, at each step of which the intermediate is purified, generally by a combination of extraction and column chromatography. Moreover, none of the synthetic methods is appropriate for the large-scale preparation of gangliosides. In view of the difficulties associated with the chemical synthesis of carbohydrates, the use of enzymes to synthesize the carbohydrate portions of glycoproteins is a promising approach to preparing glycoproteins. Enzyme-based syntheses have the advantages of regioselectivity and stereoselectivity. Moreover, enzymatic syntheses can be performed using unprotected substrates. Three principal classes of enzymes are used in the synthesis of carbohydrates, glycosyltransferases (e.g., sialyltransferases, oligosaccharyltransferases, N-acetylglucosaminyltransferases), Glycoaminidases (e.g., PNGase F) and Glycosidases. The glycosidases are further classified as exoglycosidases (e.g., β-mannosidase, β-glucosidase), and endoglycosidases (e.g., Endo-A, Endo-M). Each of these classes of enzymes has been successfully used to prepare carbohydrates. For a general review, see, Crout et al., Curr. Opin. Chem. Biol. 2: 98-111 (1998) and Arsequell, supra. Glycosyltransferases have been used to prepare oligosaccharides, and have been shown to be very effective for producing specific products with good stereochemical and regiochemical control. For example, β-1,4-galactosyltransferase was used to synthesize lactosamine, illustrating the utility of glycosyltransferases in the synthesis of carbohydrates (see, e.g., Wong et al., J. Org. Chem. 47: 5416-5418 (1982)). Moreover, numerous synthetic procedures have made use of α-sialyltransferases to transfer sialic acid from cytidine-5′-monophospho-N-acetylneuraminic acid to the 3-OH or 6-OH of galactose (see, e.g., Kevin et al., Chem. Eur. J. 2: 1359-1362 (1996)). For a discussion of recent advances in glycoconjugate synthesis f6r therapeutic use, see, Koeller et al., Nature Biotechnology 18: 835-841 (2000). Glycosidases normally catalyze the hydrolysis of a glycosidic bond, however, under appropriate conditions they can be used to form this linkage. Most glycosidases used for carbohydrate synthesis are exoglycosidases; the glycosyl transfer occurs at the non-reducing terminus of the substrate. The glycosidase takes up a glycosyl donor in a glycosyl-enzyme intermediate that is either intercepted by water to give the hydrolysis product, or by an acceptor, to give a new glycoside or oligosaccharide. An exemplary pathway using a exoglycoside is the synthesis of the core trisaccharide of all N-linked glycoproteins, including the notoriously difficult β-mannoside linkage, which was formed by the action of β-mannosidase (Singh et al., Chem. Commun. 993-994 (1996)). Although their use is less common than that of the exoglycosidases, endoglycosidases have also been utilized to prepare carbohydrates. Methods based on the use of endoglycosidases have the advantage that an oligosaccharide, rather than a monosaccharide, is transferred. Oligosaccharride fragments have been added to substrates using endo-β-N-acetylglucosamines such as endo-F, endo-M (Wang et al., Tetrahedron Lett. 37: 1975-1978); and Haneda et al., Carbohydr. Res. 292: 61-70 (1996)). Methods combining both chemical and enzymatic synthetic elements are also known. For example, Yamamoto and coworkers ( Carbohydr. Res. 305: 415-422 (1998)) reported the chemoenzymatic synthesis of the substrate, glycosylated Peptide T, using an endoglyosidase. The N-acetylglucosaminyl peptide was synthesized by purely chemical means. The peptide was subsequently enzymatically elaborated with the oligosaccharide of human transferrin substrate. The saccharide portion was added to the peptide by treating it with an endo-β-N-acetylglucosaminidase. The resulting glycosylated peptide was highly stable and resistant to proteolysis when compared to the peptide T and N-acetylglucosaminyl peptide T. Despite the many advantages of the enzymatic synthesis methods set forth above, in some cases, deficiencies remain. Since the biological activity of many commercially important recombinantly and transgenically produced substrates depends upon the presence of a particular glycoform, or the absence of a particular glycoform, a need exists for an in vitro procedure to enzymatically modify glycosylation patterns, particularly on substrates such as ceramide, sphingosine and their analogues. The present invention fulfills these and other needs. |
<SOH> SUMMARY OF THE INVENTION <EOH>It has now been discovered that gangliosides and ganglioside analogues are readily synthesized in excellent yields, in high purity and with exquisite stereochemical specificity using an enzymatic synthesis protocol. Thus, in response to the need for improved methods of preparing glycosylated species, the present invention provides methods for the enzyme-mediated formation of conjugates between glycosyl groups and selected substrates. In a first aspect the present invention provides a method of glycosylating a species according to Formula I: in-line-formulae description="In-line Formulae" end="lead"? (saccharide) q -X (I). in-line-formulae description="In-line Formulae" end="tail"? The method includes contacting (saccharide) s -X with a trans-sialidase or glycosyltransferase in presence of appropriate donor to yield (saccharide) s+1 -X. The product of the first reaction is optionally contacted with a trans-sialidase or glycosyltransferase in presence of appropriate donor to yield (saccharide) s+2 -X. The product of the second reaction is optionally contacted with a trans-sialidase or glycosyltransferase in presence of appropriate donor to yield (saccharide) s+3 -X. The process continues until the desired saccharide structure is built up. In the structures provided above, s is an integer from 0 to about 30. The symbol q represents an integer from 2 to about 30. It is generally preferred that the process of the invention include at least one sialylation that is mediated by a trans-sialidase, and two glycosylations that are mediated by the action of one or more glycosyltransferases. The method also preferably is practiced in the absence of a cellular component to the reaction mixture, and is preferably performed entirely in vitro. In another aspect, the invention provides methods for glycosylating ceramide, sphingosine and their analogues. In yet a further aspect, the invention provides ceramide and sphingosine derivatives in which the alkyl chain of the sphingosine backbone includes two or more degrees of unsaturation. Also provides are pharmaceutical compositions that include the ceramide and sphingosine derivatives of the invention. Additional objects and advantages of the present invention will be apparent from the detailed description that follows. |
Attenuation coefficient switching type hydraulic damper |
There is disclosed a damping coefficient switching-type hydraulic damper that may automatically switch a damping coefficient without needing supply of energy from the outside at all, and also may always surely exert an energy absorption capacity greater than that of a typical hydraulic damper. While a piston (3) is moving in a direction A, a mechanical drive means (30) composed of a straight gear (31) and a crank mechanism (31) allows an on-off control operation valve (11), that is, a flow regulating valve (10) to be placed in a closed state, and a damping coefficient is switched to a maximum value Cmax. When a movement of the piston (3) is turned in a direction B at a left-side maximum point of amplitude, the mechanical drive means (30) works to once open the flow regulating valve (10) to perform elimination of a load, so that the damping coefficient is switched to a minimum value (Cmin). When the piston (3) further moves in the direction B, the mechanical drive means (30) works to close the flow regulating valve (10) again, and the damping coefficient is returned to the maximum value (Cmax). Similar working to the above is also applied to a right-side maximum point of amplitude, and seismic response control is attained with repetition of the above operations. |
1. In a hydraulic damper having a cylinder, a piston movable in a reciprocating manner within said cylinder, hydraulic chambers provided at the opposite sides of said piston, and an on-off control valve provided in a passage for connecting both the hydraulic chambers and being on-off controlled to change a damping coefficient, a damping coefficient switching-type hydraulic damper, characterized by being structured so that a first damping coefficient is attained with the on-off control valve maintaining a closed state for a movement of the piston in one direction, and a second damping coefficient is attained with the on-off control valve once opened at the time when the movement of the piston is turned in the opposite direction, and afterwards, is switched to the first damping coefficient with the on-off control valve closed again. 2. In a hydraulic damper having a cylinder, a piston movable in a reciprocating manner within said cylinder, hydraulic chambers provided at the opposite sides of said piston, and an on-off control valve provided in a passage for connecting both the hydraulic chambers and being on-off controlled to change a damping coefficient, a damping coefficient switching-type hydraulic damper, characterized by providing a mechanical drive means between a piston rod and the on-off control valve, said mechanical drive means being structured so that a first damping coefficient is attained with the on-off control valve maintaining a closed state for a movement of the piston in one direction, and a second damping coefficient is attained with the on-off control valve once opened at the time when the movement of the piston is turned in the opposite direction, and afterwards, is switched to the first damping coefficient with the on-off control valve closed again. 3. The damping coefficient switching-type hydraulic damper according to claim 2, wherein said mechanical drive means for driving the on-off control valve is composed of a straight gear provided at the piston rod of the cylinder and a crank mechanism that works with the straight gear to on-off control the on-off control valve. 4. The damping coefficient switching-type hydraulic damper according to claim 2 or 3, wherein said hydraulic damper is structured so that pressures in the hydraulic chambers at the opposite sides of the piston are controlled using the single on-off control valve. 5. The damping coefficient switching-type hydraulic damper according to claim 2 or 3, wherein said hydraulic damper is structured so that pressures in the hydraulic chambers at the opposite sides of the piston are controlled using independent on-off control valves respectively. 6. In a hydraulic damper having a cylinder, a piston movable in a reciprocating manner within said cylinder, hydraulic chambers provided at the opposite sides of the piston, and an on-off control valve provided in a passage for connecting both the hydraulic chambers and being on-off controlled to change a damping coefficient, a damping coefficient switching-type hydraulic damper, characterized by providing a hydraulic drive means in a hydraulic circuit of the cylinder, said hydraulic drive means being structured so that a first damping coefficient is attained with the on-off control valve maintaining a closed state at the time when a movement of the piston in one direction causes hydraulic pressure in one hydraulic chamber to increase, and a second damping coefficient is attained with the on-off control valve once opened at the time when the movement of the piston is turned in the opposite direction to cause said hydraulic pressure to decrease, and afterwards, is switched to the first damping coefficient with the on-off control valve closed again in response to increasing hydraulic pressure in the other hydraulic chamber. 7. The damping coefficient switching-type hydraulic damper according to claim 6, wherein said hydraulic drive means for driving the on-off control valve is composed of a buffer communicating with the hydraulic chamber of the cylinder and being used to store pressure, and a selector valve that works in response to a difference in pressure between the buffer and the hydraulic chamber of the cylinder. 8. The damping coefficient switching-type hydraulic damper according to claim 6, further comprising a relief valve for limiting pressures in the hydraulic chambers at the opposite sides of the piston respectively, wherein the on-off control valve maintains the closed state in such a manner as not to allow the hydraulic drive means for driving the on-off control valve to work with pressure equal to or higher than pressure for said relief valve to start working. 9. The damping coefficient switching-type hydraulic damper according to claim 7, further comprising a relief valve for limiting pressures in the hydraulic chambers at the opposite sides of the piston respectively, wherein the on-off control valve maintains the closed state in such a manner as not to allow the hydraulic drive means for driving the on-off control valve to work with pressure equal to or higher than pressure for said relief valve to start working. 10. The damping coefficient switching-type hydraulic damper according to claim 7, further comprising a relief valve for limiting pressures in the hydraulic chambers at the opposite sides of the piston respectively, and a relief valve for limiting pressure in the buffer to pressure equal to or lower than pressure for said relief valve to start working so that the on-off control valve maintains the closed state in such a manner as not to allow the hydraulic drive means for driving the on-off control valve to work with pressure equal to or higher than the pressure for said relief valve to start working. 11. The damping coefficient switching-type hydraulic damper according to claim 6, 7, 8, 9 or 10, wherein two sets of hydraulic drive means are respectively provided for the hydraulic chambers at the opposite sides of the piston, and the single on-off control valve provided in common to the hydraulic chambers at the opposite sides of the piston is driven using said two sets of hydraulic drive means. 12. The damping coefficient switching-type hydraulic damper according to claim 6, 7, 8, 9 or 10, wherein two sets of on-off control valves and hydraulic drive means are respectively provided for the hydraulic chambers at the opposite sides of the piston. 13. The damping coefficient switching-type hydraulic damper according to claim 6, 7, 8, 9 or 10, wherein a set of on-off control valve and hydraulic drive means are provided in common to the hydraulic chambers at the opposite sides of the piston. |
<SOH> BACKGROUND ART <EOH>As one of damper-type seismic response control devices useful in reducing shaking of a structure, there is a variable damping device (as disclosed in Japanese Patent Laid-open No. 11-336366, for instance) or the like structured so that a valve opening of an on-off control valve is controllable in two stages so as to be switched between a full open position and a full closed position. The above hydraulic damper has a basic structure as shown in FIG. 11 , and, specifically, includes a cylinder 2 , a double rod-type piston 3 movable in a reciprocating manner within the cylinder 2 , hydraulic chambers 4 , 4 provided at the opposite sides of the piston 3 , an on-off control valve 6 provided in a passage 5 for connecting both the hydraulic chambers, and other components. This hydraulic damper causes the on-off control valve (electromagnetic valve) 6 to be on-off controlled in two stages so as to be switched between the full open position and the full closed position with supply of control current from a controller 7 , and thereby allows a damping coefficient of a hydraulic damper 1 to be switched in two stages, that is, between a maximum value Cmax and a minimum value Cmin. Thus-structured hydraulic damper 1 is mounted between stories of a structure through a structural component such as a brace as shown in FIG. 12 . Thus, mechanical characteristics of a device part including the brace are represented as Maxwell-type model configured so that a spring and a dashpot are joined in series as shown in FIG. 13 . The device of FIG. 11 performs large energy absorption as shown in FIG. 14 by switching the damping coefficient of the device, that is, the valve opening of the on-off control valve 6 at a maximum point of amplitude of vibrations, and attains a reduction of vibrations of the structure. In FIG. 14 , a load L of the hydraulic damper is scaled at a vertical axis, and a story deformation (deformation between Maxwell-type model ends) 6 is scaled at a horizontal axis. In addition, a portion plotted by a broken line represents a result of energy absorption using a conventional damper D 0 whose damping coefficient is constant, while a portion plotted by a solid line represents a result of energy absorption using a damping coefficient switching-type damper D 1 . Further, control of the valve opening C will do only in two stages so as to be switched between extreme positions such as the full closed position and the full open position. Thus, the device of FIG. 11 may have a more simplified structure as compared with a device (as disclosed in Japanese Patent Publication No. 7-45781, for instance) structured so that the valve opening is variably-controllable in a continuous manner. However, the conventional device as described above requires an uninterruptible power supply unit and a special-purpose power supply wiring, because of indispensable use of electric components such as a sensor, a controller and an electromagnetic valve. In addition, the above electric components include those needing to be exchanged regularly, so that the above conventional device brings about a need for a cost involving a maintenance cost. The present invention is conceived in order to solve the above problems, and an object thereof is to provide a variable damping-type hydraulic damper, more specifically, a damping coefficient switching-type hydraulic damper, which may automatically switch a damping coefficient without needing supply of energy from the outside at all, and also may always surely exert an energy absorption capacity greater than that of a typical hydraulic damper. |
<SOH> BRIEF DESCRIPTION OF THE DRAWINGS <EOH>FIG. 1 is a hydraulic circuit diagram of a first embodiment that performs switching of a damping coefficient of a damping coefficient switching-type hydraulic damper according to the present invention in a mechanical manner; FIG. 2 is a side view showing a drive mechanism of a valve of the first embodiment; FIG. 3 is a hydraulic circuit diagram of a second embodiment that performs switching of a damping coefficient of a damping coefficient switching-type hydraulic damper according to the present invention in a mechanical manner; FIG. 4 is a side view showing a drive mechanism of a valve of the first embodiment; FIG. 5 is a hydraulic circuit diagram of a third embodiment that performs switching of a damping coefficient of a damping coefficient switching-type hydraulic damper according to the present invention in a hydraulic manner; FIG. 6 is a hydraulic circuit diagram of a fourth embodiment that performs switching of a damping coefficient of a damping coefficient switching-type hydraulic damper according to the present invention in a hydraulic manner; FIG. 7 is a hydraulic circuit diagram of a fifth embodiment that performs switching of a damping coefficient of a damping coefficient switching-type hydraulic damper according to the present invention in a hydraulic manner; FIG. 8 is a hydraulic circuit diagram showing an embodiment, in which a relief valve is provided for the third embodiment of FIG. 5 ; FIG. 9 is a hydraulic circuit diagram showing an embodiment, in which a relief valve is provided for the fourth embodiment of FIG. 6 ; FIG. 10 is a hydraulic circuit diagram showing an embodiment, in which a relief valve is provided for the fifth embodiment of FIG. 7 ; FIG. 11 is a schematic view showing a basic structure of a damping coefficient switching-type hydraulic damper; FIG. 12 is a front view showing an exemplified installation of a hydraulic damper for seismic response control; FIG. 13 is a dynamic model diagram showing a hydraulic damper for seismic response control; FIG. 14 is a graph showing a load-to-deformation relation of a hydraulic damper for seismic response control; and FIG. 15 is a graph showing a load-to-deformation relation of a hydraulic damper for seismic response control when the hydraulic damper has a relief valve. detailed-description description="Detailed Description" end="lead"? |
Iron ore briquetting |
A method of producing an iron ore briquette that is suitable for use as a blastfurnace or other direct reduction furnace feedstock which includes the steps of: (1) mixing ore and a flux to form an ore/flux mixture (2) pressing the ore/flux mixture into a green briquette using a low roll pressure; and (3) indurating the green briquette to form a fired briquette. |
1. A method of producing an iron ore briquette that is suitable for use as a blast furnace or other direct reduction furnace feedstock which includes the steps of: (a) mixing ore and a flux to form an ore/flux mixture; (b) pressing the ore/flux mixture into a green briquette using a low roll pressure; and (c) indurating the green briquette to form a fired briquette. 2. The method defined in claim 1 wherein the low roll pressure is generated by a roll pressure force that is sufficient to produce briquettes having a green compressive strength of at least 2 kgf. 3. The method defined in claim 2 wherein the green compressive strength is at least 4 kgf. 4. The method defined in claim 2 wherein the green compressive strength is at least 5 kgf. 5. The method defined in claim 2 wherein the green compressive strength is 5-30 kgf. 6. The method defined in claim 2 wherein the green compressive strength is 15-30 kgf. 7. The method defined in claim 1 wherein the low roll pressure is generated by a roll pressing force of 10-140 kN/cm on the mixture of ore/flux. 8. The method defined in claim 7 wherein the roll pressing force is 10-60 kN/cm. 9. The method defined in claim 7 wherein the roll pressing force is 10-40 kN/cm. 10. The method defined in claim 1 wherein step (a) includes mixing ore having a predetermined particle size distribution of ore particles and flux particles. 11. The method defined in claim 10 wherein the predetermined particle size distribution of ore particles that is mixed with flux in step (a) can be produced without grinding ore. 12. The method defined in claim 10 includes crushing and screening ore to form the predetermined particle size distribution that is mixed with flux in step (a). 13. The method defined in claim 10 wherein the top size of the predetermined particle size distribution of ore that is mixed with flux in step (a) is 4.0 mm or less. 14. The method defined in claim 13 wherein the top size is 3.5 mm or less. 15. The method defined in claim 13 wherein the top size is 3.0 mm or less. 16. The method defined in claim 13 wherein the top size is 2.5 mm or less. 17. The method defined in claim 13 wherein the top size is 1.5 mm or less. 18. The method defined in claim 10 wherein the predetermined particle size distribution of ore that is mixed with flux in step (a) includes less than 50% passing a 45 μm screen. 19. The method defined in claim 18 wherein the particle size distribution includes less than 30% passing the 45 μm screen. 20. The method defined in claim 18 wherein the particle size distribution includes less than 10% passing the 45 μm screen. 21. The method defined in claim 1 wherein the ore is a hydrated iron ore. 22. The method defined in claim 21 wherein the hydrated ore is a goethite-containing ore. 23. The method defined in claim 1 wherein the flux has a particle size distribution that is predominantly less than 100 μm. 24. The method defined in claim 23 wherein the particle size distribution of the flux includes more than 95% passing a 250 μm screen. 25. The method defined in claim 1 wherein the ore/flux mixture produced in step (a) is selected so that the basicity of the fired briquette is greater than 0.2. 26. The method defined in claim 25 wherein preferably the basicity is greater than 0.6. 27. The method defined in claim 1 wherein there is no binder in the ore/flux mixture. 28. The method defined in claim 1 wherein the method includes adjusting the water content of the ore prior to or during mixing step (a) to optimise briquette quality and product yield. 29. The method defined in claim 28 wherein the step of adjusting the water content of the ore includes adjusting the water content so that the moisture content of the ore/flux mixture is 2-12% by weight of the total weight of the ore/flux mixture. 30. The method defined in claim 28 wherein the step of adjusting the water content of the ore includes adjusting the water content so that the moisture content of the ore/flux mixture is 2-5% by weight of the total weight of the ore/flux mixture for ores that are dense hematite ores. 31. The method defined in claim 28 wherein the step of adjusting the water content of the ore includes adjusting the water content so that the moisture content of the ore/flux mixture is 4-8% by weight of the total weight of the ore/flux mixture for ores containing up to 50% geothite. 32. The method defined in claim 28 wherein the step of adjusting the water content of the ore includes adjusting the water content so that the moisture content of the ore/flux mixture is 6-12% by weight of the total weight of the ore/flux mixture for ores that are predominantly, ie contain more than 50%, goethite ores. 33. The method defined in claim 1 wherein pressing step (c) produces briquettes that are 10 cc or less in volume. 34. The method defined in claim 33 wherein pressing step (c) produces briquettes that are 8.5 cc or less in volume. 35. The method defined in claim 33 wherein pressing step (b) produces briquettes that are 6.5 cc or less in volume. 36. The method defined in claim 1 wherein indurating step (c) includes heating the briquette to a firing temperature with 40 minutes. 37. The method defined in claim 36 wherein indurating step (d) includes heating the briquette to a firing temperature within 35 minutes. 38. The method defined in claim 36 wherein indurating step (d) includes heating the briquette to the firing temperature within 30 minutes. 39. The method defined in claim 36 wherein step (c) includes heating the briquette to the firing temperature within 20 minutes. 40. The method defined in claim 36 wherein step (c) includes heating the briquette to the firing temperature within 15 minutes. 41. The method defined in claim 36 wherein the firing temperature is at least 1200° C. 42. The method defined in claim 41 wherein the firing temperature is at least 1260° C. 43. The method defined in claim 41 wherein the firing temperature is at least 1320° C. 44. The method defined in claim 41 wherein the firing temperature is at least 1350° C. 45. The method defined in claim 41 wherein the firing temperature is at least 1380° C. 46. The method defined in claim 1 wherein the fired briquette has a crush strength of at least 200 kgf. 47. The method defined in claim 46 wherein the fired briquette has a crush strength of at least 250 kgf. |
Fenestration unit with screen coil apparatus |
A fenestration unit including screen coil apparatus is provided by the invention. The fenestration unit includes a frame defining an opening. A sash—is slideably received by the opening of the frame. The fenestration unit includes a screen coil assembly attached to the sash. The screen coil assembly includes a screen having first and second edges, and a roll core, wherein the screen is capable of being coiled and uncoiled on the roll core. The fenestration unit further includes an edge support having first and second support members having at least a portion located between the frame and the sash, the first and second support members for fastening to the screen first and second edges. |
1. A fenestration unit including a screen coil apparatus comprising: (a) a frame defining an opening, wherein the frame includes a first member; (b) a sash slidably received by in the opening, wherein the sash is movable in an opening direction away from the first member and in a closing direction toward the first member; (c) a screen coil assembly comprising: (i) a screen coil assembly capable of being coiled onto a roll core the screen having an end and first and second edges wherein the end is attached to the first member; (ii) the roll core attached to the sash for slidable movement therewith; (d) an edge support comprising a first support member and a second support member having at least a portion located between the frame and sash, wherein the first and second support members are arranged longitudinally parallel to each other and parallel to the sliding motion of the sash, wherein the first edge of the screen is removably secured to the first support member and the second edge of the screen is removably secured to the second support member and wherein when the end of the screen is attached to the first member of the frame and the sash is moved in the opening direction, the screen at least partially uncoils from the roll core. 2. The fenestration unit of claim 1 wherein the edge support comprises a track and a fastener, wherein the first support member comprises a first track member and a first fastener attached to the first track member, and wherein the second support member comprises a second track member and a second fastener attached to the second lock. 3. The fenestration of claim 1 wherein the sash slides in a vertical direction. 4. The fenestration unit of claim 3 wherein the first member is a horizontal sill member and the opening direction is upward against gravity. 5. The fenestration unit of claim 2 wherein the first and second fasteners are reclosable fasteners. 6. The fenestration unit of claim 2 wherein the first and second fasteners are reclosable fasteners. 7. The fenestration unit of claim 6 wherein the first and second fasteners are mushroom fasteners. 8. The fenestration unit of claim 1 further comprising a fastening assist member for pressing the screen and the edge support together. 9. The fenestration unit of claim 7 wherein the fastening assist member is a feed wheel connected to the sash. 10. The fenestration unit of claim 2 wherein the track further comprises a header located perpendicular to, and connecting, the first and second track members. 11. The fenestration unit of claim 10 wherein the header, first track member and second track member comprise an integral member. 12. The fenestration unit of claim 10 wherein the header of the track is removably attachable to the first member of the frame wherein the header may be unfastened from the first member and slid toward the sash when the sash is at least partially opened for egress through the fenestration unit. 13. The fenestration unit of claim 1 wherein the sash includes a bottom rail defining an opening and the roll core is received by the opening. 14. The fenestration unit claim 1 wherein the roll core is spring-loaded. 15. The fenestration unit of claim 14 wherein the roll core is a double sprung roll core. 16. A fenestration unit including a screen coil apparatus comprising: (a) a frame defining an opening, wherein the frame includes a first member; (b) a sash slidably received in the opening, wherein the sash is movable in an opening direction away from the first member and in a closing direction toward the first member; (c) a screen coil assembly comprising: (i) a screen capable of being coiled onto roll core means, the first screen having an end and first and second edges wherein the end is attached to the first member; (ii) the roll core means supporting the screen in a coiled configuration; (d) edge support means including a structure to attach the first and second edges as the sash is moved in the opening direction. 17. A hung window including a screen coil apparatus comprising: (a) a frame defining an opening, wherein the frame includes a horizontal member; (b) a sash slidably received in the opening, wherein the sash is movable in an opening direction away from the horizontal member and in a closing direction toward the horizontal member, and wherein the sash includes a horizontal rail defining a horizontal rail opening; (c) a screen coil assembly comprising: (i) a screen capable of being coiled onto a roll core, the screen having a horizontal end and first and second vertical edges; (ii) the roll core received in the horizontal rail opening in the and attached to the sash for slidable movement therewith; (d) a track comprising first and second vertical track members connected by a horizontal header, wherein the end of the screen attached to the header and the header is removably attachable to the horizontal member of the frame, and wherein the first and second track member are slidably received between the frame and sash; (e) a first fastener is attached to the first track member and a second fastener attached to the second track member, wherein when the header is attached to the horizontal member, movement of the sash in the opening direction at least partially uncoils the screen from the roll core and causes the first edge of the screen to be removably secured to the first fastener and the second edge of the screen to be removably secured to the second fastener. 18. The fenestration unit claim 17 wherein the first and second fasteners are reclosable fasteners. 19. The fenestration unit claim 18 wherein the reclosable fasteners are mushroom fasteners. 20. The fenestration unit of claim 17 comprising a fastening assist member for pressing the screen and the fastener together. 21. The fenestration unit of claim 20 wherein the fastening assist member is a feed wheel connected to the sash. 22. The fenestration unit claim 17 wherein the roll core is spring-loaded. 23. The fenestration unit including screen coil apparatus of claim 17 wherein the horizontal member of the frame is a horizontal sill member and the opening direction of the sash is upward against gravity. 24. The fenestration unit of claim 17 wherein the horizontal member of the frame is a horizontal upper member and the opening direction of the sash is downward with gravity. |
<SOH> BACKGROUND OF THE INVENTION <EOH>Traditional window units utilize a screen permanently attached to a screen frame. The result is that the screen is always obstructing the view through the window even when the window is closed and the screen is not needed. In the traditional window screen, the screen and screen frame must be removed from the window and placed in storage to eliminate this obstruction to the view. U.S. Pat. No. 5,915,443 discloses a window screen that can be concealed in the bottom lateral member of the sash of a hung window and unwound as the sash is raised thus providing an automatic window screen. |
<SOH> SUMMARY OF THE INVENTION <EOH>A fenestration unit including screen coil apparatus is provided by the invention. The fenestration unit includes a frame defining an opening. A sash—is slideably received by the opening of the frame. The fenestration unit includes a screen coil assembly attached to the sash. The screen coil assembly includes a screen having first and second edges, and a roll core, wherein the screen is capable of being coiled and uncoiled on the roll core. The fenestration unit further includes an edge support having first and second support members having at least a portion located between the frame and the sash, the first and second support members for fastening to the screen first and second edges. |
Surface treatment system and method |
A surface treatment system is disclosed to form a deposition layer at a surface of an object of surface treatment by using a deposition reaction in which an electrode (110) for applying power to form a deposition reaction in the deposition chamber (100) is installed between an inner wall (120) of the deposition chamber (100) and an object of surface treatment (900) and further includes a cooling unit (200) installed at the inner wall (120) of the deposition chamber (100) facing the electrode (110) and cooling ambient thereof. |
1. A surface treatment system for forming a deposition layer at a surface of an object of surface treatment by using a deposition reaction in which electrode unit for applying power to form a deposition reaction in the deposition chamber is installed between an inner wall of the deposition chamber and an object of surface treatment, further comprising: a cooling unit installed at the inner wall of the deposition chamber facing the electrode and cooling ambient thereof. 2. The system of claim 1, wherein the cooling unit has a water-cooling structure. 3. The system of claim i, wherein the cooling unit comprises: a cooling plate unit installed at an inner wall of the deposition chamber; and a heat-releasing unit connected to the cooling plate unit and releasing heat generated in the deposition chamber. 4. The system of claim 3, wherein the cooling plate unit is installed integrally at the inner wall of the deposition chamber facing the electrode. 5. The system of claim 3, wherein a gas injection unit for injecting gas for deposition reaction is installed together with the cooling plate unit in the deposition chamber. 6. The system of claim 3, wherein the cooling plate unit comprises: a refrigerant passage formed for letting refrigerant to flow therein; and a refrigerant inlet through which the refrigerant is introduced into the refrigerant passage and a refrigerant outlet through which the refrigerant is discharged from the refrigerant passage, the refrigerant inlet and the refrigerant outlet being connected to the heat-releasing unit. 7. The system of claim 6, wherein the cooling plate unit includes a plurality of slots for receiving the gas injection unit, and the refrigerant passage is formed around the slots. 8. A surface treatment system in which gas for deposition reaction is injected into a deposition chamber and power is applied to form a deposition reaction to form a deposition layer at a surface of an object of surface treatment, comprising: a gas injection unit installed at both sides of the deposition chamber, through which gas for the deposition reaction is injected into a deposition space; a gas discharge unit disposed at the center of the deposition chamber to divide the deposition space into two areas and discharging the deposition reaction-finished gas outwardly of the deposition chamber; a plurality of electrodes installed with a deposition space therebetween and applying power to the deposition chamber; and a cooling unit installed at both sides of the deposition chamber and cooling the ambient. 9. The system of claim 8, wherein the cooling unit comprises: a cooling plate unit installed at an inner wall of the deposition chamber; and a heat-releasing unit connected to the cooling plate unit and releasing heat generated in the deposition chamber. 10. The system of claim 9, wherein the cooling plate unit is installed integrally at the inner wall of the deposition chamber. 11. The system of claim 9, wherein the gas injection unit is installed together with the cooling plate unit. 12. The system of claim 9, wherein the cooling plate unit comprises: a refrigerant passage formed for letting refrigerant to flow therein; and a refrigerant inlet through which the refrigerant is introduced into the refrigerant passage and a refrigerant outlet through which the refrigerant is discharged from the refrigerant passage, the refrigerant inlet and the refrigerant outlet being connected to the heat releasing unit. 13. The system of claim 12, wherein the cooling plate unit includes a plurality of slots for receiving the gas injection unit, and the refrigerant passage is formed around the slots. 14. The system of claim 8, wherein the cooling unit has a water-cooling structure. |
<SOH> BACKGROUND ART <EOH>In general, a surface treatment is to make a surface of a product made of a material such as a metal look good, or to improve a surface to have heat resistance, corrosion resistance, abrasion resistance, etc. so that a function of the product can be improved according to a condition of usage of the product. That is, the surface treatment is concealing inner defects, etc. by properly treating a surface of the metal. The surface treatment includes plating on a surface of accessory, chromium plating on brass, or a tinplating for iron sheet, etc. The surface treatment methods include alumite for protecting an inside of an object of surface treatment by making oxide layer, an anticorrosive coating by paint, a chemical vapor deposition (CVD) reaction, or a physical vapor deposition (PVD) reaction. In the meantime, a heat exchanger used in an air conditioner, a refrigerator, a heating apparatus, etc. is a device for transferring heat from fluid of high temperature to fluid of low temperature through a heat transfer wall. At this time, a flow of the fluid becomes different according to a characteristic of a surface of the heat transfer wall, and the characteristic of the surface of the heat transfer wall greatly influences to a heat exchange efficiency of the heat exchanger. Accordingly, a radiator surface of the heat exchanger is required to have a surface treatment having various characteristics according to a performance of the heat exchanger. To this end, fins of the heat exchanger are fabricated by processing a sheet having a treated surface to improve hydrophilicity, hydrophobicity, or corrosion resistance. Also, the sheet for processing the fins of the exchanger has a surface treatment that forms a deposition layer at the surface of the sheet by using the chemical vapor deposition reaction or the physical vapor deposition reaction. In the meantime, for the surface treatment, reaction gas is injected in a deposition chamber and then power is applied thereto for a deposition reaction. A method for applying power includes a method for applying power to the object of surface treatment for the deposition reaction. In the conventional surface treatment method represented in PCT Publication No. WO9927157, power is directly applied to an object of surface treatment in a polymerization chamber injected by reaction gas to cause a plasma polymerization reaction, thereby forming a deposition layer at a surface of the object of surface treatment. The deposition layer formed at the surface of the surface-processed product differs depending on chemical compositions, but the deposition layer forming process also has a great influence on the quality of the deposition layer formed at the surface of the product. The quality differs depending on a composition of gas for the deposition reaction, configuration of the deposition chamber or the like. Consequently, a surface treatment system is needed to form a satisfactory deposition layer at the surface of an object of surface treatment. In addition, a surface treatment system is needed to effectively process the surface of a product in line with the mass surface processing. |
<SOH> BRIEF DESCRIPTION OF THE DRAWINGS <EOH>FIG. 1 is a conceptual view showing a surface treatment system in accordance with the first embodiment of the present invention; FIG. 2 is a plan view showing a cooling plate unit of the surface treatment system in FIG. 1 ; FIG. 3 is a conceptual view showing a surface treatment system in accordance with the second embodiment of the present invention; and FIG. 4 is a plan view showing a cooling plate unit of the surface treatment system in accordance with the second embodiment of the present invention. detailed-description description="Detailed Description" end="lead"? |
Wiper arm |
The invention starts with a wiper arm (10), which includes a fastening part (14) and an articulated part (16) with a wiper rod (18), of which at least one part (14, 16, 18) is fabricated of sheet metal by stamping and bending and features at least one area with several sheet metal layers (26, 28). It is proposed that an external sheet metal plate (26) and an internal sheet metal plate (28) lying on top of one another are jointly bent around a bending edge (52), whereby the external sheet metal plate (26) features connecting toes (32) on its side edges (54) that run longitudinally to the bending edge (52), which engage in matching recesses (30) on the corresponding side edges (56) of the internal sheet metal plate (28), and, after bending under an initial tension, the internal sheet metal plate (28) is adjacent to the external sheet metal plate (26). |
1. Wiper arm (10), which includes a fastening part (14) and an articulated part (16) with a wiper rod (18), of which at least one part (14, 16, 18) is fabricated of sheet metal by stamping and bending, and features at least one area with several sheet metal layers (26, 28), characterized in that an external sheet metal plate (26) and an internal sheet metal plate (28) lying on top of one another are jointly bent around a bending edge (52), whereby the external sheet metal plate (26) features connecting toes (32) on its side edges (54) that run longitudinally to the bending edge (52), which engage in matching recesses (30) on the corresponding side edges (56) of the internal sheet metal plate (28), and, after bending under an initial tension, the internal sheet metal plate (28) is adjacent to the external sheet metal plate (26). 2. Wiper arm (10) according to claim 1, characterized in that the sheet metal plates (26, 28) are composed of different materials. 3. Wiper arm (10) according to claim 1, characterized in that the external sheet metal plate (26) and the internal sheet metal plate (28) are formed from a sheet metal strip (36) and placed on top of one another via folding by 180°, whereby the fold (42) runs transverse to the bending edge (52). 4. Wiper arm (10) according to claim 1, characterized in that the internal sheet metal plate (28) is a partial reinforcing sheet metal plate (44). 5. Wiper arm (10) according to claim 1, characterized in that a first sheet metal part (46) is connected to a second sheet metal part (48) by overlapping the two sheet metal parts (46, 48) in a connection area (50) and one of the sheet metal parts (46, 48) is fashioned as an external sheet metal plate (26) and one as an internal sheet metal plate (28). 6. Wiper arm (10) according to claim 5, characterized in that the second sheet metal part (48) fashioned as the internal part (26) features a step (58) towards the connection area (50), whose height corresponds to the sheet metal thickness of the first sheet metal part (46). 7. Process to manufacture a wiper arm according to claim 1, characterized in that the contours of the external sheet metal plate (26) and the internal sheet metal plate (28) are stamped out of sheet metal in a first procedural step, that the connecting toes (32) are bent in a second procedural step, that the external sheet metal plate (26) is placed on the internal sheet metal plate (28) in a third procedural step so that the connecting toes (32) are aligned with the recesses (30), and that the external sheet metal plate (26) and the internal sheet metal plate (28) are jointly bent around a bending edge (52) in a fourth procedural step. 8. Process according to claim 7, characterized in that the external sheet metal plate (26) and the internal sheet metal plate (28) are stamped out of a sheet metal strip (36) arranged one after the other in the direction of the bending edge (52) and folded together in such a way that they are lying on top of one another and the connecting toes (32) are aligned with the recesses (30). |
Electric hoist |
The present invention is to provide an electric hoist using a suspended electric winch that maintains a horizontal posture in any cargo handling operation. A hoist in one aspect includes a winch including a drum axially connected to a drive shaft of a motor, a suspension hook attached to the winch above the center of gravity of the winch that is in a horizontal posture thereof in and empty load state thereof, a first roller arranged on the opposite side of the winch from the suspension hook and turning the direction of a wire paid out from the drum toward the center of gravity, and a second roller for turning the direction of the wire to be aligned with a vertical line downward extended from the center of gravity of the winch. The winch is suspended in the simplest suspension method when the winch is used as a hoist. The suspension method is implemented in many plants and warehouses without any particular facility. The winch in the suspended posture thereof is balanced in a fore-after direction and a lateral direction, and continuously maintains a horizontal aligned posture during a load empty period and a load raising and lowering period. |
1. An electric hoist comprising an electric winch including a drum axially connected to a drive shaft of a motor, a suspension hook attached to said electric winch right above the center of gravity of said electric winch, said electric winch being in a horizontal posture in an empty load state thereof, a first roller arranged on the opposite side of said electric winch from said suspension hook and turning the direction of a wire paid out from the drum toward the center of gravity, and a second roller for turning the direction of the wire to be aligned with a vertical line downward extended from the center of gravity of said electric winch. 2. An electric hoist according to claim 1, wherein each of said first and second rollers comprises a rotary shaft and a sheave secured on said rotary shaft. 3. An electric hoist according to claim 2, wherein said sheave is secured to said rotary shaft using a screw. 4. An electric hoist according to claim 2, wherein said sheave of said first roller and said sheave of the second roller are arranged at an angle equal to the angle of inclination of the wire stretched between said two sheaves. 5. An electric hoist according to claim 4, wherein said rotary shaft is set to be at a right angle to said wire stretched between the sheaves. 6. An electric hoist according to claim 1, wherein said sheave that turns said wire to a vertically downward direction is rotatably supported around said rotary shaft thereof. 7. An electric hoist according to claim 6, wherein said two sheaves are arranged on the respective rotary shafts at an angle with respect to the respective rotary shafts so that said wire stretched between said two sheaves is aligned with said sheaves. 8. An electric hoist according to claim 1, wherein a weight is attached to one end of said wire. 9. An electric hoist according to claim 1, wherein a stopper is attached to one end of said wire. |
<SOH> BACKGROUND OF THE INVENTION <EOH>Electric winches typically have a relatively simple structure in which a drum is coupled to a drive shaft of an electric motor such as a geared motor through a reduction device. A variety of types of electric winches are commercially available in wide ranges of price and performance. A BADA product catalog issued by ZHENJIANG BADA MECHANICAL & ELECTRICAL CO., LTD. in October 2002 discloses a heavy load lifting hoist using an electric winch. FIG. 8 illustrates the disclosed structure. A horizontal extending arm 51 is connected to a vertically aligned pole 50 and an electric winch 52 is supported on the arm 51 . A clamp 54 having a socket 53 is fixed to the pole 50 . A wedge 55 is welded to one end of the arm 51 . With the wedge 55 received in the socket 53 , the arm 51 is secured to the pole 50 . The other end of the arm 51 is supported by a brace 56 . A cover frame 57 covers the electric winch 52 . Arranged on the cover frame 57 are two brackets 58 through which the arm 51 extends. The electric winch 52 is supported by the arm 51 with the arm 51 extending through the brackets 58 . The electric winch 52 is used as a hoist in this structure that a wire 60 (alternatively, a rope or a chain) wound around a drum 59 is suspended. The electric winch 52 supported by two brackets 58 is free from being inclined during lifting of a heavy cargo. In view of safety cargo handling operation, an uninclined electric winch 52 is important to maintain an appropriate positional relationship between the wire 60 and the drum 59 and to prevent the wire 60 from being wound on the drum 59 on a one-sided manner and from being unwound unintentionally from the drum 59 . The pole 50 in the conventional art must be erected if the electric winch 52 is used in a cargo handling operation within a plant building or warehouse. Since the pole 50 is not permanently installed, the area that permits the pole 50 to be erected is limited. It is not practical to newly erect the pole 50 within a plant building or a warehouse. If the arm 51 is secured to the ceiling of a building, the pole 50 is dispensed with. Even in this case, the area that permits the arm 51 to be installed is also limited. A simplest fixing method of the electric winch 52 is to suspend it. More specifically, the electric winch 52 is easily suspended as an electric hoist if a suspension tool such as a wire is available in a cargo handling place. FIG. 9 illustrates such an example. A hook 61 is arranged on the electric winch 52 . The hook 61 is secured to the electric winch 52 at the center of gravity thereof in an empty load condition. By hanging the hook 61 on a wire 62 that is suspended from an appropriate posture on the ceiling, the electric winch 52 remains in a horizontal posture thereof. The electric winch 52 includes the motor and drum side by side. During cargo lifting, a load acts on the drum causing the center of gravity of the entire electric winch 52 to be shifted toward the drum. The electric winch 52 is thus inclined downward at the drum 59 in response to the weight of the load. If the cargo handling operation is performed with the electric winch 52 inclined, the wire 60 may be wound in a one-sided fashion on the drum 59 . Such an operation is dangerous. Since the load is varied in weight, it is impossible to set the position of the hook 61 to the center of gravity during cargo operation. |
<SOH> SUMMARY OF THE INVENTION <EOH>Accordingly, it is an object of the present invention to provide an electric hoist as a suspended electric winch that maintains a horizontal posture in any cargo handling operation. An electric hoist of the present invention in one aspect includes an electric winch including a drum axially connected to a drive shaft of a motor, a suspension hook attached to the electric winch right above the center of gravity of the electric winch, the electric winch being in a horizontal posture thereof in and empty load state thereof, a first roller arranged on the opposite side of the electric winch from the suspension hook and turning the direction of a wire paid out from the drum toward the center of gravity, and a second roller for turning the direction of the wire to be aligned with a vertical line downward extended from the center of gravity of the electric winch. The hook for suspending the electric winch may be a ring. The hook may be directly secured to the electric winch or to the cover frame already discussed in the Description of the Related Art. The wire paid out from the drum is wrapped around the first roller along about the lower half circumference thereof and wrapped around the second roller along about the upper half of the circumference thereof. The wire thus runs to be aligned with a line vertically downward extending from the center of gravity of the electric winch (right below the position of the hook). As a result, the center of gravity of the electric winch in the suspended electric winch and the center of gravity of the load are in alignment. Regardless of whether the electric winch is in an empty load condition or a loaded condition, the hoist remains to be laterally balanced. The roller may be a round shaft having a predetermined length. The wire is thus directly wrapped around the shaft. A method for securing the roller to the electric winch is not limited to any particular means. The rotatably supported shaft allows the wire to be paid out and wound up in a smooth manner and reduces friction between the shaft and the wire. The roller may include a sheave fixed to the shaft. The wire is wrapped around the sheave. If the wire is directly wrapped around the shaft, the wire may slip along the length thereof during the cargo handling operation. The use of the sheave fixed to the shaft is preferable. The shaft may be rotatably supported (with the sheave integrally rotatable with the shaft). The advantage of this arrangement has already been discussed. The sheaves of the first roller and the second roller are shifted in the fixed positions thereof along the longitudinal direction of the shafts. By shifting the sheave of the second roller to the vertically aligned line extending from the center of gravity, the wire is suspended downward right below the center of gravity of the hoist. As a result, the hoist is balanced in a fore-aft direction and is not inclined in the fore-aft direction during an empty load period and a loaded period. This arrangement allows the electric hoist to more smoothly lift a load. If the fixing positions of the sheaves are shifted between the first roller and the second roller, the wire is stretched between the sheaves at an inclination. As a result, the wire touches and bends at the flange of the sheave other than the groove of the sheave, thereby causing excessive friction there. A cargo handling operation for a long period of time in this condition may lead to a broken wire. To avoid such a problem, the wire stretched between the sheaves must be clear of the flange of the sheaves. In accordance with the present invention, the sheaves of the first and second rollers are aligned at the same angle as the wire stretched between the sheaves. This arrangement is achieved by inclining the rotary shaft of the sheave. The wire stretched between the sheaves is correctly aligned to the groove of each sheave. One of the two sheaves of the first and second rollers for running the wire in the vertically downward direction may be rotatably supported around the rotary shaft thereof. The sheave rotates following the wire which could be moved when the load rolls and pitches. The winding position of the wire along the sheave is appropriately maintained. In this arrangement, the shaft of the sheave is inclined in a manner such that the shaft is at a right angle with respect to the wire. The wire is thus aligned with the groove of the sheave. In the same way as the cylindrical shaft is inclined, the winding position of the wire is correctly aligned. The wire is prevented from being cut or damaged due to the rubbing of the wire against the flange of the sheave. |
Electrode for use in urological resectoscopes |
An electrode (9,) for use in urological resectoscopes including an elongated electrode carrier (7, 18, 19) that is provided in its proximal region with a spring element (20, 30′, 39, 40, 45) in order to establish an electric contact (12) and to mechanically fasten a sliding body (5) in a receiving guide (6, 36) via a snap-in connection. The spring element (20, 30′, 39, 40, 45) is disposed on the electrode body (7, 18, 19). |
1. An electrode (9) for urological resectoscopes including an elongate electrode carrier (7, 18, 19), which is constructed proximately for electrical contact (12) and for mechanical fastening in a receiving guide (6, 36) in a sliding body (5) by a locking connection with a spring element (20, 20′, 39, 40, 45), wherein the spring element (20, 20′, 39, 40, 45) is arranged on the electrode body (7, 18, 19). 2. The electrode as claimed in claim 1, wherein the spring element (20, 20′, 39, 40) is constructed to move under its resilience radially outwardly. 3. The electrode as claimed in claim 2, wherein the spring element has one or more peripherally spaced spring tongues (20, 20′), whose proximal end is connected to the electrode carrier (19) and extend from there distally and obliquely outwardly. 4. The electrode as claimed in claim 3, wherein the spring tongues (20, 20′) are constructed in the form of partial cutouts in a sleeve (19, 19′) connected to the electrode carrier (18). 5. The electrode as claimed in claim 1, wherein the electrode carrier (7) has an end stop (17, 17′) limiting an insertion depth into the receiving guide (6). 6. The electrode as claimed in claim 1, wherein the electrode carrier has a peripherally thickened portion (7, 33) at a distal spacing from the spring element (20, 20′). 7. The electrode as claimed in claim 6, wherein the peripherally thickened portion is constructed in the form of a ring (33), which is slidably mounted on the electrode carrier (7) and is acted on by the proximal end of a longitudinally elastic hose (34), which is mounted on the electrode carrier (7) and whose proximal end is connected to the electrode carrier. 8. The electrode as claimed in claim 1, wherein the spring element (45) carries a radial projection (46), which is rotationally resiliently mounted with respect to the distal region (7) of the electrode carrier. 9. A resectoscope for receiving an electrode, said electrode including an elongate electrode carrier (7, 18, 19), which is constructed proximately for electrical contact (12) and for mechanical fastening in a receiving guide (6, 36) in a sliding body (5) by a locking connection with a spring element (20, 20′, 39, 40, 45), wherein the spring element (20, 20′, 39, 40, 45) is arranged on the electrode body (7, 18, 19), and wherein the receiving guide (6, 36) has, in a fastening region, an edge engaging the electrode carrier (18, 19) proximal of which an empty space is defined adjacent the electrode carrier (18). 10. The resectoscope as claimed in claim 9, wherein the edge is formed on a locking element (21, 38), which is movable out of locking engagement. 11. The resectoscope as claimed in claim 10, wherein the electrode spring element (20, 20′, 39, 40) is constructed to move under its resilience radially outwardly, and wherein the locking element is constructed in the form of a slider (21), which is mounted in the sliding body (5) and is slidable transversely to the electrode carrier (7), and has a hole (25, 25′) which is elongated in a sliding direction and provides the edge at one of its end regions. 12. The resectoscope as claimed in claim 11, wherein the width of the elongate hole (25) corresponds to a diameter of the electrode carrier (19) with the spring tongues (20) moved resiliently inwards, whereby the elongate hole (25), in the locked position of the slider, receives the electrode carrier (18) in its one end region and, at this end region, has a step (26) of increased width on its proximal edge, which tapers obliquely in the direction towards the other end region (27) of the elongate hole (25) to the width thereof. |
<SOH> BACKGROUND OF THE INVENTION <EOH>Urological resectoscopes have, within an elongate tubular shaft, an elongate, tubular optical system and an elongate electrode carrier, disposed on the distal end of which in the field of view of the optical system there is an HF electrode, generally constructed in the form of a cutting blade. The electrode carrier projects, together with the optical system, proximally beyond the shaft region of the resectoscope and is connected there to a sliding body, which is slidably mounted e.g. on the optical tube and is actuated back and forth by the operator to move the electrode longitudinally. Provided in the sliding body is a contacting device, with which a conductive wire extending longitudinally through the electrode carrier to the electrode is contacted. Also provided is a fastener with which the electrode carrier may be fastened to the sliding body. In constructions of the type referred to above, the proximal end region of the rod-shaped electrode carrier is inserted into a receiving guide on the sliding body, which is generally constructed in the form of a receiving bore. Fastening is effected by means of a locking connection with a spring element. In the prior art, the spring element is constructed, e.g. in the form of a blade mounted resiliently transversely to the electrode carrier which springs lockingly into a peripheral groove in the electrode carrier. A disadvantage is that in the event of a defect on the spring element, the sliding body must be replaced, which is extremely complex in a urological resectoscope. The object of the present invention resides in improving the possibilities for repairing a defective spring element. |
<SOH> SUMMARY OF THE INVENTION <EOH>The electrode in accordance with the invention has a spring element on the electrode carrier. A simple edge on the sliding body in the region of the fastener is sufficient, behind which the spring element can move out resiliently to lock it, when it is inserted. If defects occur on the spring element, the electrode is replaced but is in any event replaced after each operation. As a result of the constant use of new spring elements, a constantly optimal function is thus ensured. The spring element on the electrode carrier can advantageously be constructed to move radially outwardly under its resilience, e.g. with resiliently supported locking balls or the like. One or more spring tongues are provided which can be fabricated substantially more simply in a necessary small size in the region of about 1 mm. If only one spring tongue or some other spring element is provided on the electrode carrier at a predetermined peripheral angular position and if the edge is situated only on one side adjacent the electrode carrier, the precisely matching angular position of the one spring element must be ensured. If, on the other hand, a plurality of tongues or spring elements are provided distributed over the periphery, one of these always comes into engagement so that the exact angular position is not critical. This facilitates the installation of the spring tongues on the electrode carrier, e.g. by an arrangement independent of peripheral angle. The spring tongues can, for instance, be secured to a metallic end member of the electrode carrier by riveting or soldering. The spring tongues are constructed as portions of a sleeve, which slides onto the electrode carrier and is secured by clamping, which makes manufacture substantially easier. An end stop is preferably formed on the electrode carrier, which, in the opposite direction to the locking connection preventing withdrawal, ensures a secure mounting of the electrode carrier in the sliding body in both sliding directions. The peripherally thickened portion, which is provided adjacent to the outwardly projecting spring element, a sharp edged spring tongue, provides protection against injury on the sharp edge spring tongue, for instance when touching it with the finger or when moving through a seal which seals the electrode carrier. A locking element can engage in the space between the spring element and peripheral thickened portion which affords the edge towards the spring element and engages the peripheral thickened portion, constituting the end stop, with a proximally situated further edge. The longitudinally elastic hose can push the ring constituting the peripheral thickened portion into engagement with the spring element, a plurality of spring tongues, so that sharp edged spring tongues are completely shielded without injury by the engaging ring. If the electrode carrier is inserted, the spring tongues move in resiliently at the edge and the locking element carrying the edge pushes the ring before it, whilst shortening the longitudinally elastic hose, until it is locked in between the ring and spring tongues. Instead of a radially resilient spring element, a rotationally resilient spring element can advantageously be provided which carries a radial projection, which is movable rotationally resiliently into and out of engagement with a fixed projection. A portion of the electrode carrier itself can bring about the rotational resilience in a structurally very simple manner, with respect to the distal end region of the electrode carrier, which, in the conventional construction of recectoscopes, is rotationally fixedly mounted on its optical tube. The edge on the receiving guide with an empty space situated proximally thereof constitutes a distal abutment for the spring element which has moved resiliently outwards. It can be of very simple and stable construction so that long term functional security is ensured. The edge can be of oblique shape so that, when the electrode carrier is pulled strongly, the spring element is forced radially inwards and the electrode carrier can be withdrawn. The edge can be moved out of engagement with the spring element by moving the locking element. The edge can therefore be of perpendicular construction. The result of this is that with the edge in the engaged position unintentional release of the electrode carrier is precluded but with the edge moved out of engagement the electrode carrier is very easily removable. At one of its longitudinal ends, the elongate hole in the slider affords the edge, which ensures the locking engagement with the spring element. The edge can be moved out of engagement by movement of the slider. The elongate hole can, for instance, be broadened in its other end region such that it permits the electrode carrier to pass through freely with all the spring tongues, even in the state in which they have moved resiliently outwardly. When passing through the narrow elongate hole, the spring tongues move in and move resiliently out in the region of the broadened step, where they lock against reverse movement. If the slider is moved in the direction of the elongate hole, the portion of the elongate hole where no step is present moves into engagement with the spring tongues. The broadened side wall of the step narrows down to the normal width of the elongate hole so that when the elongate hole is moved the spring tongues engage the electrode carrier and the latter can then be withdrawn with the electrode carrier. The invention is schematically illustrated by way of example in the drawings |
Selective herbicides based on substituted cyclic keto-enols and safeners |
The present invention relates to selective herbicidal compositions comprising an effective amount of an active compound combination comprising (a) at least one substituted cyclic ketoenol of the formula (I) in which X, Z, W and Y and the group CKE are as defined in the disclosure, and (b) at least one compound which improves crop plant compatibility selected from the group of compounds listed in the description, particularly cloquintocet-mexyl and mefenpyr-diethyl. The invention further relates to the use of these compositions as herbicides and to a method for controlling undesirable vegetation using these compositions. |
1-11. (canceled) 12. A composition comprising an effective amount of an active compound combination comprising (a) at least one substituted cyclic ketoenol of formula (I) including any tautomeric forms thereof or a salt or an acid or base adduct of the compounds of formula (I) including any tautomeric forms thereof, in which X represents halogen, alkyl, alkenyl, alkoxy, alkenyloxy, alkylthio, alkyl-sulphinyl, alkylsulphonyl, haloalkyl, haloalkoxy, haloalkenyloxy, nitro, or cyano, Z represents hydrogen; or represents optionally substituted alkenyl, alkynyl, aryl, or hetaryl, W and Y independently of one another represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, haloalkyl, haloalkoxy, haloalkenyloxy, nitro, or cyano, with the proviso that W and X do not simultaneously represent ethyl when Y represents 4-methyl and W does not represent methoxy or difluoromethoxy when X represents ethyl, and CKE represents one of the groups in which A represents hydrogen; represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, or saturated or unsaturated optionally substituted cycloalkyl in which one or more ring atoms is optionally replaced by a heteroatom; or represents optionally halogen-, alkyl-, haloalkyl-, alkoxy-, haloalkoxy-, cyano-, or nitro-substituted aryl, arylalkyl, or hetaryl, B represents hydrogen, alkyl, or alkoxyalkyl, or A and B together with the carbon atom to which they are attached represent a saturated or unsaturated unsubstituted or substituted cycle that optionally contains one or more heteroatoms, D represents hydrogen; or represents an optionally substituted radical selected from the group consisting of alkyl, alkenyl, alkynyl, alkoxyalkyl, saturated or unsaturated cycloalkyl in which one or more ring members are optionally replaced by hetero-atoms, arylalkyl, aryl, hetarylalkyl, or hetaryl, or A and D together with the atoms to which they are attached represent a saturated or unsaturated cycle that is unsubstituted or substituted in the A, D moiety and optionally contains one or more heteroatoms, Q1 represents hydrogen or alkyl, or A and Q1 together represent alkanediyl or alkenediyl that are each optionally substituted by hydroxyl or by optionally substituted alkyl, alkoxy, alkylthio, cycloalkyl, benzyloxy, or aryl, Q2, Q4, Q5, and Q6 independently of one another represent hydrogen or alkyl, Q3 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, optionally substituted cycloalkyl in which one methylene group is optionally replaced by oxygen or sulphur, or optionally substituted phenyl, or Q3 and Q4 together with the carbon atom to which they are attached, represent a saturated or unsaturated unsubstituted or substituted cycle that optionally contains a heteroatom, and G represents hydrogen (a) or represents one of the groups in which E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur, M represents oxygen or sulphur, R1 represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, or polyalkoxyalkyl; represents optionally halogen-, alkyl-, or alkoxy-substituted cycloalkyl that is optionally interrupted by one or more heteroatoms; or represents optionally substituted phenyl, phenylalkyl, hetaryl, phenoxyalkyl, or hetaryloxyalkyl, R2 represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, or polyalkoxyalkyl; or represents optionally substituted cycloalkyl, phenyl, or benzyl, R3, R4, and R5 independently of one another represent optionally halogen-substituted alkyl, alkoxy, alkylamino, dialkylamino, alkylthio, alkenylthio, or cycloalkylthio; or represent optionally substituted phenyl, benzyl, phenoxy, or phenylthio, and R6 and R7 independently of one another represent hydrogen; represent optionally halogen-substituted alkyl, cycloalkyl, alkenyl, alkoxy, or alkoxyalkyl; represent optionally substituted phenyl; represent optionally substituted benzyl; or together with the N atom to which they are attached represent a cycle that is optionally interrupted by oxygen or sulphur, and (b) at least one compound that improves crop plant compatibility selected from the compounds 4-dichloroacetyl-1-oxa-4-aza-spiro[4.5]-decane (AD-67, MON-4660), 1-dichloroacetyl-hexahydro-3,3,8a-trimethylpyrrolo[1,2-a]-pyrimidin-6(2H)-one (dicyclonon, BAS-145138), 4-dichloroacetyl-3,4-dihydro-3-methyl-2H-1,4-benzoxazine (benoxacor), 1-methyl-hexyl 5-chloro-quinolin-8-oxy-acetate (cloquintocet-mexyl), 3-(2-chloro-benzyl)-1-(1-methyl-1-phenyl-ethyl)-urea (cumyluron), α-(cyanomethoximino)-phenylacetonitrile (cyometrinil), 2,4-dichloro-phenoxyacetic acid (2,4-D), 4-(2,4-dichloro-phenoxy)-butyric acid (2,4-DB), 1-(1-methyl-1-phenyl-ethyl)-3-(4-methyl-phenyl)-urea (daimuron, dymron), 3,6-dichloro-2-methoxy-benzoic acid (dicamba), S-1-methyl-1-phenyl-ethyl piperidine-1-thiocarboxylate (dimepiperate), 2,2-dichloro-N-(2-oxo-2-(2-propenylamino)-ethyl)-N-(2-propenyl)-acetamide (DKA-24), 2,2-dichloro-N,N-di-2-propenyl-acetamide (dichlormid), 4,6-dichloro-2-phenyl-pyrimidine (fenclorim), ethyl 1-(2,4-dichloro-phenyl)-5-trichloromethyl-1H-1,2,4-triazole-3-carboxylate (fenchlorazole-ethyl), phenyl-methyl 2-chloro-4-trifluoromethyl-thiazole-5-carboxylate (flurazole), 4-chloro-N-(1,3-dioxolan-2-yl-methoxy)-α-trifluoro-acetophenone oxime (fluxofenim), 3-dichloroacetyl-5-(2-furanyl)-2,2-dimethyl-oxazolidine (furilazole, MON-13900), ethyl 4,5-dihydro-5,5-diphenyl-3-isoxazolecarboxylate (isoxadifen-ethyl), 1-(ethoxycarbonyl)-ethyl 3,6-dichloro-2-methoxybenzoate (lactidichlor), (4-chloro-o-tolyloxy)-acetic acid (MCPA), 2-(4-chloro-o-tolyloxy)-propionic acid (mecoprop), diethyl 1-(2,4-dichloro-phenyl)-4,5-dihydro-5-methyl-1H-pyrazole-3,5-dicarboxylate (mefenpyr-diethyl), 2-dichloromethyl-2-methyl-1,3-dioxolane (MG-191), 2-propenyl-1-oxa-4-azaspiro[4.5]decane 4-carbodithioate (MG-838), 1,8-naphthalic anhydride, α-(1,3-dioxolan-2-yl-methoximino)-phenylacetonitrile (oxabetrinil), 2,2-dichloro-N-(1,3-dioxolan-2-yl-methyl)-N-(2-propenyl)-acetamide (PPG-1292), 3-dichloroacetyl-2,2-dimethyl-oxazolidine (R-28725), 3-dichloro-acetyl-2,2,5-trimethyl-oxazolidine (R-29148), 4-(4-chloro-o-tolyl)-butyric acid, 4-(4-chloro-phenoxy)-butyric acid, diphenylmethoxyacetic acid, methyl diphenylmethoxyacetate, ethyl diphenylmethoxyacetate, methyl 1-(2-chloro-phenyl)-5-phenyl-1H-pyrazole-3-carboxylate, ethyl 1-(2,4-dichloro-phenyl)-5-methyl-1H-pyrazole-3-carboxylate, ethyl 1-(2,4-dichloro-phenyl)-5-isopropyl-1H-pyrazole-3-carboxylate, ethyl 1-(2,4-dichloro-phenyl)-5-(1,1-dimethyl-ethyl)-1H-pyrazole-3-carboxylate, ethyl 1-(2,4-dichloro-phenyl)-5-phenyl-1H-pyrazole-3-carboxylate, ethyl 5-(2,4-dichloro-benzyl)-2-isoxazoline-3-carboxylate, ethyl 5-phenyl-2-isoxazoline-3-carboxylate, ethyl 5-(4-fluoro-phenyl)-5-phenyl-2-isoxazoline-3-carboxylate, 1,3-dimethyl-but-1-yl 5-chloro-quinolin-8-oxy-acetate, 4-allyloxy-butyl 5-chloro-quinolin-8-oxy-acetate, 1-allyloxy-prop-2-yl 5-chloro-quinolin-8-oxy-acetate, methyl 5-chloro-quinoxalin-8-oxy-acetate, ethyl 5-chloro-quinolin-8-oxy-acetate, allyl 5-chloro-quinoxalin-8-oxy-acetate, 2-oxo-prop-1-yl 5-chloro-quinolin-8-oxy-acetate, diethyl 5-chloro-quinolin-8-oxy-malonate, diallyl 5-chloro-quinoxalin-8-oxy-malonate, diethyl 5-chloro-quinolin-8-oxy-malonate, 4-carboxy-chroman-4-yl-acetic acid (AC-304415), 4-chloro-phenoxy-acetic acid, 3,3′-dimethyl-4-methoxy-benzophenone, 1-bromo-4-chloromethylsulphonyl-benzene, 1-[4-(N-2-methoxybenzoylsulphamoyl)-phenyl]-3-methyl-urea (alias N-(2-methoxy-benzoyl)-4-[(methylamino-carbonyl)-amino]-benzenesulphonamide), 1-[4-(N-2-methoxybenzoylsulphamoyl)-phenyl]-3,3-dimethyl-urea, 1-[4-(N-4,5-dimethylbenzoylsulphamoyl)-phenyl]-3-methyl-urea, 1-[4-(N-naphthylsulphamoyl)-phenyl]-3,3-dimethyl-urea, and N-(2-methoxy-5-methyl-benzoyl)-4-(cyclopropylaminocarbonyl)-benzenesulphonamide, and/or one or more compounds of formulas (IIa), (IIb), or (IIc) where n represents a number between 0 and 5, A1 represents one of the divalent heterocyclic groups A2 represents optionally C1-C4-alkyl- and/or C1-C4-alkoxy-carbonyl-substituted alkanediyl with 1 or 2 carbon atoms, R8 represents hydroxyl, mercapto, amino, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylamino, or di-(C1-C4-alkyl)-amino, R9 represents hydroxyl, mercapto, amino, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylamino, or di-(C1-C4-alkyl)-amino, R10 represents optionally fluorine-, chlorine-, and/or bromine-substituted C1-C4-alkyl, R11 represents hydrogen; represents optionally fluorine-, chlorine-, and/or bromine-substituted C1-C6-alkyl, C2-C6-alkenyl, or C2-C6-alkynyl, C1-C4-alkoxy-C1-C4-alkyl, dioxolanyl-C1-C4-alkyl, furyl, furyl-C1-C4-alkyl, thienyl, thiazolyl, or piperidinyl; or represents optionally fluorine-, chlorine-, and/or bromine- or C1-C4-alkyl-substituted phenyl, R12 represents hydrogen; represents optionally fluorine-, chlorine-, and/or bromine-substituted C1-C6-alkyl, C2-C6-alkenyl, or C2-C6-alkynyl, C1-C4-alkoxy-C1-C4-alkyl, dioxolanyl-C1-C4-alkyl, furyl, furyl-C1-C4-alkyl, thienyl, thiazolyl, or piperidinyl; or represents optionally fluorine-, chlorine-, and/or bromine- or C1-C4-alkyl-substituted phenyl; or together with R11 represents C3-C6-alkanediyl or C2-C5-oxaalkanediyl, each of which is optionally substituted by C1-C4-alkyl, phenyl, furyl, a fused-on benzene ring or two substituents that together with the carbon atom to which they are attached form a 5- or 6-membered carbocycle, R13 represents hydrogen, cyano, or halogen; or represents optionally fluorine-, chlorine-, and/or bromine-substituted C1-C4-alkyl, C3-C6-cycloalkyl, or phenyl, R14 represents hydrogen; or represents optionally hydroxyl-, cyano-, halogen-, or C1-C4-alkoxy-substituted C1-C6-alkyl, C3-C6-cycloalkyl, or tri-(C1-C4-alkyl)-silyl, R15 represents hydrogen, cyano, or halogen; or represents optionally fluorine-, chlorine-. and/or bromine-substituted C1-C4-alkyl, C3-C6-cycloalkyl, or phenyl, X1 represents nitro, cyano, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy, X2 represents hydrogen, cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy, and X3 represents hydrogen, cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy, and/or one or more compounds of formulas (lid) or (lie) where n represents a number between 0 and 5, R16 represents hydrogen or C1-C4-alkyl, R17 represents hydrogen or C1-C4-alkyl, R18 represents hydrogen; represents optionally cyano-, halogen-, or C1-C4-alkoxy-substituted C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylamino, or di-(C1-C4-alkyl)-amino; or represents optionally cyano-, halogen-, or C1-C4-alkyl-substituted C3-C6-cycloalkyl, C3-C6-cycloalkyloxy, C3-C6-cycloalkylthio, or C3-C6-cycloalkylamino, R19 represents hydrogen; represents optionally cyano-, hydroxyl-, halogen-, or C1-C4-alkoxy-substituted C1-C6-alkyl; represents optionally cyano- or halogen-substituted C3-C6-alkenyl or C3-C6-alkynyl; or represents optionally cyano-, halogen-, or C1-C4-alkyl-substituted C3-C6-cycloalkyl, R20 represents hydrogen; represents optionally cyano-, hydroxyl-, halogen-, or C1-C4-alkoxy-substituted C1-C6-alkyl; represents optionally cyano- or halogen-substituted C3-C6-alkenyl or C3-C6-alkynyl; represents optionally cyano-, halogen-, or C1-C4-alkyl-substituted C3-C6-cycloalkyl; or represents optionally nitro-, cyano-, halogen-, C1-C4-alkyl-, C1-C4-haloalkyl-, C1-C4-alkoxy-, C1-C4-haloalkoxy-substituted phenyl; or together with R19 represents optionally C1-C4-alkyl-substituted C2-C6-alkanediyl or C2-C5-oxaalkanediyl, X4 represents nitro, cyano, carboxyl, carbamoyl, formyl, sulphamoyl, hydroxyl, amino, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy, and X5 represents nitro, cyano, carboxyl, carbamoyl, formyl, sulphamoyl, hydroxyl, amino, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy. 13. A composition according to claim 12 where in formula (I) X represents halogen, C1-C6-alkyl, C2-C6-alkenyl, C1-C6-haloalkyl, C1-C6-alkoxy, C3-C6-alkenyloxy, C1-C6-haloalkoxy, C3-C6-haloalkenyloxy, nitro, or cyano, Z represents hydrogen, C2-C6-alkenyl, or C2-C6-alkynyl; or represents one of the radicals in which V1 represents hydrogen, halogen, C1-C12-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulphinyl, C1-C6-alkylsulphonyl, C1-C4-haloalkyl, C1-C4-haloalkoxy, nitro, or cyano, V2 and V3 independently of one another represent hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, or C1-C4-haloalkoxy, W and Y independently of one another represent hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, nitro, or cyano, with the proviso that W and X do not simultaneously represent ethyl when Y represents 4-methyl and W does not represent methoxy or difluoromethoxy when X represents ethyl, and CKE represents one of the groups in which A represents hydrogen; represents optionally halogen-substituted C1-C12-alkyl, C3-C8-alkenyl, C1-C10-alkoxy-C1-C8-alkyl, C1-C10-alkylthio-C1-C6-alkyl; represents optionally halogen-, C1-C6-alkyl-, or C1-C6-alkoxy-substituted C3-C8-cycloalkyl in which one or two ring members that are not directly adjacent are optionally replaced by oxygen and/or sulphur; or represents optionally halogen-, C1-C6-alkyl-, C1-C6-haloalkyl-, C1-C6-alkoxy-, C1-C6-haloalkoxyl, cyano-, or nitro-substituted phenyl or phenyl-C1-C6-alkyl, B represents hydrogen, C1-C12-alkyl, or C1-C8-alkoxy-C1-C6-alkyl, or A, B, and the carbon atom to which they are attached represent saturated C3-C10-cycloalkyl or unsaturated C5-C10-cycloalkyl in which one ring member is optionally replaced by oxygen or sulphur and that are optionally mono- or disubstituted by C1-C8-alkyl, C3-C10-cycloalkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-alkylthio, halogen, or phenyl; or represent C3-C6-cycloalkyl that is substituted by an alkylenediyl, alkylenedioxyl, or alkylenedithioyl group that, together with the carbon atom to which it is attached, forms a further five- to eight-membered ring and that is optionally substituted by C1-C4-alkyl that optionally contain one or two oxygen and/or sulphur atoms that are not directly adjacent; or represent C3-C8-cycloalkyl or C5-C8-cycloalkenyl in which two substituents together with the carbon atoms to which they are attached represent optionally C1-C6-alkyl-, C1-C6-alkoxy-, or halogen-substituted C2-C6-alkanediyl, C2-C6-alkenediyl, or C4-C6-alkanedienediyl in which one methylene group is optionally replaced by oxygen or sulphur, D represents hydrogen; represents optionally halogen-substituted C1-C12-alkyl, C3-C8-alkenyl, C3-C8-alkynyl, or C1-C10-alkoxy-C2-C8-alkyl; represents optionally halogen-, C1-C4-alkyl-, C1-C4-alkoxy-, or C1-C4-haloalkyl-substituted C3-C8-cycloalkyl in which one ring member is optionally replaced by oxygen or sulphur; or represents optionally halogen-, C1-C6-alkyl-, C1-C6-haloalkyl-, C1-C6-alkoxy-, C1-C6-haloalkoxy-, cyano-, or nitro-substituted phenyl or phenyl-C1-C6-alkyl, or A and D together represent optionally substituted C3-C6-alkanediyl or C3-C6-alkenediyl in which one methylene group is optionally replaced by a carbonyl group, oxygen, or sulphur, wherein the substituents are halogen, hydroxyl, or mercapto; optionally halogen-substituted C1-C10-alkyl or C1-C6-alkoxy; or a further C3-C6-alkanediyl, C3-C6-alkenediyl, or butadienyl group that is optionally substituted by C1-C6-alkyl or in which two adjacent substituents together with the carbon atoms to which they are attached optionally form a further saturated or unsaturated cycle having 5 or 6 ring atoms that optionally contain oxygen or sulphur, Q1 represents hydrogen or C1-C4-alkyl, or A and Q1 together represent C3-C6-alkanediyl or C4-C6-alkenediyl, each of which is optionally mono- or disubstituted by identical or different halogens, by C1-C10-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, or C3-C7-cycloalkyl, each of which is optionally mono- to trisubstituted by identical or different halogens, or by benzyloxy or phenyl, each of which is optionally mono- to trisubstituted by identical or different substituents selected from the group consisting of halogen, C1-C6-alkyl, and C1-C6-alkoxy in which C3-C6-alkanediyl or C4-C6-alkenediyl is further bridged by a C1-C2-alkanediyl group or by an oxygen atom, Q2, Q4, Q5, and Q6 independently of one another represent hydrogen or C1-C4-alkyl, Q3 represents hydrogen, C1-C6-alkyl, C1-C6-alkoxy-C1-C2-alkyl, C1-C6-alkylthio-C1-C2-alkyl, optionally halogen-, C1-C4-alkyl-, or C1-C4-alkoxy-substituted C3-C8-cycloalkyl in which one methylene group is optionally replaced by oxygen or sulphur or represents optionally halogen-, C1-C4-alkyl-, C1-C4-alkoxy-, C1-C2-haloalkyl-, C1-C2-haloalkoxy-, cyano-, or nitro-substituted phenyl, or Q3 and Q4 together with the carbon atom to which they are attached represent an optionally C1-C4-alkyl-, C1-C4-alkoxy-, or C1-C2-haloalkyl-substituted C3-C7-ring in which one ring atom is optionally replaced by oxygen or sulphur, and G represents hydrogen (a) or represents one of the groups in which E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur, M represents oxygen or sulphur, R1 represents optionally halogen-substituted C1-C20-alkyl, C2-C20-alkenyl, C1-C8-alkoxy-C1-C8-alkyl, C1-C8-alkylthio-C1-C8-alkyl, or poly-C1-C8-alkoxy-C1-C8-alkyl; or represents optionally halogen-, C1-C6-alkyl-, or C1-C6-alkoxy-substituted C3-C8-cycloalkyl, in which optionally one or more ring members that are not directly adjacent are replaced by oxygen and/or sulphur; represents optionally halogen-, cyano-, nitro-, C1-C6-alkyl-, C1-C6-alkoxy-, C1-C6-haloalkyl-, C1-C6-haloalkoxy-, C1-C6-alkylthio-, or C1-C6-alkylsulphonyl-substituted phenyl; represents optionally halogen-, nitro-, cyano-, C1-C6-alkyl-, C1-C6-alkoxy-, C1-C6-haloalkyl-, or C1-C6-haloalkoxy-substituted phenyl-C1-C6-alkyl; represents optionally halogen- or C1-C6-alkyl-substituted 5- or 6-membered hetaryl; represents optionally halogen- or C1-C6-alkyl-substituted phenoxy-C1-C6-alkyl; or represents optionally halogen-, amino-, or C1-C6-alkyl-substituted 5- or 6-membered hetaryloxy-C1-C6-alkyl, R2 represents optionally halogen-substituted C1-C20-alkyl, C2-C20-alkenyl, C1-C8-alkoxy-C2-C8-alkyl, or poly-C1-C8-alkoxy-C2-C8-alkyl; represents optionally halogen-, C1-C6-alkyl-, or C1-C6-alkoxy-substituted C3-C8-cycloalkyl; or represents optionally halogen-, cyano-, nitro-, C1-C6-alkyl-, C1-C6-alkoxy-, C1-C6-haloalkyl-, or C1-C6-haloalkoxy-substituted phenyl or benzyl, R3 represents optionally halogen-substituted C1-C8-alkyl; or represents optionally halogen-, C1-C6-alkyl-, C1-C6-alkoxy-, C1-C4-haloalkyl-, C1-C4-haloalkoxy-, cyano-, or nitro-substituted phenyl or benzyl, R4 and R5 independently of one another represent optionally halogen-substituted C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkylamino, di-(C1-C8-alkyl)amino, C1-C8-alkylthio, C2-C8-alkenylthio, or C3-C7-cycloalkylthio; or represent optionally halogen-, nitro-, cyano-, C1-C4-alkoxy-, C1-C4-haloalkoxy-, C1-C4-alkylthio-, C1-C4-haloalkylthio-, C1-C4-alkyl-, or C1-C4-haloalkyl-substituted phenyl, phenoxy or phenylthio, and R6 and R7 independently of one another represent hydrogen; represent optionally halogen-substituted C1-C8-alkyl, C3-C8-cycloalkyl, C1-C8-alkoxy, C3-C8-alkenyl, or C1-C8-alkoxy-C1-C8-alkyl; represent optionally halogen-, C1-C8-haloalkyl-, C1-C8-alkyl-, or C1-C8-alkoxy-substituted phenyl; represent optionally halogen-, C1-C8-alkyl-, C1-C8-haloalkyl-, or C1-C8-alkoxy-substituted benzyl; or together represent an optionally C1-C4-alkyl-substituted C3-C6-alkylene radical in which one carbon atom is optionally replaced by oxygen or sulphur. 14. A composition according to claim 12 where in formula (I) X represents fluorine, chlorine, bromine, C1-C4-alkyl, C2-C4-alkenyl, C1-C4-alkoxy, trifluoromethyl, trifluoromethoxy, trifluoroethoxy, or cyano, Z represents hydrogen, C2-C4-alkenyl, or C2-C4-alkynyl; or represents the radical in which V1 represents hydrogen, fluorine, chlorine, bromine, C1-C6-alkyl, C1-C4-alkoxy, C1-C2-haloalkyl, C1-C2-haloalkoxy, nitro, or cyano, and V2 represents hydrogen, fluorine, chlorine, bromine, C1-C4-alkyl, C1-C4-alkoxy, C1-C2-haloalkyl, or C1-C2-haloalkoxy, W and Y independently of one another represent hydrogen, fluorine, chlorine, bromine, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, or C1-C4-haloalkoxy, with the proviso that W and X do not simultaneously represent ethyl when Y represents 4-methyl and W does not represent methoxy or difluoromethoxy when X represents ethyl, and with the further proviso that X does not represent alkenyl if Z does not represent hydrogen, and CKE represents one of the groups in which A represents hydrogen; represents optionally fluorine- or chlorine-substituted C1-C6-alkyl, C1-C4-alkoxy-C1-C4-alkyl; or represents optionally fluorine-, chlorine-, C1-C4-alkyl-, or C1-C4-alkoxy-substituted C3-C7-cycloalkyl, B represents hydrogen or C1-C6-alkyl, or A, B, and the carbon atom to which they are attached represent saturated C3-C7-cycloalkyl or unsaturated C5-C7-cycloalkyl in which one ring member is optionally replaced by oxygen or sulphur and that is optionally monosubstituted by C1-C6-alkyl, C1-C3-haloalkyl, or C1-C6-alkoxy; or represent C5-C6-cycloalkyl that is substituted by an alkylenediyl, alkylenedioxy, or alkylenedithiol group that, together with the carbon atom to which it is attached, forms a further five- or six-membered ring and that is optionally substituted by methyl or ethyl and optionally contains one or two oxygen or sulphur atoms that are not directly adjacent; represent C3-C6-cycloalkyl or C5-C6-cycloalkenyl in which two substituents together with the carbon atoms to which they are attached represent optionally C1-C5-alkyl-, C1-C5-alkoxy-, fluorine-, chlorine-, or bromine-substituted C2-C4-alkanediyl, C2-C4-alkenediyl in which one methylene group is optionally replaced by oxygen or sulphur; or represent butadienediyl, D represents hydrogen; represents optionally fluorine- or chlorine-substituted C1-C6-alkyl, C3-C6-alkenyl, or C1-C4-alkoxy-C2-C3-alkyl; represents optionally C1-C4-alkyl-, C1-C4-alkoxy-, or C1-C2-haloalkyl-substituted C3-C7-cycloalkyl in which one methylene group is optionally replaced by oxygen or sulphur; or, except for compounds of formula (I-1) represents optionally fluorine-, chlorine-, bromine-, C1-C4-alkyl-, C1-C4-haloalkyl-, C1-C4-alkoxy-, or C1-C4-haloalkoxy-substituted phenyl, pyridyl, or benzyl; or A and D together represent optionally substituted C3-C5-alkanediyl in which one methylene group is optionally replaced by oxygen or sulphur, wherein the substituents are C1-C4-alkyl; or, for compounds of formula (I-1) together represent one of the groups AD-1 to AD-10: Q1 represents hydrogen, or A and Q1 together represent C3-C4-alkanediyl or C3-C4-alkenediyl, each of which is optionally mono- or disubstituted by identical or different substituents selected from the group consisting of C1-C4-alkyl and C1-C4-alkoxy, Q2 represents hydrogen, Q4, Q5 and Q6 independently of one another represent hydrogen or C1-C2-alkyl, Q3 represents hydrogen, C1-C4-alkyl, C1-C4-alkoxy-C1-C2-alkyl, C1-C4-alkylthio-C1-C2-alkyl or optionally methyl- or methoxy-substituted C3C6-cycloalkyl in which optionally one methylene group is replaced by oxygen or sulphur, or Q3 and Q4 together with the carbon to which they are attached represent an optionally C1-C4-alkyl- or C1-C4-alkoxy-substituted saturated C5-C6-ring in which one ring member is optionally replaced by oxygen or sulphur, and G represents hydrogen (a) or represents one of the groups in which E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur, M represents oxygen or sulphur, R1 represents optionally fluorine- or chlorine-substituted C1-C16-alkyl, C2-C16-alkenyl, C1-C6-alkoxy-C1-C4-alkyl, or C1-C6-alkylthio-C1-C6-alkyl; represents optionally fluorine-, chlorine-, C1-C4-alkyl-, or C1-C4-alkoxy-substituted C3-C7-cycloalkyl in which one or two ring members that are not directly adjacent are optionally replaced by oxygen and/or sulphur; represents optionally fluorine-, chlorine-, bromine-, cyano-, nitro-, C1-C4-alkyl-, C1-C4-alkoxy-, C1-C3-haloalkyl-, or C1-C3-haloalkoxy-substituted phenyl, R2 represents optionally fluorine-substituted C1-C16-alkyl, C2-C16-alkenyl, or C1-C6-alkoxy-C2-C6-alkyl; represents optionally fluorine-, chlorine-, C1-C4-alkyl-, or C1-C4-alkoxy-substituted C3-C7-cycloalkyl; or represents optionally fluorine-, chlorine-, bromine-, cyano-, nitro-, C1-C4-alkyl-, C1-C3-alkoxy-, C1-C3-haloalkyl-, or C1-C3-haloalkoxy-substituted phenyl or benzyl, R3 represents optionally fluorine-substituted C1-C6-alkyl; or represents optionally fluorine-, chlorine-, bromine-, C1-C4-alkyl-, C1-C4-alkoxy-, C1-C3-haloalkyl-, C1-C3-haloalkoxy-, cyano-, or nitro-substituted phenyl, R4 represents C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylamino, di-(C1-C6-alkyl)amino, C1-C6-alkylthio, C3-C4-alkenylthio, or C3-C6-cycloalkylthio; or represents optionally fluorine-, chlorine-, bromine-, nitro-, cyano-, C1-C3-alkoxy-, C1-C3-halo-alkoxy-, C1-C3-alkylthio-, C1-C3-haloalkylthio-, C1-C3-alkyl-, or C1-C3-haloalkyl-substituted phenyl, phenoxy, or phenylthio, R5 represents C1-C6-alkoxy or C1-C6-alkylthio, R6 represents hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl, C1-C6-alkoxy, C3-C6-alkenyl, or C1-C6-alkoxy-C1-C4-alkyl; represents optionally fluorine-, chlorine-, bromine-, C1-C3-haloalkyl-, C1-C4-alkyl-, or C1-C4-alkoxy-substituted phenyl; represents optionally fluorine-, chlorine-, bromine-, C1-C4-alkyl-, C1-C3-haloalkyl-, or C1-C4-alkoxy-substituted benzyl, and R7 represents C1-C6-alkyl, C3-C6-alkenyl, or C1-C6-alkoxy-C1-C4-alkyl, or R6 and R7 together represent an optionally methyl- or ethyl-substituted C4-C5-alkylene radical in which one methylene group is optionally replaced by oxygen or sulphur. 15. A composition according to claim 12 where in formula (I) X represents chlorine, bromine, methyl, ethyl, propyl, vinyl, ethynyl, methoxy, ethoxy, trifluoromethyl, difluoromethoxy, trifluoromethoxy, or cyano, Z represents hydrogen, vinyl, or ethynyl; or represents the radical in which V1 represents hydrogen, fluorine, chlorine, bromine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, methoxy, ethoxy, n-propoxy, isopropoxy, trifluoromethyl, trifluoromethoxy, trifluoroethoxy, or cyano, and V2 represents hydrogen, fluorine, chlorine, methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, trifluoromethyl, or trifluoromethoxy, W and Y independently of one another represent hydrogen, fluorine, chlorine, bromine, methyl, ethyl, n-propyl, methoxy, or ethoxy, with the proviso that W and X do not simultaneously represent ethyl when Y represents 4-methyl and W does not represent methoxy or difluoromethoxy when X represents ethyl, and with the further proviso that X does not represent vinyl or ethynyl if Z does not represent hydrogen, and CKE represents one of the groups in which A represents hydrogen; represents C1-C4-alkyl or C1-C2-alkoxy-C1-C2-alkyl, each of which is optionally mono- to trisubstituted by fluorine; or represents C3-C6-cycloalkyl that is optionally monosubstituted by fluorine, methyl, ethyl, or methoxy, B represents hydrogen, methyl, or ethyl, or A, B, and the carbon atom to which they are attached represent saturated C5-C6-cycloalkyl in which one ring member is optionally replaced by oxygen or sulphur and that is optionally monosubstituted by methyl, ethyl, propyl, isopropyl, trifluoromethyl, methoxy, ethoxy, propoxy, butoxy, or isobutoxy; or represent C5-C6-cycloalkyl that is substituted by an alkylenedioxyl group that contains two oxygen atoms that are not directly adjacent, D represents hydrogen; represents optionally fluorine- or chlorine-substituted C1-C4-alkyl, C3-C4-alkenyl, C1-C2-alkoxy-C2-C3-alkyl, or C3-C6-cycloalkyl in which one methylene group is optionally replaced by oxygen or sulphur, or, except for compounds of formula (I-1) represents phenyl or pyridyl, each of which is optionally mono-substituted by fluorine, chlorine, bromine, methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, trifluoromethyl, or trifluoromethoxy, or A and D together represent optionally substituted C3-C4-alkanediyl in which one carbon atom is optionally replaced by oxygen or sulphur and that is optionally substituted by methyl; or, for compounds of formula (I-1) together represent the group Q1 represents hydrogen, or A and Q1 together represent C3-C4-alkanediyl that is optionally mono- or disubstituted by methyl, or methoxy, Q2 represents hydrogen, Q4, Q5, and Q6 independently of one another represent hydrogen or methyl, Q3 represents hydrogen, methyl, ethyl, or C3-C6-cycloalkyl, or Q3 and Q4 together with the carbon to which they are attached represent an optionally methyl- or methoxy-substituted saturated C5-C6-ring in which one ring member is optionally replaced by oxygen or sulphur, and G represents hydrogen (a) or represents one of the groups in which E represents a metal ion equivalent or an ammonium ion, L represents oxygen, M represents oxygen or sulphur, R1 represents C1-C10-alkyl, C2-C10-alkenyl, C1-C4-alkoxy-C1-C2-alkyl, C1-C4-alkylthio-C1-C2-alkyl, each of which is optionally mono- to trisubstituted by fluorine or chlorine; or represents C3-C6-cycloalkyl which is optionally mono- to trisubstituted by fluorine, chlorine, methyl, ethyl, or methoxy; represents phenyl that is optionally mono- or disubstituted by fluorine, chlorine, bromine, cyano, nitro, methyl, methoxy, trifluoromethyl, or trifluoromethoxy, R2 represents C1-C10-alkyl, C2-C10-alkenyl, or C1-C4-alkoxy-C2-C4-alkyl, each of which is optionally mono- to trisubstituted by fluorine; represents C3-C6-cycloalkyl that is optionally mono-substituted by fluorine, methyl, or methoxy; or represents phenyl or benzyl, each of which is optionally mono- or disubstituted by fluorine, chlorine, cyano, nitro, methyl, methoxy, trifluoromethyl, or trifluoromethoxy, R3 represents methyl, ethyl, n-propyl, or isopropyl, each of which is optionally mono- to trisubstituted by fluorine; or represents phenyl that is optionally monosubstituted by fluorine, chlorine, bromine, methyl, tert-butyl, methoxy, trifluoromethyl, trifluoro-methoxy, cyano, or nitro, R4 represents C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkylamino, di-(C1-C4-alkyl)amino, or C1-C4-alkylthio; or represents phenyl, phenoxy, or phenylthio, each of which is optionally mono-substituted by fluorine, chlorine, bromine, nitro, cyano, C1-C2-alkoxy, C1-C2-fluoroalkoxy, C1-C2-alkylthio, C1-C2-fluoroalkyl-thio, or C1-C3-alkyl, R5 represents C1-C3-alkoxy or C1-C3-alkylthio, R6 represents hydrogen; represents C1-C4-alkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C3-C4-alkenyl, OR C1-C4-alkoxy-C1-C4-alkyl; represents phenyl that is optionally mono- or disubstituted by fluorine, chlorine, bromine, trifluoromethyl, methyl, or methoxy; or represents benzyl that is optionally monosubstituted by fluorine, chlorine, bromine, methyl, trifluoromethyl, or methoxy, and R7 represents C1-C4-alkyl, C3-C4-alkenyl, or C1-C4-alkoxy-C1-C2-alkyl, or R6 and R7 together represent a C5-C6-alkylene radical in which one methylene group is optionally replaced by oxygen or sulphur. 16. A composition according to claim 15 in which, in formula (I), Z represents hydrogen and Y is located in the position para to the group CKE, or in which Z represents the group in the position para or meta to the group CKE. 17. A composition according to claim 12 in which, in formulas (IIa), (IIb), (IIc), (IId), and (IIe), n represents the number 0, 1, 2, 3, or 4, A1 represents one of the divalent heterocyclic groups A2 represents optionally methyl-, ethyl-, methoxycarbonyl-, or ethoxycarbonyl-substituted methylene or ethylene, R8 represents hydroxyl, mercapto, amino, methoxy, ethoxy, n- or i-propoxy, n-, i-, s-, or t-butoxy, methylthio, ethylthio, n- or i-propylthio, n-, i-, s-, or t-butylthio, methylamino, ethylamino, n- or i-propylamino, n-, i-, s-, or t-butylamino, dimethylamino, or diethylamino, R9 represents hydroxyl, mercapto, amino, methoxy, ethoxy, n- or i-propoxy, n-, i-, s-, or t-butoxy, methylthio, ethylthio, n- or i-propylthio, n-, i-, s-, or t-butylthio, methylamino, ethylamino, n- or i-propylamino, n-, i-, s-, or t-butylamino, dimethylamino, or diethylamino, R10 represents optionally fluorine-, chlorine-, and/or bromine-substituted methyl, ethyl, or n- or i-propyl, R11 represents hydrogen; represents optionally fluorine- and/or chlorine-substituted methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, propenyl, butenyl, propynyl, butynyl, methoxymethyl, ethoxymethyl, methoxyethyl, ethoxyethyl, dioxolanylmethyl, furyl, furylmethyl, thienyl, thiazolyl, or piperidinyl; or represents optionally fluorine-, chlorine-, methyl-, ethyl-, n- or i-propyl, or n-, i-, s-, or t-butyl-substituted phenyl, R12 represents hydrogen; represents optionally fluorine- and/or chlorine-substituted methyl, ethyl, n- or i-propyl, n-, i-, s- or t-butyl, propenyl, butenyl, propynyl, butynyl, methoxymethyl, ethoxymethyl, methoxyethyl, ethoxyethyl, dioxolanylmethyl, furyl, furylmethyl, thienyl, thiazolyl, or piperidinyl; or represents optionally fluorine-, chlorine-, methyl-, ethyl-, n- or i-propyl-, or n-, i-, s-, or t-butyl-substituted phenyl; or together with R11 represents one of the radicals —CH2—O—CH2—CH2— and —CH2—CH2—O—CH2—CH2—, each of which is optionally substituted by methyl, ethyl, furyl, phenyl, a fused-on benzene ring, or by two substituents that together with the carbon atom to which they are attached form a 5- or 6-membered carbocycle, R13 represents hydrogen, cyano, fluorine, chlorine, or bromine; or represents optionally fluorine-, chlorine-, and/or bromine-substituted methyl, ethyl, n- or i-propyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or phenyl, R14 represents hydrogen; or represents optionally hydroxyl-, cyano-, fluorine-, chlorine-, methoxy-, ethoxy-, or n- or i-propoxy-substituted methyl, ethyl, n- or i-propyl, or n-, i-, s-, or t-butyl, R15 represents hydrogen, cyano, fluorine, chlorine, or bromine; or represents optionally fluorine-, chlorine-, and/or bromine-substituted methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or phenyl, X1 represents nitro, cyano, fluorine, chlorine, bromine, methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, difluoromethyl, dichloromethyl, trifluoromethyl, trichloromethyl, chlorodifluoromethyl, fluorodichloromethyl, methoxy, ethoxy, n- or i-propoxy, difluoromethoxy, or trifluoromethoxy, X2 represents hydrogen, nitro, cyano, fluorine, chlorine, bromine, methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, difluoromethyl, dichloromethyl, trifluoromethyl, trichloromethyl, chlorodifluoromethyl, fluorodichloromethyl, methoxy, ethoxy, n- or i-propoxy, difluoromethoxy, or trifluoromethoxy, X3 represents hydrogen, nitro, cyano, fluorine, chlorine, bromine, methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, difluoromethyl, dichloromethyl, trifluoromethyl, trichloromethyl, chlorodifluoromethyl, fluorodichloromethyl, methoxy, ethoxy, n- or i-propoxy, difluoromethoxy, or trifluoromethoxy, R16 represents hydrogen, methyl, ethyl, or n- or i-propyl, R17 represents hydrogen, methyl, ethyl, or n- or i-propyl, R18 represents hydrogen; represents optionally cyano-, fluorine-, chlorine-, methoxy-, ethoxy-, or n- or i-propoxy-substituted methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, methoxy, ethoxy, n- or i-propoxy, n-, i-, s-, or t-butoxy, methylthio, ethylthio, n- or i-propylthio, n-, i-, s-, or t-butylthio, methylamino, ethylamino, n- or i-propylamino, n-, i-, s-, or t-butylamino, dimethylamino, or diethylamino; or represents optionally cyano-, fluorine-, chlorine-, bromine-, methyl-, ethyl-, or n- or i-propyl-substituted cyclopropyl, cyclobutyl, cyclo-pentyl, cyclohexyl, cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclo-hexyloxy, cyclopropylthio, cyclobutylthio, cyclopentylthio, cyclohexylthio, cyclopropylamino, cyclobutylamino, cyclopentylamino, or cyclohexylamino, R19 represents hydrogen; represents optionally cyano-, hydroxyl-, fluorine-, chlorine, methoxy-, ethoxy-, or n- or i-propoxy-substituted methyl, ethyl, n- or i-propyl, n-, i-, or s-butyl; represents optionally cyano-, fluorine-, chlorine-, or bromine-substituted propenyl, butenyl, propynyl, or butynyl; or represents optionally cyano-, fluorine-, chlorine-, bromine-, methyl-, ethyl-, n- or i-propyl-substituted cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl, R20 represents hydrogen; represents optionally cyano-, hydroxyl-, fluorine-, chlorine-, methoxy-, ethoxy-, or n- or i-propoxy-substituted methyl, ethyl, n- or i-propyl, or n-, i-, or s-butyl; represents optionally cyano-, fluorine-, chlorine-, or bromine-substituted propenyl, butenyl, propynyl, or butynyl; represents optionally cyano-, fluorine-, chlorine-, bromine-, methyl-, ethyl-, or n- or i-propyl-substituted cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; or represents optionally nitro-, cyano-, fluorine-, chlorine-, bromine-, methyl-, ethyl-, n- or i-propyl-, n-, i-, s-, or t-butyl-, trifluoromethyl-, methoxy-, ethoxy-, n- or i-propoxy-, difluoromethoxy-, or trifluoromethoxy-substituted phenyl; or together with R19 represents optionally methyl- or ethyl-substituted butane-1,4-diyl (trimethylene), pentane-1,5-diyl, 1-oxa-butane-1,4-diyl, or 3-oxa-pentane-1,5-diyl, X4 represents nitro, cyano, carboxyl, carbamoyl, formyl, sulphamoyl, hydroxyl, amino, fluorine, chlorine, bromine, methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, trifluoromethyl, methoxy, ethoxy, n- or i-propoxy, difluoromethoxy, or trifluoromethoxy, and X5 represents nitro, cyano, carboxyl, carbamoyl, formyl, sulphamoyl, hydroxyl, amino, fluorine, chlorine, bromine, methyl, ethyl, n- or i-propyl, n-, i-, s-, or t-butyl, trifluoromethyl, methoxy, ethoxy, n- or i-propoxy, difluoromethoxy, or trifluoromethoxy. 18. A composition according to claim 12 in which the compound that improves crop plant compatibility is cloquintocet-mexyl, fenchlorazole-ethyl, isoxadifen-ethyl, mefenpyr-diethyl, furilazole, fenclorim, cumyluron, dymron, dimepiperate, or the compound 19. A composition according to claim 12 in which the compound that improves crop plant compatibility is cloquintocet-mexyl or mefenpyr-diethyl. 20. A composition according to claim 12 wherein from 0.05 to 10 parts by weight of the compound that improves crop plant compatibility are present per part by weight of the active compound of the formula (I). 21. A method for controlling undesirable vegetation comprising allowing an effective amount of a composition according to claim 12 to act on plants and/or their habitat. |
High-density multi-layer optical disc, method for recording data thereon on layer-by-layer basis, and method for managing spare areas thereof |
A high-density multi-layer optical disc, a method for recording data thereon on a layer-by-layer basis, and a method for managing spare areas thereof. In a high-density multi-layer optical disc, having a plurality of recording layers formed thereon, such as a Blu-ray disc rewritable (BD-RE) dual layer, management information is recorded and managed appropriately to the multiple layers so that data can be recorded in a state where the recording layers are linked to each other or the recording layers are separated from each other. Inner and outer spare areas are separately assigned to each of the recording layers formed on the high-density multi-layer optical disc. The management information is recorded and managed appropriately to the multiple layers so that the data can be recorded in a state where the spare areas of the recording layers or used together irrespective of the recording layers or used separately on the layer-by-layer basis. The recording layers can be effectively used and managed, and the spare areas separately assigned to the respective recording layers can be effectively used and managed. |
1. A high-density multi-layer optical disc having a plurality of recording layers formed thereon, comprising: at least one of spare areas separately assigned to each of the recording layers, the spare areas being usable when a defect is detected and to be managed; and at least one specified area contained in at least one of recording layers, the specified area having management information indicating whether the recording layers must be used together or separately. 2. The high-density multi-layer optical disc as set forth in claim 1, wherein the management information is contained and recorded in a field of disc definition structure (DDS) information and/or disc information (DI) recorded and managed in a lead-in area or lead-out area separately assigned to each recording layer. 3. The high-density multi-layer optical disc as set forth in claim 2, wherein the DDS information comprises spare area management information needed for managing the spare areas separately assigned to the recording layers, and a defect address management (DAM) information needed for managing a defect list (DFL), the DDS information being recorded on at least one of the recording layers. 4. The high-density multi-layer optical disc as set forth in claim 3, wherein the spare area management information comprises information indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on a layer-by-layer basis. 5. The high-density multi-layer optical disc as set forth in claim 4, wherein the spare area management information comprises information indicating a size of an inner spare area or outer spare area separately assigned to a data area of each recording layer, and spare area full flag information indicating whether or not a corresponding spare area is full. 6. The high-density multi-layer optical disc as set forth in claim 5, wherein the spare area full flag information comprises information of at least two bits indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on the layer-by-layer basis. 7. The high-density multi-layer optical disc as set forth in claim 5, wherein the DDS information comprises information of at least two bits indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on the layer-by-layer basis, separated from the spare area full flag information indicating whether each of the spare areas is full. 8. The high-density multi-layer optical disc as set forth in claim 3, wherein the DDS information further comprises last verified address (LVA) pointer information on a layer-by-layer basis, said last verified address specifying the first physical sector number of the last cluster that has been verified. 9. The high-density multi-layer optical disc as set forth in claim 2, wherein the DT comprises layer separate use information indicating whether the recording layers must be used together or separately at the time of performing the data recording operation. 10. The high-density multi-layer optical disc as set forth in claim 9, wherein the layer separate use information is recorded and managed as a 1-bit flag. 11. A high-density multi-layer optical disc having a plurality of recording layers formed thereon, comprising: an inner spare area and outer spare area assigned to each data area, while each data area being assigned to each of the recording layers; and management information, additionally recorded in a lead-in area, indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on a layer-by-layer basis. 12. The high-density multi-layer optical disc as set forth in claim 11, wherein the management information is contained and recorded in a field of disc definition structure (ADS) information contained and recorded in the lead-in area. 13. The high-density multi-layer optical disc as set forth in claim 12, wherein the DDS information comprises information indicating a size of the inner spare area or outer spare area separately assigned to the data area for each recording layer, and spare area full flag information indicating whether or not a corresponding spare area is full. 14. The high-density multi-layer optical disc as set forth in claim 13, wherein the spare area full flag information comprises information of at least two bits indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on the layer-by-layer basis. 15. The high-density multi-layer optical disc as set forth in claim 13, wherein the DDS information comprises information of at least two bits indicating whether the spare areas of the recording layers must be used together irrespective of the recording layers or used separately on the layer-by-layer basis, separated from the spare area full flag information indicating whether each of the spare areas is full. 16. The high-density multi-layer optical disc as set forth in claim 14, wherein the management information indicates that a data recording operation for a spare area can be omitted if data to be recorded in the spare area is audio/video (A/V) data, and that the data recording operation for the spare area can be performed if the data to be recorded in the spare area is predetermined information data other than the AN data. 17. A method for recording data on a high-density multi-layer optical disc on a layer-by-layer basis, comprising the steps of: (a) reading disc definition structure (DDS) information recorded in at least one specified area of the high-density multi-layer optical disc, and storing the read information in a memory, wherein the disc definition structure information includes control information for indicating whether recording layers must be used together or separately; (b) determining whether to use the recording layers together or separately based on the control information; and (c) performing the data recording operation and/or a defect management operation according to a result of the determination. 18. The method as set forth in claim 17, wherein the step (b) is carried out by searching for and confirming the control information contained in a field of the DDS, and determining whether the recording layers must be used together or separately at the time of performing the data recording operation. 19. The method as set forth in claim 17, wherein the step (c) is carried out by referring to the control information contained in DDS information and performing the data recording operation and/or the defect management operation for only an arbitrary recording layer according to the result of the determination. 20. The method as set forth in claim 17, wherein the step (c) is carried out by referring to the control information contained in DDS information and performing the data recording operation and/or the defect management operation for the recording layers according to the result of the determination. 21. The method as set forth in claim 20, wherein the step (c) comprises the steps of: (c-1) detecting a defect within a data area of the high-density multi—layer optical disc while the data is recorded in the data area; (c-2) searching for and confirming spare area management information from the read DDS information, when the defect is detected; (c-3) determining whether spare areas separately assigned to a current recording layer must be used together with other spare areas separately assigned to another recording layer or only the spare areas of the current recording layer must be used separately, according to the confirmed spare area management information; and (c-4) generating a defect list (DFL) entry needed for managing the defect and recording the generated DFL entry to 15 manage the recorded DFL entry, when the data is recorded in an arbitrary spare area. 22. A method for managing spare areas of a high-density multi-layer optical disc, comprising the steps of: (a) detecting a defect within a data area of the high-density multi-layer optical disc while the data is recorded in the data area; (b) confirming spare area management information read from a lead-in area of the high-density multi-layer optical disc, when the defect is detected; and (c) determining whether spare areas separately assigned to a current recording layer must be used together with other spare areas separately assigned to another recording layer or only the spare areas of the current recording layer must be used separately, according to the confirmed spare area management information. 23. The method as set forth in claim 22, wherein the step (b) is carried out by confirming the spare area management information within disc definition structure (DDS) information read from the lead-in area of the high-density multi-layer optical disc. 24. The method as set forth in claim 22, further comprising the steps of: (d) generating a defect list (DFL) entry needed for managing the defect and recording the generated DFL entry to manage the recorded DFL entry, when the data is recorded in an arbitrary spare area. 25. A method for managing spare area of a high-density multi-layer optical recording medium, comprising the steps of: (a) reading control information stored in an area of the optical recording medium, said control information including indication information for indicating whether or not at least two layers are associated with each other to record data to or read data from the recording medium; and (b) controlling recording or reading based on the control information. 26. A method for managing spare area of a high-density multi-layer optical recording medium, comprising the steps of: (a) recording control information on an area of the optical recording medium, said control information including indication information for indicating whether or not at least two recording layers are associated with each other for data to he recorded or read; and (b) controlling recording or reading based on the control information. 27. The high-density multi-layer optical disc as set forth in claim 15, wherein the management information indicates that a data recording operation for a spare area can be omitted if data to be recorded in the spare area is audio/video (A/V) data, and that the data recording operation for the spare area can be performed if the data to be recorded in the spare area is predetermined information data other than the AN data. |
<SOH> 2. BACKGROUND ART <EOH>As standardization of a high-density rewritable optical disc, e.g., a Blu-ray disc rewritable (BD-RE), capable of storing high-quality video and audio is rapidly progressed, it is expected that related products will be developed, commercialized and supplied. A conventional BD-RE single layer 100 is shown in FIG. 1 . As shown in FIG. 1 , there is a distance of approximately 0.1 mm between a recording layer and the surface of a transparent film being arranged between the recording layer and an objective lens (OL) 11 of an optical pick-up. When an optical disc apparatus for reading and reproducing data recorded on the recording layer of the BD-RE single layer 100 or recording data thereon determines that a defect is detected on the layer 100 while performing a data recording operation, the optical disc apparatus records the data in an inner spare area (ISA) or outer spare area (OSA) separately assigned to a data area as shown in FIG. 2 , in place of a data area. Further, the optical disc apparatus generates a defect list (DFL) entry needed for identifying a cluster associated with a recording unit block (RUB) recorded in the spare area in place of a data area, and performs a recording and management operation for the generated DFL entry. As shown in FIG. 2 , management information associated with the spare areas is contained and recorded in a field of rewritable disc definition structure (DDS) information of a lead-in area. The DDS information includes information items associated with the first physical sector number (PSN) of the DFL (P_DFL), a location of a logical sector number (LSN) 0 of a user data area, the last LSN of the user data area, a size of the ISA (ISA_size), a size of the OSA (OSA_size), spare area full flags indicating whether the respective spare areas are full, the last verified address (LVA) pointer, etc. The spare area full flags are recorded by one byte consisting of a 1-bit ISA full flag, a 1-bit OSA full flag and 6-bit reserved information assigned to a reserved area. As described above, when the defect is detected in the data area while the optical disc apparatus records data in the data area, the optical disc apparatus searches for the spare area full flags contained and recorded in the DDS information field, selects the ISA or OSA in which the data can be recorded, and performs a sequence of data recording operations for recording the data in the selected spare area. A high-density dual-layer optical disc, i.e., a BD-RE dual layer, capable of recording twice as much video and audio data as the BD-RE single layer, has been developed. As shown in FIG. 3 , there is a distance d2 between the first recording layer (Layer 0 ) and the second recording layer (Layer 1 ) formed in the BD-RE dual layer 200 . The first and second recording layers are formed at a location, within the BD-RE dual layer 200 , having a bias toward the OL 11 of the optical pick-up. The first and second recording layers of the BD-RE dual layer 200 are linked to each other so that the large-capacity data can e recorded. The ISA and OSA can be separately assigned to each of the data areas associated with the first and second recording layers. However, there is not yet provided a method for efficiently employing the first and second recording layers of the BD-RE dual layer 200 on a layer-by-layer basis. Moreover, there is not yet provided a method for efficiently employing and managing a plurality of spare areas separately assigned to each recording layer. |
<SOH> 4. BRIEF DESCRIPTION OF DRAWINGS <EOH>The accompanying drawings, which are included to provide a further understanding of the invention, illustrate the preferred embodiments of the invention, and together with the description, serve to explain the principles of the present invention. FIG. 1 is a view illustrating the structure of a conventional Blu-ray disc rewritable (BD-RE); FIG. 2 is a table illustrating disc definition structure (DDS) information recorded and managed in a lead-in area of the conventional BD-RE; FIG. 3 is a view illustrating the structure of a high-density dual-layer optical disc; FIG. 4 is a view illustrating a state where disc information (DI) and disc definition structure (DDS) information are contained in lead-in and lead-out areas of the high-density dual-layer optical disc in accordance with the present invention; FIG. 5 is a table illustrating the DDS information recorded and managed in each of the lead-in and lead-out areas of the high-density dual-layer optical disc in accordance with the present invention; FIG. 6 is a view illustrating the configuration of an optical disc apparatus to which a method for recording data on the disc on a layer-by-layer basis and managing spare areas of the disc is applied in accordance with the present invention; FIG. 7 is a flowchart illustrating a method for recording data on the high-density dual-layer optical disc on the layer-by-layer basis in accordance with the present invention; FIG. 8 is a flowchart illustrating a method for managing spare areas of the high-density dual-layer optical disc in accordance with the present invention; and FIG. 9 is another table illustrating the DDS information based on the spare area management method in accordance with the present invention. detailed-description description="Detailed Description" end="lead"? Features, elements, and aspects of the invention that are referenced by the same numerals in different figures represent the same, equivalent, or similar features, elements, or aspects in accordance with one or more embodiments. |
High-density multi-layer optical disc and method for managing layer formatting thereof |
A high-density multi-layer optical disc and a method for managing layer formatting thereof. A high-density multi-layer optical disc such as a Blu-ray disc rewittable (BD-RE) dual layer includes management information, additionally recorded in a lead-in area, needed for identifying formatting status of a plurality of recording layers. After the management information is referred to, at least one unformatted recording layer is automatically formatted. Optionally, the unformatted recording layer is formatted on the basis of a formatting method selected by a user. The multiple recording layers formed on the high-density multi-layer optical disc can be conveniently and effectively formatted. |
1. A high-density multi-layer optical disc, comprising: a plurality of recording layers formed thereon; and management information, additionally recorded in a specified area thereof, needed for identifying formatting status of the recording layers. 2. The high-density multi-layer optical disc as set forth in claim 1, wherein the management information is recorded in disc definition structure (DDS) information contained in the lead-in area. 3. The high-density multi-layer optical disc as set forth in claim 2, wherein the management information consists of the predetermined number of bits indicating the formatting status of the recording layers. 4. The high-density multi-layer optical disc as set forth in claim 2, wherein the management information comprises the status information indicating that none of first and second recording layers are formatted, or only the first or second recording layer is formatted, or all of the first and second recording layers are formatted, if the high-density multi-layer optical disc is a dual-layer optical disc. 5. The high-density multi-layer optical disc as set forth in claim 1, further comprises position information for respective recording layers, while the position information specifying a first physical sector number (PSN) of the last unit that has been formatted. 6. A method for managing layer formatting of a high-density multi-layer optical disc, comprising the steps of: (a) reading management information indicating formatting status of recording layers, while the management information being recorded in a specified area of the high-density multi-layer optical disc; (b) determining formatting status of recording layers based on the read management information; and (c) performing a formatting operation automatically or in response to a user's selection for at least one unformatted recording layer according to a result of the determination. 7. The method as set forth in claim 6, wherein the step (a) comprises the steps of: (a-1) searching for disc definition structure (DDS) information contained in the lead-in area of the high-density multi-layer optical disc; and (a-2) reading the management information indicating formatting status of recording layers, while the management information having the predetermined number of bits recorded in the DDS information; and 8. The method as set forth in claim 6, wherein the step (c) is carried out by automatically performing a formatting operation for said at least one unformatted recording layer using a predetermined formatting method, if said at least one unformatted recording layer exists as the result of the determination. 9. The method as set forth in claim 8, wherein the predetermined formatting method is a background formatting method. 10. The method as set forth in claim 6, wherein the step (c) is carried out by generating and outputting an image of an on-screen display (OSD) indicating that all recording layers are not formatted if none of the recording layers are formatted as the result of the determination, and performing the formatting operation in response to the user's selection. 11. The method as set forth in claim 10, wherein the OSD image comprises a selection menu for allowing the user to select said at least one unformatted recording layer to be formatted and a formatting method. 12. The method as set forth in claim 6, wherein the step (a) further comprises the step of reading position information for respective recording layers, while the position information specifying a first physical sector number of the last unit that has been formatted. 13. The method as set forth in claim 12, wherein the step (c) is carried out by continuing a formatting operation for said at least one unformatted recording layer from the PSN contained in the read position information. |
<SOH> 2. BACKGROUND ART <EOH>As standardization of a high-density rewritable optical disc, e.g., a Blu-ray disc rewritable (BD-RE), capable of storing high-quality video and audio is rapidly progressed, it is expected that related products will be developed, commercialized and supplied. A conventional BD-RE single layer 100 is shown in FIG. 1 . As shown in FIG. 1 , there is a distance of approximately 0.1 mm between a recording layer and the surface of a transparent film being arranged between the recording layer and an objective lens (OL) 11 of an optical pick-up. When an optical disc apparatus for reading and reproducing data recorded on the recording layer of the BD-RE single layer 100 or recording data thereon determines that a defect is detected on the layer 100 while performing a data recording operation, the optical disc apparatus records the data in an inner spare area (ISA) or outer spare area (OSA) separately assigned to a data area as shown in FIG. 2 , in place of a data area. Further, the optical disc apparatus generates a defect list (DFL) entry needed for identifying a cluster associated with a recording unit block (RUB) recorded in the spare area in place of a data area, and performs a recording and management operation for the generated DFL entry. As shown in FIG. 2 , management information associated with the spare areas and defects is contained and recorded in a field of rewritable disc definition structure (DDS) information of a lead-in area. The DDS information includes information items associated with the first physical sector number (PSN) of the DFL (P_DFL) a location of a logical sector number (LSN) 0 of a user data area, the last LSN of the user data area, a size of the ISA (ISA size), a size of the OSA (OSA size), spare area full flags indicating whether or not the respective spare areas are full, etc. As described above, when the defect is detected in the data area while the optical disc apparatus records data in the data area, the optical disc apparatus searches for the spare area full flags contained and recorded in the DDS information field, selects the ISA or OSA in which the data can be recorded, and performs a sequence of data recording operations for recording the data in the selected spare area. The recording layer of the BD-RE single layer 100 must be previously formatted so that the data can be recorded on the recording layer. The layer formatting method includes a general formatting method requiring a long formatting time, a recently proposed background formatting method, etc. Here, the background formatting method is that a formatting operation is performed automatically when or whenever the recording or reproducing device is idle, and stores information associated with the location of a formatted area until a time point when a data recording request is received from a user, thereby enabling the data, corresponding to the data recording request, to be recorded in the formatted area until the time point. A high-density multi-layer optical disc, i.e., a BD-RE dual layer, capable of recording twice as much video and audio data as the BD-RE single layer, has been developed. As shown in FIG. 3 , there is a distance d2 between the first recording layer (Layer 0) and the second recording layer (Layer 1) formed in the BD-RE dual layer 200 . The first and second recording layers are formed at a location, within the BD-RE dual layer 200 , having a bias toward the OL 11 of the optical pick-up. The ISA and OSA are separately assigned to each of data areas associated with the first and second recording layers of the BD-RE dual layer 200 . The first and second recording layers can be linked to each other so that large-capacity data can be recorded. However, there is not yet provided a method for effectively formatting the first and second recording layers provided in the BD-RE dual layer 200 . |
<SOH> 4. BRIEF DESCRIPTION OF DRAWINGS <EOH>The accompanying drawings, which are included to provide a further understanding of the invention, illustrate the preferred embodiments of the invention, and together with the description, serve to explain the principles of the present invention. FIG. 1 is a view illustrating the structure of a conventional Blu-ray disc rewritable (BD-RE); FIG. 2 is a table illustrating disc definition structure (DDS) information recorded and managed in a lead-in area of the conventional BD-RE; FIG. 3 is a view illustrating the structure of a high-density dual-layer optical disc; FIG. 4 is a view illustrating a state where disc definition structure (DDS) information is contained in a lead-in area of the high-density dual-layer optical disc in accordance with the present invention; FIG. 5 is a table illustrating the DDS information recorded and managed in the lead-in area of the high-density dual-layer optical disc in accordance with the present invention; FIG. 6 is a view illustrating the configuration of an optical disc apparatus to which a method for managing layer formatting of a high-density multi-layer optical disc is applied in accordance with the present invention; FIGS. 7A and 7B are flowcharts illustrating the method for managing layer formatting of a high-density multi-layer optical disc in accordance with the present invention; and FIG. 8 is a view illustrating an image of an on-screen display (OSD) displayed by the method for managing layer formatting of a high-density multi-layer optical disc in accordance with the present invention. detailed-description description="Detailed Description" end="lead"? Features, elements, and aspects of the invention that are referenced by the same numerals in different figures represent the same, equivalent, or similar features, elements, or aspects in accordance with one or more embodiments. |
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