An image processing apparatus includes: a reading part for optically reading an image from an original image on a recording medium; a conversion part for converting the read-out image into a digital image; a first storage part for storing the digital image; an input part for inputting an instruction and a password number; an encoding part for transforming the digital image to an encoded image when an encoding process for the digital image is selected according to the instruction; a decoding part for transforming the digital image to a decoded image when a decording process for the digital image is selected according to the instruction, a second storage part for storing the encoded image in accordance with a memory address determined based on the password number when the encoding process is selected, and for storing the decoded image in accordance with the memory address determined based on the password number when the decoding process is selected, and an output part for outputting either the encoded image or the decoded image onto a recording medium so that either an image encoded from the original image or an image decoded from the encoded image is recorded.

The present invention generally relates to reproduction of bit information on a recording medium, and more particularly to an image processing apparatus for transforming bit information on a recording medium to encoded data and for transforming the encoded data to decoded data, so that a reconstructed data from the encoded data is recorded on a recording medium.
There is an information reproducing device which is of the type relevant to the present invention. Japanese Laid-Open Patent Publication No.3-123988 discloses this information reproducing device for reproducing data from original bit information recorded on a recording medium so that reproduced data of characters, pictures, or sound is recorded on a recording medium. The device disclosed in this publication relates to correct and precise reproduction of bit array information on a recording medium.
In the case of the information reproducing device mentioned above, a sequence of codes or bit array information of character, picture or sound data is recorded on a sheet-like recording medium, and it can be easily read by an optical reader. The data on the recording medium is transmitted from an information reproducing device to another information reproducing device via the existing mailing system. On reception of the data by the receiving device, the code sequence of the original data of characters, pictures, or sound is reproduced. In order to increase the performance and operability of the device, start data, end data and identification data are added to the code sequence of the original data, and such composite data is transmitted and received.
However, in the conventional device disclosed in the above mentioned publication, the receiving device can easily reproduce the bit information when the data of the bit information is received from the transmitting device, even if the data of the bit information is confidential. That is, in the above mentioned publication, there is no disclosure of a technique for preventing the leakage of the confidential data of the bit information to an unauthorized person.
There are other techniques relevant to the apparatus according to the present invention. A data encoding method appropriate for transmitting and receiving data of facsimile communications is disclosed in a transaction of the Institute of Picture and Communication Engineers of Japan, vol.17, No.6, 1988, entitled "Confidential Data protective Facsimile Communication Method Using A Scramble Technique". A data encoding method appropriate for digital images is disclosed in a transaction of the Institute of Electronics and Communication Engineers of Japan, 86/11 vol.1, J69-B No.11, entitled "A Technique of Data Encoding Appropriate For Digital Images".
In the cases of the above mentioned methods, the encoding process is carried out for data of digital signals only. However, there is no disclosure of handling of a recording medium on which bit information is recorded in order for the encoding and decoding of the bit information on the recording medium. That is, in the above mentioned methods, there is no disclosure of a device for transforming bit information on a recording medium to encoded data, and for transforming the encoded data to decoded data to record the reconstructed data on a recording medium.

Apparatus for encoding and decoding information on recording medium


Methods and apparatuses for automatic restoration detection and automatic restoration of optical communication system are disclosed. In the methods, a first station sends an automatic restoration detection message to a second station at the opposite side of a failed link; in response to receiving an automatic restoration request message, determines that the link has been repaired in two directions, and sends an automatic restoration confirmation message to the second station; or in response to receiving the automatic restoration detection message, determines that the link from the second station to the first station has been repaired, and sends the automatic restoration request message to the second station; in response to receiving the automatic restoration confirmation message, determines that the link has been repaired in two directions; and switching to normal working states. The safety problem that the laser leakage occurs in the failed link is solved.

Because of the excellent directivity, the power density of laser in the output direction is especially high, which greatly threatens human eyes. The wavelength of lasers used in the existing communication system is generally around 870 nm, 1310 nm and 1550 nm, which are all beyond the wavelength range of visible light. Because it is invisible to the naked eye, the light beam has a greater possibility to hurt human eyes. After the inventions of Erbium-Doped Fiber Amplifier (EDFA) and Wavelength Division Multiplexing (WDM) techniques, the output power of optical signals carried in fibers is even higher than that of conventional Synchronous Digital Hierarchy (SDH) devices. In addition, such apparatuses as RAMAN amplifier may be introduced into the existing communication system, which makes the power of optical signals carried in fibers of some systems reach or even exceed 30 dBm. Such high power of the optical signal greatly threatens the safety of operators and maintenance personnel of telecommunication system.
The safety level of laser apparatus and device is defined in Standard IEC60825, which specifies the specific operational measure and safety identifier as well. The International Telecommunication Union-Telecommunication Standardization Sector (ITU-T) constitutes Standard G.664 for laser safety in communication system. According to the Standard G.664, an optical communication apparatus should be able to automatically reduce the output power to a power threshold for safety and even turn off a laser when a laser leakage occurs. The solution is expressed as an Automatic Power Reduction (APR) and an Automatic Power Shutdown (APSD) solution in G.664.

Method and apparatus for automatic restoration detection and automatic restoration of optical communication system


An efficient process for saccharifying lignocellulosic biomass in concentrated aqueous solutions of certain bromine salts, particularly LiBr and CaBr2. Real lignocellulose biomass, such as corn stover, switchgrass, waste paper, hardwood, and softwood, can be hydrolyzed without the need for any prior pretreatment. Complete saccharification of both cellulose and hemicellulose is achieved within 5-200 min at temperatures ranging from about 100 to about 160° C. Residual lignin is readily separated from product sugars by filtration or centrifugation and can be used to prepare beneficial coproducts. The bromine salt can be recovered and separated from product sugars (predominantly monosaccharides) by any art-known method and in particular solvent extraction, anti-solvent precipitation, ion-exclusion chromatography and/or ion-exchange chromatography can be employed. Hydrolysis product containing sugars can be employed for in fermentation for the production of value added products or useful fuels.

Production of transportation fuels from renewable biomass resources can reduce dependence on traditional fossil fuel, relieve the energy crisis, create new jobs, stimulate local economies, and reduce greenhouse gas emissions. Currently bioethanol is produced from cornstarch or sugarcane. Such processes are not sustainable and are unable to meet the increasing demand for renewable fuels. Sustainable production of biofuel must rely on abundant, inexpensive, and non-food lignocellulosic biomass. A core bottleneck of biomass conversion processes based on a sugar platform is the effective release of sugars from inexpensive, non-food and abundant lignocellulosic biomass at low cost and low energy input[1]. Cellulose in lignocellulosic materials is wrapped by hemicellulose and especially lignin, making cellulose far more difficult to hydrolyze into glucose than starch. In addition cellulose has a crystalline structure and stronger glucosidic bonds than starch (β- vs. α-glucosidic bonds). As a consequence, relatively harsh conditions such as high temperature and more chemicals are needed for hydrolyzing cellulose[2]. Primary methods that have been extensively investigated for saccharification of lignocellulosic materials include concentrated acid, diluted acid, ionic liquid and enzymatic processes.
Concentrated acid saccharification is the most extensively studied cellulose hydrolysis process. This process is conducted at relatively mild temperature and can lead to nearly theoretical yield of sugars. In this process, cellulose in lignocellulosic materials is first swollen at room temperature with concentrated acid (typically sulfuric acid), and then the swollen cellulose is hydrolyzed in diluted acid at elevated temperature (50˜120° C.)[3]. However, acid corrosion of equipment and the difficulty in recycling concentrated sulfuric acid have restricted the development of this technology. Although ion exclusion chromatography can be used to separate sugars and sulfuric acid, the method is costly and energy-intensive. In addition, the acid is extensively diluted during the sugar-acid separation, and of the recovered sulfuric acid has to be reconcentrated to 70%˜80% prior to reuse.[4]
In order to avoid the use of concentrated acid, a saccharification method using diluted acid at higher temperatures (160˜190° C.) was developed. Unfortunately, the dilute acid process only gives a sugar yield of about 50% because of incomplete hydrolysis of cellulose and sugar degradation at high temperature. Additionally, the sugar degradation products, such as furfural, hydroxymethylfurfural (HMF), and levulinic acid, can inhibit the fermentation of the sugars, for example, to produce ethanol. In order to reduce the degradation of sugars, in particular of pentoses, a two-stage process was developed. In a first stage, hemicellulose was first extracted at moderate temperature; and in a second stage, temperature was elevated to hydrolyze cellulose into glucose. Even so, the total yield of sugars was only 60˜70%, depending on feedstock and processing conditions[3b, 5]. Further, the need to employ a two-stage process adds to complexity and cost.
In summary, problems encountered with acid processes include low sugar yield due to the incomplete hydrolysis of cellulose and undesirable degradation of the sugars, formation of fermentation inhibitors (furfural, HMF, and levulinic acid etc.), extensively condensed lignin (which limits the coproducts potential of the lignin), equipment corrosion, acid recovery, and wastewater treatment.
The enzymatic saccharification of lignocellulose using cellulose and hemicellulose hydrolytic enzymes is another popular method used to break down cellulose and hemicellulose into monosaccharides. Enzymatic saccharification itself is inexpensive and less hazardous than acid hydrolysis because of the use of mild process conditions (˜50° C. and pH 4-5). However, enzymatic saccharification of lignocellulosic biomass is economically less attractive which limits its commercialization. A major obstacle to successful commercialization of enzymatic saccharification is the unavailability of high-activity and low-cost enzymes (both cellulases and hemicellulases). Although significant progress has been made in recent decades in improving enzyme activity and reducing enzyme production cost, enzyme is still a considerable contributor to the high cost of the sugars from lignocellulosic biomass[6]. Additionally, because of the natural recalcitrance of lignocellulosic biomass to the enzymes, enzymatic saccharification of untreated raw biomass is very difficult and very slow. In order to achieve a satisfactory level of cellulose hydrolysis, an energy- and cost-intensive pretreatment operation is required. Such pretreatment functions to remove lignin and/or hemicellulose to expose cellulose. Pretreatment can result in destruction of the physical matrix by mechanically grinding or milling to reduce particle size (and thereby increasing accessible surface area to enzymes), enhancing cellulose hydrolysis by decrystallization and depolymerization, or combinations thereof. Representative pretreatment technologies include, for example, acid treatment (e.g., with diluted acid, concentrated phosphoric acid, etc.); the organosolv process (e.g., U.S. Pat. No. 3,585,104), ammonia fiber expansion (AFEX), treatment with ionic liquid, treatment with alkali, and sulfite processes[7]. However, due to technical and/or economic barriers, none of these technologies has as yet commercially succeeded. In addition, unlike chemical reaction, enzymatic hydrolysis is a time-consuming process and typically takes days to complete. Finally, since high consistency (substrate solid content) hydrolysis is an engineering challenge, enzymatic hydrolysis typically generates a dilute (5-10%, w/w) sugar stream.
Recently, direct hydrolysis of lignocellulosic biomass in ionic liquid has been reported from pure cellulose and real biomass, such as untreated corn stover, wheat and rice straws, and wood powder[8, 9]. The use of ionic liquids can be problematic due to the generally higher cost of these materials and to the complexity that can be encountered in separation of the ionic liquids from products and the recycling of ionic liquids.
U.S. Pat. No. 4,018,620 (Penque) relates to a method of hydrolyzing cellulose to mono saccharides by treating cellulose with aqueous CaCl2 and acid, using 55% calcium chloride in the presence of acid to hydrolyze newsprint (newspaper). An overall saccharification yield of 50% was reported, but cellulose was only hydrolyzed by 20%[10c]. Because of its capability of swelling and dissolving cellulose, ZnCl2 is widely used in cellulose solvent systems[11]. A two-step process was reported to hydrolyze cellulose with ZnCl2, swelling and dissolving cellulose at high ZnCl2 concentration followed by hydrolyzing cellulose to glucose at diluted ZnCl2 in the presence of acid[10d]. It was reported that over 90% of pure cellulose could be saccharified to glucose with the process. However, the process was less effective when applied to real lignocellulosic biomass where an overall saccharification yield of polysaccharides (cellulose and hemicellulose) was 60˜70%, but that of cellulose was only 30˜50%.
U.S. Pat. Nos. 4,713,118 and 4,787,939 relate to a process for modification, solubilization and/or hydrolysis of a glycosidically linked carbohydrate having reducing groups. The process employs a mixture of water, an inorganic acid and a halide of lithium, magnesium or calcium.
While processes are known in the art for hydrolyzing lignocellulosic materials there is still a significant need in the art for efficient and low-cost processes which provide hydrolysis of lignocellulosic materials, particularly wood-based materials that are hard to hydrolyze, predominantly to monosaccharides, with minimal loss to undesired coproducts and preferably without the need for pretreatment of lignocellulosic materials.

Saccharification of lignocellulosic biomass


Rotation angle sensor, in particular for an electrical steering system of an industrial truck, in which two magnetic field sensitive sensor elements are arranged on orthogonal axes and a permanent magnet is attached to a shaft extending through the axis intersection point and the output signals X, Y of the sensor elements are given to an evaluation unit, which determines from the two output signals X, Y the rotation angle value by means of a function saved in the evaluation unit, characterized in that for a plurality of predetermined values of one of the output signals X or Y associated ideal values calculated from the geometrical relationship of the sensors of the other output signal Y, X are saved in the evaluation unit, the measured values of the other output signal Y, X are compared with the ideal values and a warning or stop signal is created if the difference between the measured and ideal value reaches a predetermined amount.

It is known to provide industrial trucks and other vehicles with an electrical steering system. The rotation of a steering transmitter is measured with the help of a rotation angle sensor and the rotation angle signal is given to an actuator, which depending on the measured rotation angle creates a steering angle for a wheel to be steered. For these types of electrical steering systems as well as for other applications, the security in the angle capture is of importance. A failure of the electrical steering system or a wrong angle display can have uncomfortable consequences if not detected in a timely manner.
It is known to determine a rotation angle with the help of an electrical potentiometer. It is also known to determine an angle of rotation in that two magnetic field sensitive orthogonally arranged sensor elements, e.g. hall sensors, work together with one permanent magnet, which is e.g. arranged on the shaft of the steering transmitter. The sensor elements create sinusoidal output signals depending on the rotary motion of the magnet [X=A·cos(Θ)+B und Y=A·sin(Θ)+B]. With the help of a formula saved in an evaluation unit, e.g. Θ=α tan 2(Y−B, X−B), a rotation angle is calculated in a processor and processed further. The rotation angle can be determined relatively exactly with this type of rotation angle sensor. It is disadvantageous that errors, which are caused by the failure of a sensor element, e.g. due to a wire break or the appearance of impermissible drift phenomena, such as static external magnetic fields, are not detected right away under some circumstances.
The object of the invention is to create a rotation angle sensor, in particular for electrical steering systems for industrial trucks, which is monitored for failures.


Compounds of the formula I

The invention relates to novel sulfonylaminophosphinic and sulphonylaminophosphonic acid derivatives, processes for their preparation and use thereof as pharmaceuticals.
The present application claims priority under 35 U.S.C. xc2xa7 119 to German applications No. 19831980.0 filed Jul. 16, 1998, and No. 19921680.0 filed May 12, 1999. Both priority applications are entirely incorporated herein by reference.
The applications EP 0 606 046, WO 95/35276 and WO 96/27583 describe arylsulfonamidohydroxamic acids and their action as matrix metalloproteinase inhibitors. Specific arylsulfonamidocarboxylic acids are used as intermediates for the preparation of thrombin inhibitors (EP 0 468 231) and aldose reductase inhibitors (EP 0 305 947). The application EP 0 757 037 also describes the action of sulfonylaminocarboxylic acid derivatives as metalloproteinase inhibitors. The arylsulfonyl group has furthermore proved to be an effective protective group of the amino function of xcex1-aminocarboxylic acids. R. Roemmele, H. Rapoport, 53 J. ORG. CHEM. 2367 (1988).
In the attempt to find efficacious compounds for the treatment of connective tissue disorders, it has now been found that the sulfonylaminophosphinic and -phosphonic acid derivatives according to the invention are strong inhibitors of metalloproteinases. Particular value is placed here on the inhibition of stromelysin (matrix metalloproteinase 3, xe2x80x9cMMP-3xe2x80x9d), of neutrophil collagenase (xe2x80x9cMMP-8xe2x80x9d) and of aggrecanase, since these enzymes are involved to a considerable extent in the degradation of proteoglycans, as important constituents of the cartilaginous tissue. A. J. Fosang et al., 98 J. CLIN. INVEST. 2292 (1996).
The pathological loss of aggrecan, the main proteoglycan of the cartilage, includes proteolytic cleavages in its interglobular domain. Amino acid sequence analyses of proteoglycan metabolites, isolated from the synovial fluid of patients who are suffering from injury to a joint, from osteoarthrosis or from an inflammatory joint condition, showed that a proteolytic cleavage preferably takes place between the amino acids Glu373 and Ala374 in the interglobular domain of human aggrecan. Lohmander et al., 36 ARTHRITIS RHEUM. 1214 (1993). Until now, it was not yet possible to identify the proteolytic activity which is responsible for this cleavage. It is designated as xe2x80x9caggrecanasexe2x80x9d and can be included in the metalloproteinases family.
The detection of the expression of MT1-MMP in human cartilaginous tissue for the first time (Bxc3xcttner et al., 40 ARTHRITIS RHEUM. 704 (1997)), combined with the proof that the catalytic domain of this enzyme cleaves at the xe2x80x9caggrecanasexe2x80x9d cleavage site in the recombinant aggrecan fusion protein rAgg1mut (Bxc3xcttner et al., 333 BIOCHEM. J. 159 (1998)), led to the testing of the strong matrix metalloproteinase inhibitors described here with respect to their action against an xe2x80x9caggrecanasexe2x80x9d activity. It was possible here to show using various assay systems that the sulfonylaminophosphinic and -phosphonic acid derivatives are also strong inhibitors for the xe2x80x9caggrecanasexe2x80x9d activity.
The invention therefore relates to the compounds of the formula I
stereoisomeric forms thereof, and physiologically tolerable salts thereof, where
(A.) R1 is
1. phenyl;
2. phenyl, which is mono- or disubstituted by
2.1. (C1-C6)-alkyl,
2.2. hydroxyl,
2.3. (C1-C6)-alkyl-C(O)xe2x80x94Oxe2x80x94,
2.4. (C1-C6)-alkyl-Oxe2x80x94,
2.5. (C1-C6)-alkyl-Oxe2x80x94(C1-C4)-alkyl-Oxe2x80x94,
2.6. halogen,
2.7. xe2x80x94CF3,
2.8. xe2x80x94CN,
2.9. xe2x80x94NO2,
2.10. HOxe2x80x94C(O)xe2x80x94,
2.11. (C1-C6)-alkyl-Oxe2x80x94C(O)xe2x80x94,
2.12. methylenedioxo,
2.13. R4xe2x80x94(R5)Nxe2x80x94C(O)xe2x80x94,
2.14. R4xe2x80x94(R5)Nxe2x80x94, or
2.15 a heteroaromatic described under A.3.1 to A.3.16;
3. a heteroaromatic described under A.3.1 to A.3.16, which is unsubstituted or substituted by one or more radicals described under A.2.1 to A.2.15,
3.1. pyrrole,
3.2. pyrazole,
3.3. imidazole,
3.4. triazole,
3.5. thiophene,
3.6. thiazole,
3.7. oxazole,
3.8. isoxazole,
3.9. pyridine,
3.10. pyrimidine,
3.11. pyrrolidine,
3.12. indole,
3.13. benzothiophene,
3.14. benzimidazole,
3.15. benzoxazole, or
3.16. benzothiazole; or
4. xe2x80x94Oxe2x80x94(C1-C6)-alkyl;
(B.) R2, R4 and R5 independently of one another are identical or different and are
1. a hydrogen atom;
2. (C1-C6)-alkyl-;
3. HOxe2x80x94C(O)xe2x80x94(C1-C6)-alkyl-;
4. phenyl- (CH2)nxe2x80x94, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, or is substituted by xe2x80x94NHxe2x80x94C(O)xe2x80x94(C1-C3)-alkyl, and n is the integer zero, 1, or 2;
5. picolyl; or
6. R4 and R5, together with the nitrogen to which they are bonded, form a 4- to 7-membered ring, and the ring is unsubstituted, or a carbon atom in the ring is replaced by xe2x80x94Oxe2x80x94, xe2x80x94Sxe2x80x94, or xe2x80x94NHxe2x80x94, or two adjacent carbon atoms of the 4- to 7-membered ring are part of a benzyl radical;
(C.) R and R3 are identical or different and are
1. a hydrogen atom;
2. (C1-C10)-alkyl-, in which alkyl is unsubstituted or monosubstituted by xe2x80x94OH;
3. (C2-C10)-alkenyl-, in which alkenyl is linear or branched;
4. R2xe2x80x94Oxe2x80x94(C1-C6)-alkyl-;
5. R2xe2x80x94S(O)nxe2x80x94(C1-C6)-alkyl-, where n is the integer zero, 1, or 2;
6. R2xe2x80x94S(O)(xe2x95x90NH)xe2x80x94(C1-C6)-alkyl-;
7. a radical of formula IIo
in which n is the integer zero, 1, or 2, and W is a nitrogen, oxygen, or sulfur atom;
8. phenyl-(CH2)mxe2x80x94, in which m is the integer zero, 1, 2, 3, 4, 5, or 6, wherein the xe2x80x94(CH2)mxe2x80x94 chain is unsubstituted or monosubstituted by xe2x80x94OH, and wherein phenyl is unsubstituted or mono- or disubstituted by
8.1 radicals described under A.2.1 to A.2.15,
8.2 xe2x80x94Oxe2x80x94(CH2)m-phenyl, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and m is the integer zero, 1, 2, 3, 4, 5, or 6,
8.3 xe2x80x94C(O)xe2x80x94(CH2)m-phenyl, in which phenyl is defined under C.8.2;
9. heteroaryl-(CH2)mxe2x80x94, in which heteroaryl is defined under A.3.1 to A.3.16, m is defined under C.8, the xe2x80x94(CH2)mxe2x80x94 chain is unsubstituted or monosubstituted by xe2x80x94OH, and heteroaryl is unsubstituted or mono- or disubstituted by
9.1 radicals described under A.2.1 to A.2.15,
9.2 xe2x80x94CH(O),
9.3 xe2x80x94SO2-phenyl, in which phenyl is unsubstituted or substituted as defined under C.8.2 or C.8.3,
9.4 xe2x80x94Oxe2x80x94(CH2)m-phenyl;
10. xe2x80x94(CH2)mxe2x80x94P(O)(OH)xe2x80x94(C1-C3)-alkyl, in which m is defined under C.8;
11. a characteristic radical of an amino acid;
12. R6xe2x80x94C(O)xe2x80x94(C0C6)-alkyl- in which R6 is
12.1. a hydrogen atom,
12.2. (C1-C6)-alkyl-,
12.3. phenyl, which is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15,
12.4. heteroaryl, which is defined under A.3.1 to A.3.16, and is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15, or is substituted by xe2x80x94(C1-C4)-alkyl-COOH,
12.5. xe2x80x94OH,
12.6. xe2x80x94OR2, in which R2 has the meaning described under B.1 to B.6,
12.7. xe2x80x94NR4xe2x80x94(R5), in which R4 and R5 are defined under B.1 to B.6,
12.8. heteroaryl-(CH2)mxe2x80x94NHxe2x80x94, in which heteroaryl is defined under A.3.1 to A.3.16, and is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15, and m is defined under C.8,
12.9. R4xe2x80x94(R5)Nxe2x80x94NHxe2x80x94, in which R4 and R5 are defined under B.1 to B.6,
12.10. HOxe2x80x94C(O)xe2x80x94CH(R3)xe2x80x94NHxe2x80x94, in which R3 is defined under C.1 to C.11;
13. xe2x80x94(CH2)pxe2x80x94N(R9)(R10), in which p is an integer zero, 1, 2, 3, or 4, in which R9 and R10 are identical or different and are
13.1. a hydrogen atom,
13.2. phenyl-(CH2)mxe2x80x94, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and m is the integer zero, 1, 2, or 3,
13.3. Rxxe2x80x94C(O)xe2x80x94, in which Rx is
3.1 (C1-C6)-alkyl-,
3.2 (C2-C6)-alkenyl-,
3.3 phenyl-(CH2)mxe2x80x94, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and m is the integer zero, 1, 2, or 3, or
3.4 heteroaryl-(CH2)mxe2x80x94, in which heteroaryl is defined under A.3.1 to A.3.16,
13.4. Rxxe2x80x94Oxe2x80x94C(O)xe2x80x94, in which Rx is defined under C.13.3,
13.5. Rxxe2x80x94CH(NH2)xe2x80x94C(O)xe2x80x94, in which Rx is defined under C.13.3,
13.6. R8xe2x80x94N(R7)xe2x80x94C(O)xe2x80x94, in which R8 is
6.1 a hydrogen atom
6.2 (C1-C6)-alkyl-,
6.3 phenyl-(CH2)m, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and m is the integer zero, 1, 2, or 3, or
6.4 heteroaryl-(CH2)m, in which heteroaryl is defined under A.3.1 to A.3.16, and is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15, m is the integer zero, 1, 2, or 3, and in which R7 is a hydrogen atom or (C1-C6)-alkyl-, or in which R7 and R8, together with the nitrogen atom to which they are bonded, form a 4- to 7-membered ring, and the ring is unsubstituted or a carbon atom in the ring is replaced by xe2x80x94Oxe2x80x94, xe2x80x94Sxe2x80x94, or xe2x80x94NHxe2x80x94,
13.7. Rxxe2x80x94SO2xe2x80x94, in which Rx is defined under C.13.3,
13.8. Rxxe2x80x94NHxe2x80x94C(xe2x95x90NR7)xe2x80x94, in which Rx is defined under C.13.3 and R7 is defined under C.13.6.4, or Rx and R7 are
8.1 (C1-C6)-alkyl-C(O)xe2x80x94,
8.2 xe2x80x94NO2 or
8.3 xe2x80x94SO2xe2x80x94(CH2)q-phenyl, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and q is the integer zero, 1, 2, or 3,
13.9. xe2x80x94SO2xe2x80x94(CH2)q-phenylxe2x80x94phenyl, in which each phenyl independently is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15, and q is the integer zero, 1, 2, or 3, or
13.10. a radical of formula IIp
in which m is the integer zero, 1, 2, or 3, and W is a nitrogen atom or sulfur atom, or
R9 and R10, together with the nitrogen atom to which they are bonded, form a ring chosen from radicals of the subformulae IIa to IIn,
where r is the integer 1 or 2, R11 is a radical described under A.2.1 to A.2.15, R7 is defined under C.13.6.4, and m is defined under C.13.2, and a carbon atom in the ring is replaced by zero or one heterospecies chosen from oxygen, sulfur, or nitrogen atom which is unsubstituted or monosubstituted with R2;
14. xe2x80x94OH;
15. xe2x95x90O;
16. (C1-C6)-alkyl-; or
in the compound of formula I, a xe2x80x94C(R)(R3)xe2x80x94 radical is optionally replaced by xe2x80x94NHxe2x80x94 or xe2x80x94NR2xe2x80x94 in which R2 is defined under B.1 to B.6;
(D.) t is an integer 1, 2, 3, or 4;
(E.) R2 and R3 together form a ring with an exocyclic phosphinic or phosphonic acid radical of the subformula II
in which r is the integer zero, 1, 2, or 3, and one carbon atom in the ring of the radical of subformula II is replaced by zero or one heterospecies chosen from xe2x80x94Oxe2x80x94, xe2x80x94Sxe2x80x94, or xe2x80x94(R7)Nxe2x80x94, in which R7 is
1. a hydrogen atom;
2. (C1-C6)-alkyl;
3. phenyl, in which phenyl is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15;
4. benzyl, in which benzyl is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15; or
5. R2Nxe2x80x94C(xe2x95x90NH)xe2x80x94 where R2 has the meaning described under B.1 to B.6, and the carbon atoms in the ring of the subformula II are unsubstituted or mono- or polysubstituted by (C1-C6)-alkyl-, phenyl-, phenyl-(CH2)mxe2x80x94 or HOxe2x80x94, or combinations thereof;
(F.) U is xe2x80x94SO2xe2x80x94 or xe2x80x94COxe2x80x94;
(G.) Y1 and Y2 are identical or different and independently of one another are
a) a hydrogen atom;
b) xe2x80x94OH;
c) xe2x80x94(C1-C4)-alkyl, in which alkyl is linear or branched;
d) xe2x80x94(CH2)u-phenyl, in which u is zero or 1;
e) xe2x80x94Oxe2x80x94(C1-C4)-alkyl, in which alkyl is linear or branched; or
f) xe2x80x94Oxe2x80x94(CH2)s-phenyl, in which s is zero or 1;
(H.) A is
a) a covalent bond;
b) xe2x80x94Oxe2x80x94;
c) xe2x80x94CHxe2x95x90CHxe2x80x94; or
d) xe2x80x94Cxe2x89xa1Cxe2x80x94;
(I.) B is
a) xe2x80x94(CH2)mxe2x80x94, in which m is defined under C.13.2;
b) xe2x80x94Oxe2x80x94(CH2)p, in which p is an integer from 1 to 5; or
c) xe2x80x94CHxe2x95x90CHxe2x80x94; and
(J.) X is xe2x80x94CHxe2x95x90CHxe2x80x94, an oxygen atom, or a sulfur atom.
A preferred compound of the formula I is one where
R1 is
1. phenyl;
2. phenyl which is monosubstituted by
2.1. (C1-C5)-alkyl-,
2.2. xe2x80x94OH,
2.3. xe2x80x94C(O)xe2x80x94OH,
2.4. xe2x80x94Oxe2x80x94(C1-C6)-alkyl,
2.5. pyrrolidone,
2.6. halogen, or
2.7. xe2x80x94CF3; or
3. xe2x80x94Oxe2x80x94(C1-C6)-alkyl;
R2, R4 and R5 are identical or different and are a hydrogen atom or (C1-C6)-alkyl-;
R is a hydrogen atom;
R3 is
1. (C1-C6)-alkyl-, in which alkyl is unsubstituted or monosubstituted by xe2x80x94OH,
2. R2xe2x80x94S(O)nxe2x80x94(C1-C6)-alkyl-, in which R2 is (C1-C6)-alkyl- or phenyl-(CH2)nxe2x80x94, and n is the integer zero or 1;
3. xe2x80x94(CH2)m-phenyl, in which phenyl is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15 in the original definition of the compound of formula I, the xe2x80x94(CH2)mxe2x80x94 chain is unsubstituted or monosubstituted by xe2x80x94OH, and m is the integer 1, 2, 3, 4, or 5;
4. xe2x80x94(CH2)m-heteroaryl, in which heteroaryl has the meaning mentioned under A.3.3, A.3.5, A.3.6, A.3.9, or A.3.11 in the original definition of the compound of formula I, and is unsubstituted or substituted with one or more radicals described under A.2.1 to A.2.15 in the original definition of the compound of formula I, the xe2x80x94(CH2)mxe2x80x94 chain is unsubstituted or monosubstituted by xe2x80x94OH, and m is the integer 1, 2, 3, or 4;
5. a characteristic radical of an amino acid;
6. xe2x80x94(CH2)pxe2x80x94N(R9)(R10), in which p is the integer zero, 1, or 2 in which R9 and R10 are identical or different and are a hydrogen atom or xe2x80x94SO2xe2x80x94(CH2)q-phenylxe2x80x94phenyl, in which each phenyl independently is unsubstituted or mono- or disubstituted with radicals described under A.2.1 to A.2.15 in the original definition of the compound of formula I, and q is the integer zero, 1, 2, or 3; or
7. R6xe2x80x94C(O)xe2x80x94, in which R6 is
7.1. xe2x80x94OH,
7.2. R2Oxe2x80x94, in which R2 is defined under B.1 to B.6 in the original definition of the compound of formula I, or
7.3. R4xe2x80x94(R5)Nxe2x80x94, in which R4 and R5 are defined under B.1 to B.6 in the original definition of the compound of formula I;
8. a hydrogen atom;
9. xe2x80x94OH;
10. xe2x95x90O; or
11. (C1-C6)-alkyl-; or
in the compound of formula I, a xe2x80x94C(R)(R3)xe2x80x94 radical is optionally replaced by xe2x80x94NHxe2x80x94 or xe2x80x94NR2xe2x80x94, in which R2 is defined under B.1 to B.6 in the original definition of the compound of formula I; and
t is an integer 1, 2, 3, or 4;
U is xe2x80x94SO2xe2x80x94;
Y1 is xe2x80x94OH;
Y2 is
a) xe2x80x94Oxe2x80x94(C1-C4)-alkyl, in which alkyl is linear or branched,
b) xe2x80x94OH, or
c) xe2x80x94(C1-C4)-alkyl, in which alkyl is linear or branched;
A is a covalent bond or xe2x80x94Oxe2x80x94;
B is a covalent bond or xe2x80x94(C1-C4)-alkyl; and
X is xe2x80x94CHxe2x95x90CHxe2x80x94.
A particularly preferred compound of the formula I is one where
R1 is phenyl which is monosubstituted by halogen;
R2 is a hydrogen atom;
R is a hydrogen atom;
R3 is
1. (C1-C4)-alkyl-;
2. -phenyl, in which phenyl is unsubstituted or mono- or disubstituted by xe2x80x94CF3 or xe2x80x94COOH;
3. a hydrogen atom;
4. xe2x80x94OH; or
5. xe2x80x94NHxe2x80x94SO2-phenylxe2x80x94phenyl, in which each phenyl independently is unsubstituted or substituted by one ore more identical or different halogen atoms;
t is an integer 1, 2, 3, or 4;
U is xe2x80x94SO2xe2x80x94;
Y1 and Y2 are identical or different and are xe2x80x94OH or xe2x80x94Oxe2x80x94CH3;
A is a covalent bond;
B is a covalent bond or xe2x80x94(CH2)oxe2x80x94, in which o is 1, 2, or 3; and
X is CHxe2x95x90CHxe2x80x94.
Particularly preferred compounds are (R)- [1-(4xe2x80x2-chlorobiphenyl-4-sulfonyl-amino)-2-methylpropyl]phosphonic acid, dimethyl [3-(4xe2x80x2-chlorobiphenyl-4-sulfonylamino)-1-hydroxy-3-(4-trifluoromethylphenyl)propyl]phosphonate, [1-(4xe2x80x2-chlorobiphenyl4-sulfonylamino)-3-methylbutyl]phosphonic acid, stereoisomeric forms thereof, and physiologically tolerable salts of any of the foregoing.
The expression xe2x80x9cR4 and R5 together with the ring amino group form a 4- to 7-membered ring and/or one of the carbon atoms is replaced by xe2x80x94Oxe2x80x94, xe2x80x94Sxe2x80x94 or xe2x80x94NHxe2x80x94xe2x80x9d is understood as meaning radicals which are derived, for example, from azetidine, pyrrole, pyrroline, pyridine, azepine, piperidine, oxazole, isoxazole, imidazole, indoline, pyrazole, thiazole, isothiazole, diazepine, thiomorpholine, pyrimidine or pyrazine. The term xe2x80x9chalogenxe2x80x9d is understood as meaning fluorine, chlorine, bromine or iodine. The term xe2x80x9calkylxe2x80x9d or xe2x80x9calkenylxe2x80x9d is understood as meaning hydrocarbon radicals whose hydrocarbon chains are linear, branched, or cyclic, unless otherwise indicated. Cyclic alkyl radicals are, for example, 3- to 6-membered monocyclic systems such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl. The alkenyl radicals can furthermore also contain a number of double bonds.
When a radical is multisubstituted with other radicals, said other radicals are understood to be independently chosen, being identical or different from each other. For example, in the phrase xe2x80x9ca heteroaromatic . . . which is unsubstituted or substituted by one or more radicals described under A.2.1 to A. 2.15,xe2x80x9d it is intended that said radicals may be mixed and matched, with the identity of one radical having no bearing on the identity of another. Similarly, when a radical is disubstituted with other radicals, said other radicals are identical or different.
The general structural formula of xcex1-amino acids is as follows:
The xcex1-amino acids differ from one another by the radical R, which in the context of the present application is designated as a xe2x80x9ccharacteristic radicalxe2x80x9d of an amino acid.
The starting substances for the chemical reactions are known or can be easily prepared by methods known from the literature. The aminophosphinic and -phosphonic acids used as starting substances for the synthesis of the compounds according to the invention are, if not commerically obtainable in the individual case, synthesizable according to known methods (R. S. Rogers, M. K. Stern, SYNLETT, 708 (1992); P. P. Giannousis, P. A. Bartlett, 30 J. MED. CHEM. 1603 (1987); J. P. Genet, M. Uziel, A. M. Touzin, S. Roland, S. Thorimbert, S. Tanier, 33 TETRAHEDRON LETT. 77 (1992); E. K. Baylis, C. D. Campbell, J. G. Dingwall, 1 J. CHEM. SOC. PERKIN TRANS. 2845 (1984)).
The invention furthermore relates to a process for the preparation of the compounds of the formula I and/or a stereoisomeric form of the compounds of the formula I and/or of a physiologically tolerable salt of the compounds of the formula I, which comprises
a) reacting an aminophosphinic or -phosphonic acid of the formula III
in which R2, Y1, Y2, R, and R3 are as defined in formula I, with a sulfonic acid or carbonyl derivative of the formula IV
in which R1, A, X, U, and B are as defined in formula I and Z is a halogen atom, imidazolyl or xe2x80x94OR8, in which R8 is a hydrogen atom, (C1-C6)-alkyl, phenyl or benzyl, wherein said alkyl, phenyl, or benzyl is independently unsubstituted or substituted, in the presence of a base or optionally of a dehydrating agent to give a compound of the formula I, or
b) reacting an aminophosphinic or -phosphonic acid ester of the formula (V)
in which R2, R3, t, Y2 and R8 have the abovementioned meaning, with a sulfonic acid or carbonyl derivative of the formula IV to give a compound of the formula VI
and converting the compound of the formula VI with removal of the radical R8, preferably in the presence of a base or acid, into a compound of the formula I, or
c) reacting the compound of the formula VII
where n is the integer zero, 1 or 2, with the aid of a protective group E to give a compound of the formula VIII
and converting the compound of the formula VIII, using a compound of the formula IV into a compound of the formula IX
and then converting the compound of the formula IX, with removal of the protective group E and of the radical R8 with the aid of suitable cleavage reagents, into the compound of the formula I, or
d) separating a compound of the formula I prepared by one of the processes a), b) or c), which on account of its chemical structure occurs in enantiomeric forms, into the pure enantiomers by salt formation with enantiomerically pure acids or bases, chromatography on chiral stationary phases or derivatization by means of chiral enantiomerically pure compounds such as amino acids, separation of the diastereomers thus obtained, and removal of the chiral auxiliary groups, or
e) isolating the compound of the formula I prepared by one of the processes a), b), c) or d) either in free form or, in the case of the presence of acidic or basic groups, converting it into physiologically tolerable salts.
Suitable protective groups E used for this are preferably the N-protective groups customary in peptide chemistry, for example protective groups of the urethane type, benzyloxycarbonyl (Z), t-butoxycarbonyl (xe2x80x9cBocxe2x80x9d), 9-fluorenylmethoxycarbonyl (xe2x80x9cFmocxe2x80x9d), allyloxycarbonyl (xe2x80x9cAlocxe2x80x9d) or of the acid amide type, in particular formyl, acetyl or trifluoroacetyl, and of the alkyl type, for example benzyl.
Compounds of the formula III employed, in which R2 is a hydrogen atom and R3 is the characteristic radical of an amino acid, are preferably the characteristic radicals of the following naturally occurring xcex1-amino acids: glycine, alanine, valine, leucine, isoleucine, phenylalanine, tyrosine, tryptophan, serine, threonine, cysteine, methionine, asparagine, glutamine, lysine, histidine, arginine, glutamic acid and aspartic acid. Compounds of the formula III employed, in which R2 is a hydrogen atom and R3 is the characteristic radical of an amino acid, are preferably the characteristic radicals, for example, of the following non-naturally occurring amino acids: 2-aminoadipic acid, 2-aminobutyric acid, 2,4-diaminobutyric acid, 2-aminoisobutyric acid, 2,3-diaminopropionic acid, 1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, 2-amino-pimelic acid, phenylglycine, 3-(2-thienyl)alanine, 3-(3-thienyl)alanine, 2-(2-thienyl)glycine, 2-aminoheptanoic acid, pipecolic acid, hydroxylysine, sarcosine, N-methylisoleucine, 6-N-methyllysine, N-methylvaline, norvaline, norleucine, omithine, alloisoleucine, allothreonine, 4-hydroxyproline, 3-hydroxyproline, allohydroxylysine, 3-(2-naphthyl)alanine, 3-(1-naphthylalanine), homophenylalanine, homocysteine, homocysteic acid, homotryptophan, cysteic acid, 3-(2-pyridyl)alanine, 3-(3-pyridyl)alanine, 3-(4-pyridyl)alanine, citrulline, phosphinothricin, 4-fluorophenylalanine, 3-fluorophenylalanine, 2-fluorophenylalanine, 4-chlorophenylalanine, 4-nitrophenylalanine, 4-aminophenylalanine, cyclohexylalanine, 5-fluorotryptophan, 5-methoxytryptophan, methionine sulfone, methionine sulfoxide or NH2xe2x80x94NHxe2x80x94CONH2, if appropriate substituted. In the case of naturally but also of non-naturally occurring amino acids which have a functional group such as amino, hydroxyl, carboxyl, mercapto, guanidyl, imidazolyl or indolyl in the side chain R3, this group can also be protected.
If there is an imidazole radical in R3, the sulfonic acid derivative of the formula IV employed for the sulfonamide formation, for example, serves as a protective group for the imidazole nitrogen, which can be removed again, in particular in the presence of bases such as sodium hydroxide solution.
To prepare compounds of the formula I in which R2 and R3 together form a ring of the substructure II, the starting substances of the formula III utilized are, for example, 2-methylpropylphosphonic acid, piperidine-2-phosphonic acid, piperazine-2-phosphonic acid or hexahydropyridazine-3-phosphonic acid, it being possible, in particular, for the nitrogen in the 4-position of the piperazine-2-phosphonic acid to be substituted by a protective group Z, for example benzyloxycarbonyl or tert-butoxycarbonyl as described in process variant c) or by a radical R7.
Starting materials used for the preparation of the sulfonic acid derivatives of the formula IV are preferably sulfonic acids or their salts of the formula X, for example
where R9 is a radical described under 2.1. to 2.15.
For the preparation of the arylsulfonic acids of the formulae Xa and b, the sulfonation process using concentrated sulfuric acid described in Houben-Weyl, METHODEN DER ORGANISCHEN CHEMIE [METHODS OF ORGANIC CHEMISTRY] Volume 9, pp. 450-546 is preferably used, if appropriate in the presence of a catalyst, sulfur trioxide and its addition compounds or halosulfonic acids, such as chlorosulfonic acid. Particularly in the case of the diphenyl ethers of the formula Xb, the use of concentrated sulfuric acid and acetic anhydride as a solvent (cf. C. M. Suter, 53 J. AM. CHEM. SOC. 1114 (1931)), or the reaction with excess chlorosulfonic acid (J. P. Bassin, R. Cremlyn and F. Swinbourne, 72 PHOSPHORUS, SULFUR AND SILICON 157 (1992)) has proven suitable. Sulfonic acids according to the formula Xc, Xd or Xe can be prepared in a manner known per se by reacting the corresponding arylalkyl halide with sulfites such as sodium sulfite or ammonium sulfite in aqueous or aqueous/alcoholic solution, it being possible to accelerate the reaction in the presence of tetraorganoammonium salts such as tetrabutylammonium chloride.
Sulfonic acid derivatives according to formula IV used are, in particular, the sulfonyl chlorides. For their preparation, the corresponding sulfonic acids, also in the form of their salts, such as sodium, ammonium or pyridinium salts, are reacted in a known manner with phosphorus pentachloride or thionyl chloride without or in the presence of a solvent such as phosphorus oxychloride or of an inert solvent such as methylene chloride, cyclohexane or chloroform, in general at reaction temperatures from 20xc2x0 C. up to the boiling point of the reaction medium used.
The reaction of the sulfonic acid derivatives of the formula IV with the aminophosphonic acids of the formulae III, V or VII according to process variants a), b) or c) proceeds advantageously in the manner of the Schotten-Baumann reaction. Suitable bases for this are particularly alkali metal hydroxides such as sodium hydroxide, but also alkali metal acetates, hydrogencarbonates, carbonates and amines. The reaction takes place in water and/or in a water-miscible or immiscible solvent such as tetrahydrofuran (xe2x80x9cTHFxe2x80x9d), acetone, dioxane or acetonitrile, the reaction in general being kept at from xe2x88x9210xc2x0 C. to 50xc2x0 C. If the reaction is carried out in an anhydrous medium, tetrahydrofuran or methylene chloride, acetonitrile or dioxane in the presence of a base, such as triethylamine, N-methylmorpholine, N-ethyl- or diisopropylethylamine, is especially used, possibly in the presence of N,N-dimethylaminopyridine as a catalyst.
In another variant, the aminocarboxylic acids of the formula III, IV or VII can first be converted into their silylated form with the aid of a silylating agent such as bistrimethylsilyltrifluoroacetamide (xe2x80x9cBSTFAxe2x80x9d) and they can then be reacted with sulfonic acid derivatives to give the compounds of the formula I.
The preparation of physiologically tolerated salts from compounds of the formula I capable of salt formation, including their stereoisomeric forms, is carried out in a manner known per se. The phosphonic or phosphinic acids form stable alkali metal, alkaline earth metal or optionally substituted ammonium salts with basic reagents such as hydroxides, carbonates, hydrogencarbonates, alcoholates and also ammonia or organic bases, for example trimethyl- or triethylamine, ethanolamine or triethanolamine or alternatively basic amino acids, for example lysine, ornithine or arginine. If the compounds of the formula I have basic groups, stable acid addition salts can also be prepared using strong acids. Both inorganic and organic acids such as hydrochloric, hydrobromic, sulfuric, phosphoric, methanesulfonic, benzenesulfonic, p-toluenesulfonic, 4-bromo-benzenesulfonic, cyclohexylamidosulfonic, trifluoromethylsulfonic, acetic, oxalic, tartaric, succinic or trifluoroacetic acid are suitable for this.
The invention also relates to pharmaceuticals comprising an efficacious amount of at least one compound of the formula I and/or of a physiologically tolerable salt of the compound of the formula I and/or an optionally stereoisomeric form of the compound of the formula I, together with a pharmaceutically suitable and physiologically tolerable excipient, additive and/or other active compounds and auxiliaries.
On account of the pharmacological properties, the compounds according to the invention are suitable for the prophylaxis and therapy of all those disorders in the course of which an increased activity of matrix-degrading enzymes such as metalloproteinases or aggrecanase is involved. These include degenerative joint disorders such as osteoarthroses, spondyloses, chondrolysis after joint trauma or relatively long joint immobilization after meniscus or patella injuries or torn ligaments. These furthermore also include disorders of the connective tissue such as collagenoses, periodontal disorders, wound healing disorders and chronic disorders of the locomotory apparatus such as inflammatory, immunologically or metabolically related acute and chronic arthritis, arthropathies, myalgias and disorders of the bone metabolism. The compounds of the formula I are furthermore suitable for the treatment of ulceration, atherosclerosis and stenoses. The compounds of the formula I are furthermore suitable for the treatment of inflammations, carcinomatous disorders, tumor metastasis formation, cachexia, anorexia and septic shock. In general, the pharmaceuticals according to the invention are administered orally or parenterally. Rectal or transdermal administration is also possible.
The invention also relates to a process for the production of a pharmaceutical, which comprises bringing at least one compound of the formula I into a suitable administration form using a pharmaceutically suitable and physiologically tolerable excipient and, if appropriate, further suitable active compounds, additives or auxiliaries.
Suitable solid or pharmaceutical preparation forms are, for example, granules, powders, coated tablets, tablets, (micro)capsules, suppositories, syrups, juices, suspensions, emulsions, drops or injectable solutions and preparations with protracted release of active compound in the production of which customary auxiliaries such as excipients, disintegrants, binding agents, coating agents, swelling agents, glidants or lubricants, flavorings, sweeteners and solubilizers are used. Frequently used auxiliaries which may be mentioned are magnesium carbonate, titanium dioxide, lactose, mannitol and other sugars, talc, lactoprotein, gelatin, starch, cellulose and its derivatives, animal and vegetable oils such as cod liver oil, sunflower, groundnut or sesame oil, polyethylene glycol and solvents such as, for example, sterile water and mono- or polyhydric alcohols such as glycerol.
The pharmaceutical preparations are preferably prepared and administered in dose units, each unit containing as active constituent a specific dose of the compound of the formula I according to the invention. In the case of solid dose units such as tablets, capsules, coated tablets or suppositories, this dose can be up to approximately 1000 mg, but preferably approximately 50 to 300 mg, and in the case of injection solutions in ampoule form up to approximately 300 mg, but preferably approximately 10 to 100 mg.
For the treatment of an adult patient weighing approximately 70 kg, depending on the efficacy of the compound according to formula I, daily doses of approximately 20 mg to 1000 mg of active compound, preferably, for example, 100 mg to 500 mg, are indicated. Under certain circumstances, however, higher or lower daily doses may also be appropriate. The daily dose can be administered both by single administration in the form of an individual dose unit or else of a number of smaller dose units and by multiple administration of subdivided doses at specific intervals.
1H-NMR spectra have been recorded on a 400 MHz apparatus from Bruker or a 200 MHz apparatus from Varian, as a rule using tetramethylsilane (xe2x80x9cTMSxe2x80x9d) as an internal standard and at room temperature (xe2x80x9cRTxe2x80x9d). The solvents used are indicated in each case. As a rule, final products are determined by mass-spectroscopic methods (FAB-, ESI-MS); the main peak is indicated in each case. Temperatures in degrees Celsius, RT means room temperature (22xc2x0 C. to 26xc2x0 C.). Abbreviations used are either explained or correspond to the customary conventions.

Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use

Abstract: Compounds of the formula I

Abstract: are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.


A reactor including a high-temperature reaction unit which causes a reaction of a first reaction material to create a second reaction material and a product, and a low-temperature reaction unit which causes a reaction of the second reaction material at a temperature lower than in the high-temperature reaction unit. A coupling pipe is interposed between the high-temperature reaction unit and the low-temperature reaction unit and transfers the first reaction material and the product created with the reaction material between the high-temperature reaction unit and the low-temperature reaction unit. An external flow pipe is joined to the low-temperature reaction unit at its having one end. The external flow pipe has a plurality of flow pathways including a flow pathway for supplying the first reaction material to the high-temperature reaction unit through the low-temperature reaction unit and a flow pathway for discharging the product from the high-temperature reaction unit through the low-temperature reaction unit.

1. Field of the Invention
The present invention relates to a reactor for reforming a liquid fuel, and more particularly to a reactor for generating hydrogen to be supplied to a fuel cell and an electronic device equipped with such a reactor.
2. Description of the Related Art
In recent years, fuel cells are being used as clean power sources having high energy conversion efficiency in, for example, motor vehicles and mobile devices. A fuel cell of this type is a device that causes an electrochemical reaction between a fuel and oxygen in the atmosphere, thereby to directly obtain electric energy from chemical energy.
While a hydrogen monomer can be used as a fuel for use in the fuel cell, a problem arises in handling the hydrogen monomer because the hydrogen monomer is a gas at the ambient temperature and pressure. Approaches also are known in which hydrogen is stored by using a hydrogen storage alloy. The approaches, however, have a problem in that the storage amount of hydrogen per unit volume is small, so that the approaches are insufficient as power-source fuel storage means of, particularly, small electronic apparatuses such as cellular electronic devices. In comparison, in reforming fuel cells of the type that generates power by using hydrogen obtainable by reforming a liquid fuel containing hydrogen atoms, such as alcohols, the fuel can easily be stored in the form of liquid, and the amount of hydrogen per unit volume of the fuel is relatively large. For using fuel cells of this type, cases take place that require a vaporizer for vaporizing the liquid fuel, a reformer for extracting hydrogen necessary for power generation by causing the reaction between the liquid fuel and high temperature water vapor, a carbon monoxide removing unit for removing carbon monoxide that is a by-product of the reforming reaction, and the like (see Jpn. Pat. Appln. KOKAI Publication No. 2002-356310, for example).
In the disclosed technique, an optimal operation temperature range of the vaporizer and/or the carbon monoxide removing unit is different from an optimal operation temperature range of the reformer, therefore making it difficult to produce temperature differences across the different temperature ranges.
Further, several pipes have to be coupled to the vaporizer, the reformer, and the carbon monoxide removing unit to perform processes, such as supply of the fuel and/or oxygen, and discharging of hydrogen. In this case, heat of the vaporizer, the reformer, and the carbon monoxide removing unit transfers as it is to the outside through the pipes, thereby causing significant heat losses.
Further, the carbon monoxide removing unit and the reformer are interconnected through the pipes or flow pathways through which the reformed fuel and the like flow. In particular, in a case where the carbon monoxide removing unit and the reformer are interconnected through the respective coupling pipes corresponding to a plurality of flow pathways, the reformer and the carbon monoxide removing unit are different from each other in the amount of expansion depending on the temperature difference. Consequently, excessive stresses may impose on connection portions, consequently leading to damage in the connection portions.

Reformer for power supply of a portable electronic device


A system for automatically cleaning swimming pools includes a unitary body having a level control subsystem for selectively moving the body to a position either proximate to the surface of the water pool or proximate to the interior surface of the containment wall, a propulsion subsystem operable to selectively propel the body in either a forward or rearward direction, and a cleaning subsystem operable in either a water surface cleaning mode for skimming or scooping or a wall surface cleaning mode for vacuuming or sweeping. The subsystems are powered by an electric source such as solar cells and/or rechargeable batteries and/or a wire extending to the unitary body from an external power source. An alternative embodiment uses separate top and bottom units tethered together by an electric conduit.

The present invention relates to a method and apparatus for automatically cleaning a swimming pool.
U.S. Pat. No. 5,985,156 describes apparatus including a unitary body having (1) a level control subsystem for selectively moving the body to a position either proximate to the surface of a water pool or proximate to the interior surface of a wall containing the water pool, (2) a propulsion subsystem operable to selectively propel the body in either a forward or rearward direction, and (3) a cleaning subsystem operable in either a water surface cleaning mode (e.g., skimming or scooping) or a wall surface cleaning mode (e.g., vacuuming or sweeping). The patent discloses that these subsystems can be powered by hydraulic, pneumatic, and electric power sources and specifically describes hydraulic embodiments powered by positive and negative water pressure.
Applicant""s parent application Ser. No. 09/440109, now U.S. Pat. No. 6/294,084.(which is incorporated herein by reference) and this CIP application describe embodiments in which one or more of the aforementioned subsystems is powered by an electric source such as solar cells and/or rechargeable batteries and/or a wire extending to the unitary body from an external (e.g., deck mounted) power source. The batteries can be charged from solar cells carried by the unitary body or via an appropriately configured docking station. The described embodiments can use either a heavier-than-water body or a lighter-than-water body. When a heavier-than-water body is used, the body in its quiescent or rest state typically sinks to a position proximate to the bottom portion of the containment wall. In an active state, the level control subsystem produces a vertical force component for lifting the body to proximate to the water surface. When a lighter-than-water body is used, the body in its quiescent state floats at a position proximate to the water surface. In an active state, the level control subsystem produces a vertical force component for causing the body to descend to proximate the wall bottom portion.
The present CIP application introduces a further system embodiment which uses separate top and bottom units tethered together by a conduit in lieu of the unitary body heretofore described. The top unit functions to clean the water surface in a manner analogous to the unitary body when operating in the water surface mode and the bottom unit functions to clean the wall surface in a manner analogous to the unitary body when operating in the wall surface mode.
In accordance with the invention, at least one of the tethered top and bottom units includes a propulsion subsystem powered by an electric source such as solar cells and/or rechargeable batteries and/or a wire extending from an external power source.
In a preferred tethered units embodiment, the top unit includes a solar cell for charging an on-board battery. The battery powers a flow generator, e.g., a motor driven propeller, which produces a water flow for propulsion and water surface cleaning. The top unit preferably supplies electric power and/or control signals via the conduit to the bottom unit for powering a flow generator for propulsion and wall surface cleaning. The top and/or bottom units preferably include containers for collecting debris.
The conduit additionally functions to physically transfer forces between the top and bottom units so that the unit being propelled can pull the other unit along. In a preferred embodiment, the units are oppositely oriented so, for example, forward propulsion of the top unit pulls the bottom unit rearwardly. Similarly, forward propulsion of the bottom unit pulls the top unit rearwardly. This preferred orientation enables the tethered pair to readily avoid getting trapped behind an obstruction in the pool.

Electric powered automatic swimming pool cleaning system


An insert-molded suture anchor has a biodegradable polymer body molded around a loop of suture. A tapered end disposed on the proximal end of the body is received into a recess in the distal end of a hand driver. Anchoring ribs are formed along the remaining length of the anchor. The suture is held securely within the anchor body during the insert molding process. The anchor is produced by placing the braided suture within an injection mold, and injecting biodegradable polymer into the mold. Using a preferred plication driver, the suture anchor can be utilized for capsular plication procedures.

1. Field of the Invention
The present invention relates to an apparatus and method for anchoring surgical suture to bone. More specifically, the present invention relates to arthroscopic apparatus and methods for anchoring suture to bone using a suture anchor having suture molded directly into the body of the suture anchor.
2. Description of the Related Art
When soft tissue tears away from bone, reattachment becomes necessary. Various fixation devices, including sutures, screws, staples, wedges, and plugs have been used in the past to secure soft tissue to bone. More recently, various types of threaded suture anchors have been developed.
Suture anchors and implants generally include a structure for attaching or securing the suture to the anchor. U.S. Pat. No. 4,632,100, for example, discloses and claims a threaded suture anchor with a complex press-fitted disc and knot structure which secures the suture to the anchor. In other suture anchors, such as those disclosed in U.S. Pat. No. 5,370,662, the suture is attached to the anchor by passing the suture through an eyelet at the back end of the anchor. Problems can arise if the structure for attaching the suture fails, allowing the suture to become detached from the anchor. Also, in some of the known devices, the suture is exposed to abrasion or cutting by sharp or rough areas along the walls of the bone canal into which the anchor is inserted.
In addition, the eyelet or, in the case of U.S. Pat. No. 4,632,100, the axial opening for receiving the disc to which the suture is knotted, is formed as part of the drive head of the known suture anchors, which weakens the drive head. Various other modifications in the drive head are often employed in connection with suture attachment. For example, recessed grooves may be formed on opposite sides of the drive head to receive and protect the suture from the abrasive areas of the suture anchor tunnel. In such cases, the drive head often is made of a larger diameter to recover the mechanical strength lost from the removal of material relating to the suture-attachment or suture-protection modification.
Accordingly, a need exists for a suture anchor or implant to which suture is secured effectively so as to prevent detachment of the suture. A need also exists for a soft tissue fixation device having a low profile configuration particularly suited for reattachment of tissue to the glenoid rim, for example.


A method for relaying a signal in a wireless communication system is provided. The method comprises receiving in at least one of a base station and a relay station information regarding a mobile station group (MSG) of a mobile station, scheduling within a given duration uplink information to be transmitted from a first mobile station and downlink information to be transmitted to at least one mobile station, wherein the first mobile station is in each of the at least one mobile station's MSG, receiving in a relay station the uplink information and the downlink information to be transmitted within the given duration, network coding the uplink information and the downlink information in the relay station, and transmitting from the relay station a network-coded packet, wherein the network-coded packet can be received by the base station and the at least one mobile station.

In a mobile communications network, a mobile station (MS) can communicate with a base station (BS) via a relay station (RS). Typically, communication from the MS to the BS takes place over an uplink (UL) channel, and communication from the BS to the MS takes place over a downlink (DL) channel. In most time-division duplex (TDD) relay communication protocols, an MS may transmit a message intended for the BS to an RS in an UL sub-frame. The RS in turn transmits the message to the BS in an RS UL sub-frame. On the other hand, a BS may transmit a message intended for the MS to the RS in a DL sub-frame. The RS then transmits the message to the MS in an RS DL sub-frame.
The above relay scheme is inefficient, because the MS or the BS will have to schedule each of the uplink or downlink transmissions handled by the RS in separate sub-frames. The transmission throughput of a network implementing such a scheme is limited due to inefficient use of bandwidth (i.e., separate channels need to be used for UL and DL of relayed messages). If network coding is applied at the RS, the bandwidth usage of a relay link can be reduced. However, the reduction may be limited if the scheduling processes of UL and DL are operated independently.
More efficient systems and methods are desirable that can overcome the above-noted shortcomings.

Message coding in a relayed communications network


A valve device for low-viscosity to high-viscosity fluids, especially for fluid plastic components of plastic mixtures consisting of one or more components, with a valve housing having a fluid inflow and a dosaging valve, which has a dosing nozzle that can optionally be closed or opened by a closing element, as well as a pressure control device which acts on the fluid in the fluid inflow.

This application claims priority of German Application Serial No. 198 48 358.9 filed Oct. 21, 1998, and PCT/DE99/07936 filed Oct. 19, 1999.
The invention relates to a valve device for low-viscosity to high-viscosity fluids, especially for fluid plastic components of plastic mixtures consisting of one or more components. The device includes a valve housing having a fluid inflow and a dosing valve. The dosing valve has a dosing nozzle that can optionally be closed or opened by a closing element, as well as a pressure control device which acts on the fluid in the fluid inflow.
Such valve devices are used particularly in the processing of plastics with mixing heads, with the help of which the different plastic components are mixed and then ejected as a processable plastic mixture through an outlet and, for example, are immediately moulded onto a part as a seal. The valve devices are arranged at the inlets of the mixing head for the individual plastic components and serve to stop the supply of a component when the dosing valve is closed. The valve devices ensure, when the dosing valve is opened, that the supplied component is introduced into the mixing head not only with a constant volume flow, but also with a previously set, constant fluid pressure.
A valve device according to the above-mentioned type is known from DE-OS 195 42 797. With this valve device, the pressure control device is formed essentially from a compression spring which is arranged in the housing. The compression spring acts on the closing element which is formed as a valve needle. The compression spring pretension can be adjusted manually by adjusting an adjusting screw from the outside of the housing. The fluid pressure exerted by the spring on the nozzle needle is in equilibrium with the fluid pressure. The fluid pressure acts on the frontal area of the nozzle needle which lies transversely to its shift direction. The pressure of the spring and the pressure exerted on the nozzle needle due to the fluid pressure are in equilibrium when operated, so that it is possible to control the fluid pressure in the fluid inflow by adjusting the spring pretension.
The ""797 device is relatively complicated with regard to the adjustment of the correct pressure ratios in the fluid inflow. The adjustment of the correct pressure ratios takes place manually from the outside of the housing. Small adjustments of the adjusting screw result in relatively large pressure changes in the fluid, as the effective frontal area at the nozzle needle, which transfers the spring force to the fluid, is small due to its design. A particular disadvantage of the known device is that an operation at a constant fluid pressure, with the volume flow supplied by a dosing pump, is only guaranteed as long as the nozzle needle maintains its relative position in the valve housing when the valve is open. If the cross section that is opened by the nozzle needle is reduced in this relative position, for example by deposits of solidified plastic components or other build-up of material, the nozzle needle has to be opened further against the force of the spring, so as to maintain the steady cross section which is necessary for the constant volume flow of the fluid. A small movement of the nozzle needle already results in a large change in the spring tension and the spring force, so that the fluid pressure increases by a large amount, even when only a small build-up of material occurs.
It is the object of the invention to avoid the aforementioned disadvantages and to design a valve device of the above-mentioned type in such a way that a constant fluid pressure can be adjusted easily. The fluid pressure is essentially independent of the position of the closing element when the dosing valve is opened, and therefore is also maintained when contaminations occur at the nozzle cross section.
This object will be solved by means of the invention in that the pressure control device consists essentially of a pneumatically pretensionable control membrane which acts on the closing element.
The use of a pneumatically or servo-pneumatically pretensionable control membrane, which replaces the compression spring used in the state of the art, allows a particularly simple pressure control of the fluid dosed by means of the device. The air pressure for changing the membrane pretension can easily be adjusted automatically. By using a suitable pressure accumulator for the compressed air which pretentions the membrane, movements of the closing element which arise from contaminations at the nozzle outlet, result in practically no or only a negligible increase of pressure of compressed air and subsequently no change of the fluid pressure. In particular, the design of the valve device according to the invention also facilitates its automatic control by means of a computer-aided adjustment or change of the air pressure acting on the control membrane.
In a preferred design of the invention, there can also be arranged a recirculation valve in the valve housing in such a way that the dosing valve is optionally opened for the supply of fluid to a processing device or the recirculation valve is opened for the return of the fluid to a storage vessel. With this configuration, the supplied fluid is either supplied to for example the mixing head by the dosing valve of the processing device, or is conveyed in the cycle back to the storage vessel by the recirculation valve. The compact unit of dosing and recirculation valve in a common housing avoids difficulties in the starting phase of the subsequent processing device, as this is always completely filled due to the circulation of fluid in the cycle, and fresh fluid is always added as soon as the dosing valve opens.
The control membrane is preferably part of a pneumatically chargeable pressure control chamber and acts on the closing element designed as a valve needle by means of a plunger which can be moved in the housing. The pressure control chamber thereby forms the pressure storage for the compressed air which acts on the fluid in the fluid inflow by means of the control membrane. The force exerted by the compressed air is transferred to the valve needle by means of the plunger essentially without friction losses. The pressure control device is preferably arranged separately from the fluid inflow by means of a shut-off membrane, whereby it is ensured that no fluid can reach the sensitive control membrane. The shut-off membrane is preferably arranged between the closing element and the plunger, so that the plunger is also separated from the fluid inflow and that its very accurate, mainly frictionless mounting in the valve housing is not adversely affected by the entry of fluid.
The plunger can be charged by the control membrane by means of a pressure pin mounted at the control membrane, which is supported at the plunger by means of a ball bearing element. The ball bearing element, which preferably consists simply of a single ball, effects an even central transfer of the forces acting between the plunger and the pressure pin essentially without friction losses, so that an exact pressure balance can take place between the air pressure at the control membrane and the fluid pressure in the fluid inflow.
The closing element is preferably pretensioned in the direction of the plunger by means of a spring which is supported in the housing. When the dosing valve is opened, the spring draws the dosing element in the dosing nozzle back at least to such an extent that the fluid pressure of the supplied fluid can act on the closing element. The closing element of the dosing valve can be moved by an actuating device for closing or opening the dosing nozzle. The actuating device consists in a particularly advantageous manner essentially of an actuating lever that can be actuated in the actuating cylinder. The actuating lever is mounted pivotally in the housing and acts on the closing element or the pressure cylinder against the spring. In particular, with the particularly advantageous design of the invention, in which the recirculation valve and the dosing valve are constructed essentially in the same way, it is possible that the dosing valve and the recirculation valve or their closing elements can be actuated by a common actuating lever.

EDF Polymer-Applikation Maschinenfabrik GmbH


The present disclosure provides a method for modifying pairs of images for improved three-dimensional displaying. The method comprises analyzing the images for detecting the angle of incidence of the illuminating light in the images, and modifying the luminance values of at least a section of at least one of the images of each pair based on the angle of incidence and anatomical details of a human face. Further, the present invention provides a respective apparatus.

Although applicable to any type of three-dimensional display, embodiments of the present disclosure will mainly be described in conjunction with three-dimensional videos.
Today, videos like, e.g., movies in cinemas or computer games may be provided as three-dimensional videos to users for example with a respective 3D-headset or 3D-glasses. The visuals may therefore represent a three-dimensional image that may also be perceived by the human brain as a three-dimensional image. For example, with a 3D-headset the human brain may receive visual information that indicates that the body of the user is moving (as shown in the three-dimensional video). However, the user's brain will not receive the corresponding information from the body's other sensors, which will usually indicate the body being seated or standing still.
This discrepancy between the provided visuals and the information provided by the other sensors leads to many users suffering from symptoms such as headache, fatigue or the like. Such symptoms may be caused by non-naturalness of the contents, i.e., by discrepancies between what a user sees via the screen and what a user's brain expects.
Usually, the information the other sensors provide to the brain may not be influenced directly, especially if the user is, e.g., sitting on a chair. However, the visuals may be adapted to minimize the adversary symptoms that may be caused.
Accordingly, there is a need for an improved display of three-dimensional movies.

Method for modifying steroscopic pairs of images and apparatus

VESTEL ELEKTRONIK SANAYI VE TICARET A.S.


An electronic document management system that takes advantage of advanced document analysis techniques. The electronic document management system may provide automatic archiving of documents and retrieval without the need to navigate through a directory structure or specify a filename. Document comparison is facilitated by automatic retrieval of a previous version of a document. A digital copier alerts a user when a document to be copies already exists electronically within a database.

The present invention relates to an electronic document management system for and more particularly to such a system that exploits advanced document analysis techniques.
Electronic creation, editing, and storage of documents has become commonplace. However, paper documents remain important and the processes of printing, faxing, and copying are still central to document distribution and management. The reasons for the continued centrality of paper are varied. Paper documents are easy to review and annotate, portable, and in fact represent a "universal standard" for display, a goal yet tantalizingly out of reach in the electronic world.
Current document management techniques do not acknowledge the continued use of paper or the reasons for it. For example, consider existing systems for storage and retrieval of electronic documents. Typically, a document is specified for retrieval by navigation through a hierarchical directory structure and reference to a file name. However, if the hierarchical directory structure and accompanying file names are not created with great care, retrieving a desired document becomes very difficult because it will be nearly impossible to identify. Studies of electronic filing have found that users usually fail to put in the effort to establish proper electronic filing schemes, often because the effort required is not justified by the value of the information.
By contrast, paper documents are inherently recognizable by appearance. A quick glance is all that is required. Proper filing of paper documents for later retrieval requires a certain administrative discipline but the retrieval process itself is facilitated because paper files themselves are recognizable by titles on their face and by the appearance of their contents.
Present electronic document comparison procedures, i.e., procedures designed to highlight the differences between two versions of a document, are ill-suited for the hybrid world of electronic and paper documents. They assume that both versions of a document to be compared are available electronically and may be readily identified, conditions that are often not satisfied. For example, geographically dispersed authors using two different word processors may communicate with paper hardcopy drafts. Furthermore, it may be difficult to identify and retrieve a previous electronic version of a document for the reasons given above.
What is needed is an electronic document management system that recognizes the continued use of paper documents while facilitating electronic document filing and document comparison.


A method of supporting denitrification includes receiving biological material at a pulsed electric field station and applying a pulsed electric field to the biological material within a treatment zone in the pulse electric field station to generate treated biological material. The method also includes transporting at least a portion of the treated biological material to an anoxic bioreactor in substitution, at least in part, for an external source of electron donor. A system for supporting denitrification is also provided.

This patent is directed to a method and system for generating a source of electron donors for use in denitrification, and, in particular, to a method and system using pulsed electric fields to release intracellular materials from biological materials for use in denitrification.
Wastewater flowing into a conventional wastewater treatment plant may have a high level of nitrogen compounds (such as nitrates, nitrites, etc.) relative to that which is desirable in the water exiting the plant. These nitrogen compounds may be the product of commercial activity, for example. Alternatively, the nitrogen compounds may be the product of agricultural activity, including runoff from fields fertilized using ammonium nitrates.
One way to lower the level of nitrogen compounds is to pass the treated water through an anoxic reactor to conduct a process known as denitrification. However, the anoxic reactor will require a supply of electron donors and possibly a source of carbon to permit the necessary reactions to occur. Many conventional wastewater treatment plants use compounds such as methanol, ethanol or glycol as the supply of the electron donor and carbon.
The use of compounds such as methanol or ethanol is not without its disadvantages. For one thing, methanol and ethanol are flammable substances that require great care in usage, transport and storage. Additionally, while the amount of methanol or ethanol used on a daily basis may not be that large (relative to the amount of water that is treated), the amounts used over a longer period of time may be quite substantial. Given the price of these substances, and the volatility of the price, this can be a considerable budgetary concern for wastewater plant operators, on the order of $250,000 per year for a plant treating ten million gallons of wastewater per day.
Consideration has been given to using waste organic and cellular material as an electron donor. However, the kinetics of cell oxidation of waste organic and cellular material is so slow as to prevent waste organic and cellular material from being considered as a viable alternative to conventional electron donors, such as methanol or ethanol.


An aquatic weight assembly includes a handle and at least one resistance panel assembly having at least one aquatic resistance panel carried by the handle.

Water exercises are enjoyed by persons all over the world as a way to maintain strength, endurance and flexibility. Water exercises include swimming, water aerobics and resistance training. Because of their low-impact nature, water exercises are suitable for persons of all ages including the elderly.
What is needed is an aquatic resistance assembly which is suitable for imparting variable low-impact resistance to movements of an exerciser in a water environment.


A patient support for supporting a patient is provided. The patient support includes a frame and a deck. The deck includes first and second ends and longitudinal sides extending therebetween. The deck also includes a first portion and a second portion that is configured to extend laterally from the deck to widen the deck. An actuator is coupled to the deck and configured to move the second portion relative to the first portion between an extended position and a retracted position.

In the current healthcare environment, hospitals and patient care facilities are treating an ever increasing number of large patients, particularly bariatric patients. Larger patients may not be comfortable on a standard hospital bed having a standard width. Hospital beds having wider decks and corresponding wider mattresses may provide larger patients more comfort, but may be difficult to maneuver down hallways, through doorways, etc. due to the increased width. Also, current expandable width mattresses may become uneven when in the narrowest position and produce uneven raised portions which apply more pressure to a particular section of a patient than to other sections of the patient.
A patient support is provided. The patient support includes a frame, a deck supported by the frame, the deck being configureable to support a patient in a horizontal position, the deck including first and second ends and longitudinal sides extending therebetween, the deck including a first portion configured to extend laterally from the deck to widen the deck; and an actuator coupled to the deck and configured to move the first portion between an extended position and a retracted position. The deck may include a plurality of deck sections. The plurality of deck sections may include a head section, a back section, and a seat section. The head section, the back section, and the seat section may each include a portion configured to extend laterally.
The first portion may extend laterally in a first direction and the deck may include a second portion configured to extend laterally an opposing direction. The first portion may extend along one of the longitudinal sides of the deck and the second portion extends along the opposing longitudinal side of the deck.
The patient support may further include a siderail positioned adjacent the longitudinal side of the deck, the siderail being configured to extend laterally from the deck when the first portion extends to widen the deck. The actuator may be a hydraulic cylinder.
The patient support may further include a telescopic support coupled the first portion and configured to support the first portion in the laterally extended position. The patient support may further include a siderail coupled to the telescopic support. The patient support may further include a controller configured to actuate the actuator to extend or retract the first portion.
In another embodiment, a patient support is provided. The patient support includes a frame and a deck supported by the frame, the deck being configurable to support a patient in a horizontal position, the deck including a plurality of deck sections including an extendable foot section, at least one of the deck sections including first and second portions, the second portion moveable between one of a laterally extended position and a laterally retracted position relative to the first portion.
The patient support may further include an actuator configured to move the extendable foot section between a retracted position and an extended position. The patient support may further include an actuator configured to laterally extend and retract the second portion. The deck may include a head section, a back section, a seat section, and a thigh section. The head section, the back section, and the thigh section may each include first and second portions, the second portion moveable between a laterally extended position and a laterally retracted position. The mattress may include a plurality of vertical openings configured to allow the mattress to compress when the extendable foot section is moved between an extended position and a retracted position.
In yet another embodiment, a patient support is provided, including a frame, a deck supported by the frame, the deck including first and second ends and longitudinal sides extending therebetween, the deck including a first portion configured to laterally extend and retract from the deck to widen and narrow the deck, and a first siderail supported by the frame, the first siderail being positioned adjacent to the first portion and configured to laterally extend and retract with the first portion.
The first siderail may be rigidly coupled to the first portion. The first siderail may be moveable between a raised position and a lowered position. The first siderail may be moveable between the raised and lowered positions when the first portion is in one of the laterally extended and retracted positions.
The patient support may further include a second siderail positioned adjacent to the first siderail, the second siderail including a curved end portion corresponding to a relieved portion of the first siderail.
In still another embodiment, a patient support is provided, including a frame,a deck including a head end, a foot end, and longitudinal sides extending therebetween, a first siderail supported by the frame and positioned adjacent the deck; and an actuator coupled to the siderail and configured to move the siderail between a retracted position and a laterally extended position. The first siderail may be supported by a moveable deck section configured to widen the deck. The first siderail may be moveable between a raised position and a lowered position.
The deck may include at least a head section, a seat section, and a foot section, the first siderail coupled to the head section and a second siderail coupled to the seat section, the second siderail positioned adjacent the first siderail.
In yet another embodiment, a patient support is provided, including a frame, a deck including a head end, a foot end, and longitudinal sides extending therebetween, a siderail positioned adjacent the deck, the siderail being moveable between a retracted position and a laterally extended position, the siderail being lockable in one of the laterally extended position and the retracted position.
The siderail may be moved between the retracted position and the laterally extended position by a hydraulic cylinder. The siderail may be moveable between a raised position and a lowered position. The deck may include a first portion configured to extend from the deck to widen the deck.
The patient support may also include a plurality of siderails moveable between the retracted position and the laterally extended position, at least two of the plurality of siderails being lockable in one of the laterally extended position and the retracted position.
In still another embodiment, a patient support is provided, including a frame, a deck supported by the frame, the deck including first and second ends and longitudinal sides extending therebetween, the deck including a first portion configured to extend and retract laterally from the deck to widen and narrow the deck, a mattress supported by the deck; and a mattress support member positioned adjacent the mattress and configured to laterally compress the mattress when the first portion is retracted. The mattress support member may be supported by the first portion. The mattress support member may include first and second ends coupled to the first portion and a second portion extending between the first and second ends. The deck may include a second portion opposing the first portion and configured to laterally extend and retract to widen or narrow the deck, the first portion supporting a first mattress support member and the second portion supporting a second mattress support member.
The mattress support member may be positioned adjacent a siderail supported by the first portion. The siderail may be positioned adjacent to the first portion and configured to laterally extend and retract with the first portion. The siderail may be movable between a raised position and a lowered position when the first portion is extended or retracted.
The mattress may include a plurality of spaced-apart substantially diamond-shaped cut-out regions configured to allow the mattress to compress. Each of the cut-out regions may include at least one notched portion that has a profile that is one of rectangular and circular in shape.
In yet another embodiment, a patient support is provided, including a frame, a deck including a head end, a foot end, and a pair of longitudinal sides extending therebetween, the longitudinal sides defining a longitudinal axis; and a siderail supported by the frame and positioned at a first longitudinal position relative to the deck, the siderail being moveable between a raised orientation and a lowered orientation, the siderail being moveable between a retracted position and a laterally extended position in both the raised and lowered orientations, the siderail further configured to maintain the first longitudinal position in the raised orientation during movement between the retracted position and the laterally extended position. The siderail may be configured to maintain the first longitudinal position in the lowered orientation.
In still another embodiment, a patient support is provided, including a frame, a deck including a head end, a foot end, and a pair of longitudinal sides extending therebetween, the longitudinal sides defining lateral edges of the deck, the deck including a first portion moveable between a retracted position and a laterally extended position to widen and narrow the deck; and a siderail supported by the frame and spaced apart from the lateral edge of the deck by a first distance, the first distance remaining constant as the first portion is moved between the retracted position and the laterally extended position. The siderail may be moveable between a raised position and a lowered position.

Patient support having powered adjustable width