The present invention provides a joined body having a first member 7, a second member 4 and a joining material 14 interposed between the first and second members. The joining material has a porous bone structure 15 with open pores and made of a sintered product of metal powder and impregnated phase 10 impregnated into the open pores. The impregnated phase 10 includes an oxynitride glass. The joined body has improved resistance against fatigue and fracture, even when the body is subjected to thermal cycles between high and room temperatures and held at a high temperature over a long period of time.

1. Field of the Invention
The present invention relates to a joined body, a high pressure discharge lamp and an assembly therefor.
2. Description of the Related Art
A high pressure discharge lamp has a ceramic discharge vessel with two end portions. Sealing members (usually referred to as a ceramic plug) are inserted, respectively, in the end portions to seal them. A through hole is formed in each sealing member. A metal member with an electrode system is inserted in the through hole. An ionizable light-emitting material is introduced and sealed in the inner space of the discharge vessel Known high pressure discharge lamps include high pressure sodium vapor and metal halide lamps, the latter exhibiting more superior color coordination. The lamp may be used in high temperature condition by forming the discharge vessel by a ceramic material.
In such discharge lamp, it is necessary to air-tightly seal between the end portion of the ceramic discharge vessel and a member for supporting an electrode system. The vessel has a main body with a shape of a tube with two narrow ends, or a barrel or a straight tube. The discharge vessel is made of, for example, an alumina sintered body.
A Japanese patent publication No. 2001-58, 882A (EP 0982278, A1) disclose the following structure. A joining portion is provided between the end portion of a ceramic discharge vessel and a member for supporting an electrode system. The joining portion has a joining material contacting the discharge vessel and an intermediate layer contacting the supporting member and existing between the supporting member and the joining material. The joining material is composed of a porous bone structure with open pores and made of a sintered product of metal powder. The joining material further has ceramic phase impregnated into the open pores in the bone structure. Herewith, such joined body has improved air-tightness and resistance against corrosion, so that repeated thermal cycles does not result in the fracture of the joined body.

Joined bodies, high pressure discharge lamps and assemblies therefor


A new marine oil production riser system for use in deepwater applications is disclosed. An efficient means for accommodating movements of the host facility, while maintaining riser top tension within the limits for long-term riser performance. Long riser stroke lengths can be accommodated without requiring complex interfacing with the topsides. The riser assembly comprises: a generally extendable substantially non-vertical section having an upper end adapted to be in flow communication with a generally vertical marine riser carried by a facility floating on the surface of a body of water, and having a lower end adapted to be in flow communication with a fluid source on the seafloor; and tensioning means, mechanically connecting the upper end of the marine riser with the lower end of the marine riser, for biasing said ends towards each other. The tensioning means comprises: a cylinder having one end open to sea pressure, having an opposite end sealed from sea pressure, and connected to one end of the marine riser; a piston within the cylinder disposed for movement within the cylinder; and a piston rod passing through the opposite end of the cylinder and having one end connected to the other end of the marine riser.

Marine riser technology and its development have been driven by two basic needs in the oil industry.
The first need has been to resolve the challenges that are related to using drilling risers during exploratory drilling. These risers bridge between the seabed and the surface when doing exploration drilling from a floating vessel, which is normally either a semi-submersible drilling rig, or a drill ship. These riser needs can be characterized as large diameter and relatively low pressure. They are designed for rapid disconnect from the seabed equipment, efficient running and retrieval via the drilling vessel, and relatively short design life. Basic floating drilling methods were established in the 1960's1 (superscripts refer to "List of References" appearing before the Claims at the end of this specification) and these methods continue to be improved upon today2.
The second riser need occurs when exploration drilling is successful, leading to a field development. These field development risers bridge between the life-of-field development seabed and surface Host Facility. These risers have small diameters and large diameters, operate at relatively high pressures, and are designed in accordance with field development expectations for near-continuous hydrocarbon depletion that may require 20 years and more of uninterrupted service. These risers may include export and import riser systems that are related to the hydrocarbon production and sales. Also, if well drilling and completion is to be performed from the Host Facility, these riser needs have also to be addressed3.
The pace for deepwater developments in the Gulf of Mexico has been dramatic since the mid-1990's. A brief summary is presented in Appendix IV. The Industry has gone through a series of stages of riser technology development, resulting in the present preferred Steel Catenary Riser (SCR)/Flowline (FL) riser solutions for deepwater. SCR's have evolved in a natural way to replace the large, complex and costly top tensioning equipment that are required when vertical riser systems are used. Vertical risers with top tensioning are effective to water depths of about 4000 feet. However, top tensioning equipment, because of its size, weight, and tight clearances, is costly and difficult to manage. This geometric relationship becomes increasingly challenging when the Host Facility must support this equipment for riser strokes of more than 7–12 feet. For one project in the Gulf of Mexico in 6000 feet of water, riser top motions can approach about 20 feet. These motions represent major design challenge, even for the SCR/FL risers. The challenge is magnified due to the large number of risers that must bridge between the seabed and the Host Facility.
This stroke length is necessary to accommodate the change in riser system length as the Host Facility moves from its neutral position. Without this riser stroke, the riser would be subjected to either over-stressing or large stress level cycles. Riser failure can be manifested by either overstressing it, or by subjecting it to excessive stress cycling. The stress cycling can lead to riser failure due to accumulated fatigue damage, even though the allowable stress is not exceeded for the riser system.
The riser stroke length challenge is graphically represented in FIG. E-2 of a U.S. provisional patent application filed on Apr. 26, 2002 under Ser. No. 60/375,619. When a riser is attached to a fixed point on the seabed and directly to the Host Facility, the riser top must move along with the Host Facility. Considering the life of field possibilities, the range of motions that may occur is extensive. The solution to this changing riser length (stroke requirement) should be robust, as failure to do so is can lead to riser failure. Riser failure can be caused either by the immediate effect of over-stressing, or by diminished fatigue life due to excessive stress cycling. Riser failure due to collapse can also occur, but this tends to be a direct consequence of over-stressing it. In the case of Host Facilities that have very large motions, such as the FPSO systems that have been used outside the Gulf of Mexico, the riser stroke requirement can be met by using flexible pipe16.
A flexible pipe solution (See FIG. E-3(a) of the U.S. provisional patent application filed on Apr. 26, 2002 under Ser. No. 60/375,619), has been used successfully many times. However, for very deep water, this method can be costly. Also, flexible pipe technology for risers (i.e., ones that require a design combination of deepwater, high pressure, high temperature, or large size) remains under on-going development before flexible pipe will be ready for the long field life riser applications. Flexible pipe risers can provide good closing solutions when used in conjunction with a free-standing rigid riser (See FIG. E-3(b) of the U.S. provisional patent application filed on Apr. 26, 2002 under Ser. No. 60/375,619). This arrangement is sometimes referred to as a "hybrid riser" because it combines elements of both buoyancy for top tensioning of the steel risers and flexible pipe to complete the bridging from the top of the rigid risers to the Host Facility. This arrangement is commonly used for Spar well system jumpers that bridge between the well tree and the host manifold. The flexible pipe elements are comprised of a wall body that is made up of various combinations of metal and elastomers. The flexible pipe design is tailored to meet each specific application need. Although the resulting flexibility can help resolve the strokelength challenges that exist with rigid risers and they provide an efficient closing duty, their use for a life-of-field application for the entire riser system remains uncertain. Also, specialized installation methods are often used to ensure that the integrity of flexible pipe is maintained.
The fundamental need for a top-tensioning assembly is represented in FIG. E-4A of the U.S. provisional patent application filed on Apr. 26, 2002 under Ser. No. 60/375,619). In that example, no top-tensioning assembly with stroke length change is provided for the riser. Thus, it bridges directly between the seabed connection point and a point on the host facility. This is only shown as a hypothetical configuration. It assumes that the Host Facility could be designed such a way that the combination of hull and mooring would limit the hull motions so that this would be feasible. Also, it assumes that no over pull is applied to the riser at the neutral position. In an actual design, some over pull is necessary to ensure riser integrity for the range of environmental loads to which it will be subjected. However, as can be seen in this drawing, as the Host Facility moves laterally from its neutral position, the riser top-tensile stress begins to increase rapidly. In this example, an allowable material stress value of about 60,000 psi was assumed. Modern steels can be manufactured to provide material properties like this, including the direct requirement for suitable welding methods. Work to provide suitable commercial grade steels of higher stress values is continuing. But if it were possible to keep the Host Facility offset to within a very small percent of water depth, this type of rigid riser could be feasible today if cost realities related to the hull and mooring were not a consideration.
Given the recent pace of these developments, it is easy to understand why a deepwater field development would be based on the most proven riser systems that are available to the system designers. However, when subsea wells and equipment are located directly under the Host Facility, managing the seabed equipment, wells flowlines, and risers is costly and complex. The SCR/Flowline system requires that the SCR be routed in a straight line and away from the Host Facility. The flowline is routed around and back under the Host Facility, where it can then be connected to the subsea manifold using a jumper. Also, a flowline jumper arrangement is required to allow efficient transition between the SCR and the flowline. The drilling riser that is located on the Host Facility can be equipped with a conventional riser top-tensioning system. This is possible because it can be disconnected when Host Facility motions exceed a pre-determined limit. Since the production export and import risers cannot be disconnected this way, the use of a top tensioning assembly at the surface for these risers can only be obtained at the expense of space, weight, and clearance requirements on the topsides. The complexity and cost of doing this is high for deepwater applications. This is the fundamental reason why the SCR/Flowline method has been used. It represents a better solution than can be achieved by using a vertical riser with a top tensioning assembly. Top-tensioned risers continue to meet field development needs, and it is expected that they will continue to do so for many situations. Even so, the need for new approaches continues. Current riser design practices15 recognize this need, and theses practices provide guidance on the approaches that can be used to qualify new riser designs.
In those cases that require vertical access into the riser system, a top tensioning assembly may continue to be a preferred solution, as this may be the only practical means for providing vertical riser access for well drilling and completion purposes. However, some types of risers do not require vertical access. These riser systems include the export and import risers that are used to move products away from and onto the Host Facility. The SCR/FL solution can also be used to meet these duties, especially for the larger riser sizes.
These problems have existed for some time. Considerable effort has been made, and significant amounts of money have been expended to resolve this problem. In spite of this, the problem still exists. Actually, the problem has become aggravated with the passage of time because the water depth requirements continue to rely on costly solutions, or solutions that are approaching their limits of practical application.

Marine bottomed tensioned riser and method


A seat structure includes a seat frame, a three-dimensional net stretched over the seat frame, a skin material for selectively covering the three-dimensional net, and a fastener for connecting a portion of the skin material and the three-dimensional net. The fastener is selectively opened or closed to change a surface rigidity of the seat structure.

1. Field of the Invention
The present invention relates to a seat structure in which a three-dimensional net having a large hysteresis loss is employed.
2. Description of the Related Art
Conventional automobile seats generally include spring members attached to a seat frame, a pad material such as a foamed material or cotton placed thereon, and a skin such as a vinyl leather, woven cloth, or leather covered thereon.
On the other hand, seats other than the automobile seats generally include a pad material placed on the frame and covered with a skin, and some of them also include spring members for enhancing the cushioning characteristics.
Although the spring members or the pad material acts to provide desired cushioning characteristics, conventional seats are mostly thick, heavy and costly.
In view of the above, a variety of lightweight, inexpensive and thin seats have been recently proposed, and the inventors of this application have developed thin seats having a lightweight net of a three-dimensional structure that is provided with desired characteristics (spring characteristics, damping characteristics and the like) sufficient for a cushioning material.
FIG. 5 depicts an example of the seat structures employing the three-dimensional net that has been developed by the inventors of this application, and particularly depicts a horizontal section of a seat back.
In the seat structure of FIG. 5, a three-dimensional net 52 stretched over a seat back frame 50 is selectively covered with a skin material 54. The skin material 54 is sewn on the three-dimensional net 52, to which is applied a predetermined tension by a plurality of tension members 56.
With this structure, because the three-dimensional net 52 is sewn together with the skin material 54 at a location where the back of a seat occupant is brought into contact with the skin material 54, this location is high in surface rigidity and, hence, expansion and contraction of the three-dimensional net 52 takes place at locations other than the central portion (the portion with which the back of the seat occupant is brought into contact).
Although the automobile seats employing the three-dimensional net are lightweight and have certain cushioning characteristics, they do not have a structure capable of selecting a riding feeling of being high in surface rigidity or a riding feeling in which the body of the seat occupant fits well with the seat and, hence, there is still room for improvement.


An object of the present invention is to provide a stepping motor capable of reducing the number of components and the number of assembling steps, and its manufacturing method. In order to achieve the object, a stepping motor according to the present invention is constructed to include a bobbin which integrally holds a yoke and a connector housing which is disposed at one end portion in an axial direction of the bobbin and integrally holds a pin for connecting a coil wound around the bobbin to an external conductor, and to integrally form the bobbin and the connector housing of a resin.

As this kind of stepping motor, for example, the one disclosed in Patent Document 1 (Japanese Patent Laid-open No. 5-284717) is known. The stepping motor includes a molded bobbin (bobbin) molded of a resin of polybutylene terephthalate (PBT) to integrally hold a magnetic plate (yoke), and an electric connector (connector housing) which is disposed at one end portion in an axial direction of the molded bobbin and is molded of a resin of polyethylene terephthalate (PET) to integrally hold an electric terminal (pin) for connecting an end portion of a coil (winding wire) that is wound around the above described bobbin, and is constructed by ultrasonic welding of opposing resin surfaces of the above described bobbin and electric connector.
In the above described conventional stepping motor, however, the molded bobbin and the electric connector are constructed by separate pieces, and therefore, in order to fix the electric connector to the molded bobbin, ultrasonic welding as described above or another means has to be used, which causes the problem of being incapable of reducing the number of components and assembling steps.
Patent Document 1: Japanese Patent Laid-open No. 5-284717

Stepping motor and method of manufacturing the same


It is possible to know a guideline for adjusting the levels of three voltage thresholds of a PAM4 signal. An error detection device receives a measurement pattern including a pseudo random pattern having equal appearance frequencies of four levels, decodes the measurement pattern into a most significant bit sequence signal MSB and a least significant bit sequence signal LSB, based on three voltage thresholds Vth1, Vth2, and Vth3, identifies and counts, by a level counting unit, the four levels of the measurement pattern, based on the most significant bit sequence signal MSB and the least significant bit sequence signal LSB, and displays numerical values or bar graphs indicating ratios of the appearance frequencies of the four levels of the measurement pattern so as to be in the same order as waveform levels of the measurement pattern, based on a result of the counting.

In 100G and 400G standards defined by IEEE, in order to respond to ultra-high speed of bit rate, transmission employing PAM4 signal is specified instead of transmission employing PAM2 (NRZ) signal in the related art.
For the PAM4 signal, for example, as shown in Patent Document 1 below, the most significant bit sequence signal (MSB) and the least significant bit sequence signal (LSB) are generated using two signal sources, and then these signals are added together to generate signals of four values of 0(00), 1(01), 2(10), and 3(11).
To explain further, the amplitude of the PAM4 signal is divided into four types for each symbol, and as shown in FIG. 4, the PAM4 signal has four different amplitude voltages L0, L1, L2, and L3, and includes signals in an amplitude range in which the entire amplitude voltage range H is divided into a low voltage range H1, a medium voltage range H2, and a high voltage range H3, from a baseline (L0: 0 level), and three eye pattern openings formed by Upper signal (high level signal), Middle signal (medium level signal), and Lower signal (low level signal) having different amplitude levels with respect to the baseline (L0: 0 level) are continuous.
Incidentally, in order to receive this type of PAM signal, it is necessary to adjust the phase direction and adjust the three voltage thresholds Vth1, Vth2, and Vth3 for identifying the levels of the four values, and it is necessary to adjust a total of four parameters. Therefore, it is very difficult to properly match the three voltage thresholds Vth1, Vth2, and Vth3 as compared with the NRZ signal having one voltage threshold.
Here, the relationship between the PAM4 signal symbols and the three voltage thresholds Vth1, Vth2, and Vth3 is shown in FIGS. 5A to 5E.
FIG. 5A shows a case where the three voltage thresholds Vth1, Vth2, and Vth3 are set within the medium voltage range H2. In the case of FIG. 5A, the symbols of the PAM4 signal are decoded to be a combination of bits in which (MSB, LSB)=(1,0), (0,1) do not appear, and symbols 1 and 2 of the PAM4 signal are absent.
FIG. 5B shows a case where the voltage thresholds Vth1 and Vth2 are set within the medium voltage range H2 and the voltage threshold Vth3 is set within the high voltage range H3. In the case of FIG. 5B, the symbols of the PAM4 signal are decoded to be a combination of bits in which (MSB, LSB)=(0,1) does not appear, and the symbol 1 of the PAM4 signal is absent.
FIG. 5C shows a case where the voltage threshold Vth1 is set within the low voltage range H1, the voltage threshold Vth2 is set within the medium voltage range H2, and the voltage threshold Vth3 is set within the high voltage range H3. In the case of FIG. 5C, when the symbols of the PAM4 signal are decoded, the symbols 0, 1, 2, and 3 of the PAM4 signal become equal.
FIG. 5D shows a case where the voltage threshold Vth1 is set within the low voltage range H1, the voltage threshold Vth2 is set within the medium voltage range H2, and the voltage threshold Vth3 is set higher than the high voltage range H3. In the case of FIG. 5D, the symbols of the PAM4 signal are decoded to be a combination of bits in which (MSB, LSB)=(1,1) does not appear, and the symbol 3 of the PAM4 signal is absent.
FIG. 5E shows a case where the voltage threshold Vth1 is set lower than the low voltage range H1, the voltage threshold Vth2 is set within the medium voltage range H2, and the voltage threshold Vth3 is set higher than the high voltage range H3. In the case of FIG. 5E, the symbols of the PAM4 signal are decoded to be a combination of bits in which (MSB, LSB)=(1,1), (0,0) do not appear, and symbols 0 and 3 of the PAM4 signal are absent.

Error detection device and error detection method


A method of compressing an original document image in a manner assuring a minimum compression ratio includes the steps: a) storing to a tile memory a portion of the document image; b) from the document image portion stored in tile memory, using the discrete cosine transform a basis function (DCT), forming a frequency space representation of the image at a transformer; c) retrieving a set of stored values referred to as a Q-Table, d) dividing each of the Q-Table values into the DCT value, and returning the integer portion of the value as the quantized DCT value; e) encoding the quantized DCT values using a statistical encoding method; f) determining whether the data block size is larger than desired, and if not, passing the data block to an output; g) otherwise, reducing a least one high frequency component of the frequency space representation of the document image and and repeating steps e)-g) until the size of the data block is acceptable. In accordance with another aspect of the invention, the steps of f and g may be expressed as: f) counting the number of bits representing the compressed tile of image data; g) comparing the count to a reference; h) if the count is less than the reference, passing the compressed tile to an output; i) if the count is greater than the reference, modifying the quantized DCT values, and repeating steps e)-i).

Data compression is required in data handling processes, where too much data is present for practical applications using the data. Commonly, compression is used in communication links, where the time to transmit is long, or where bandwidth is limited. Another use for compression is in data storage, where the amount of media space on which the data is stored can be substantially reduced with compression. Yet another application is a digital copier or a multi-function device (MFD) where an intermediate storage for collation, reprint or any other digital copier/MFD functions is desired. Generally speaking, scanned images, i.e., electronic representations of hard copy documents, are commonly large, and thus are desirable candidates for compression.
Many different compression techniques exist, and many are proprietary to individual users. However, standards are desirable whenever intercommunication between devices will be practiced. Particularly with the advent of proliferating network communication, where formerly dissimilar devices are required to communicate, a common standard will be required. An example is the current desirability of FAX machines to be able to communicate with printers. Currently, compression standards are generally distinct for different devices.
Three major schemes for image compression are currently being studied by international standardization groups. A first, for facsimile type image transmission, which is primarily binary, is under study by the JBIG (Joint Binary Image Group) committee, a second for TV and film, a standard is worked on by the MPEG (Motion Pictures Expert Group). For non-moving general images, i.e., still images which are more general than the ones covered by JBIG, the group JPEG (Joint Photographic Expert Group) is seeking to develop a device independent compression standard, using an adaptive discrete cosine transform scheme.
ADCT (Adaptive Discrete Cosine Transform, described for example, by W. H. Chen and C. H. Smith, in "Adaptive Coding of Monochrome and Color Images", IEEE Trans. Comm., Vol. COM-25, pp. 1285-1292, November 1977), as the method disseminated by the JPEG committee will be called in this application, is a lossy system which reduces data redundancies based on pixel to pixel correlations. Generally, in images, on a pixel to pixel basis, an image does not change very much. An image therefore has what is known as "natural spatial correlation". In natural scenes, correlation is generalized, but not exact. For example, noise makes each pixel somewhat different from its neighbors.
ADCT transforms are well known, and hardware exists to perform the transform on image data, e.g., U.S. Pat. No. 5,049,991 to Nihara, U.S. Pat. No. 5,001,559 to Gonzales et al., and U.S. Pat. No. 4,999,705 to Puri. The primary thrust of these particular patents, however, is moving picture images, and not document images.
Generally, as shown in FIG. 1, the process of compression requires a tile memory 10 storing an M.times.M tile of the image. Square tiles are used in the description based on the JPEG recommendations, but it may be noted that the inventive method can be performed with any form of tiling. From the portion of the image stored in tile memory, a frequency space representation of the image is formed at transformer 12 using the discrete cosine transform (DCT). In the following we will refer to the DCT data as frequency space data. Hardware implementations are available, such as the C-Cube Microsystems CL550A JPEG image compression processor, which operates in either the compression or the decompression mode according to the proposed JPEG standard. A divisor/quantization device 14 is used, from a set of values referred to as a Q-Table, stored in a Q table memory 16, so that a distinct Q table value is divided into the DCT value, returning the integer portion of the value as the quantized DCT value. A statistical encoder 20 further compresses the quantized DCT values to generate the compressed image that is output for storage, transmission, etc.
The current ADCT compression method divides an image into M.times.M pixel blocks, where M=8. The selection of M=8 is a compromise, where the larger the block given, the higher the compression ratio obtainable. However, such a larger block is also more likely to have non-correlated pixels within the block, thereby reducing the compression ratio. If the block was smaller, greater correlation within the block might be achieved, but less overall compression would be achieved. Particularly within a document image, edges of the image are more likely to be encountered within an 8.times.8 block, than would be the case for a scene forming a natural image.
Compression schemes tend to use a set of basis functions to utilize the intra block correlations. Basis functions define the data as a projection onto a set of orthogonal functions on an interval. ADCT uses cosine functions as the basis functions and the Discrete Cosine Transform (DCT) as the projection step. In the first step of the ADCT standard, the image is tiled into 8.times.8 blocks. Within each block, a set of 64 DCT coefficients is determined for the pixels in the block. The DCT coefficients represent the coefficients of each cosine term of the discrete cosine transform of the 8.times.8 block.
Referring now to FIG. 2A, an array of 64 gray level values representing 64 pixels in an 8.times.8 block of the image is shown. This 8.times.8 block is transformed according to the JPEG ADCT specifications giving the DCT coefficients shown in FIG. 2B. These coefficients still completely describe the image data of FIG. 2A, but in general larger values will now cluster at the top left corner in the low spatial frequency region. Simultaneously, in the vast majority of images as the frequency of the image increases, the coefficient values in the lower right hand portion of the grid tend towards lower values and zero.
Generally, the human eye tends to see low frequencies in an image better than high frequencies. At higher frequencies, changes from amplitude to amplitude are unnoticeable, unless such changes occur at extremely high contrast. This is a well known effect of the Human Visual System and extensively documented, see e.g. "Visual Performance and Image Coding" by P. Roetling, Proceedings of the S.I.D. 17/2 pp. 111-114 (1976). The ADCT method makes use of the fact that small amplitude changes at high frequencies can be generally ignored.
The next step in the ADCT method involves the use of a quantization or Q-matrix. The Q-matrix shown in FIG. 2C is a standard JPEG-suggested matrix for compression, but ADCT as well as the proposed inventive method can also operate using other Q-matrices (or Q-Tables). The matrix incorporates the effect that lower frequencies are roughly more important than high frequencies by introducing generally larger quantization steps, i.e. larger entries, for larger frequencies. However, the table also attempts to internally construct some desirable variations from the general assumption. Accordingly, the values in the table do vary with frequency, where the exact variation might be a function of the human visual system, of the document type expected, i.e.: photo, text, graphic, etc., or of some other application dependent parameter. Each of the DCT values from FIG. 2B is divided by a corresponding Q-matrix value from FIG. 2C giving quantized DCT (QDCT) values by way of: EQU QDCT[m][n]=INT{DCT[m][n].div.Q-Table[m][n]+1/2}
where INT{A} denotes the integer part of A
The remainder from the division process is discarded, resulting in a loss of data. Here and in the following we use the term division to describe the process detailed in ADCT including the methods for handling truncation and round-off. Furthermore, since the Q values in the lower right hand portion of the table tend to be high, most of the values in that area go to zero, unless there were extremely high amplitudes of the image at the higher frequencies.
After deriving the quantized set of DCT values, shown in FIG. 2D, pixels are arranged in the order of a space filling zigzag curve shown in FIG. 2E and a statistical encoding method, such as the Huffman process, is used to generate the transmitted signal which in this example is described using 171 bits. This statistical coding is performed in a lossless way and the only loss introduced in the compression is the one generated by the quantization of the DCT coefficients using the Q-Table.
To decompress the now-compressed image, and with reference to FIG. 1, a series of functions or steps are followed to reverse the process described. The Huffman encoding is removed at decoder 50. The image signal now represents the quantized DCT coefficients, which are multiplied at signal multiplier 52 by the Q table values in memory 54 in a process inverse to the compression process. At inverse transformer 56, the inverse transform of the discrete cosine transform is derived, and the output image in the spatial domain is stored at image buffer 58.
The actual amount of compressed data, or the compression ratio can be seen to be a function of the image itself, and therefore cannot be predicted. Unfortunately, this leads to difficulties in designing systems that handle compressed image, in terms of selecting buffer size, bandwidth, etc.
All of the references cited herein above are incorporated by reference for their teachings.

ADCT compression with minimum compression ratio


A vehicle audio system such as a vehicle radio is integrated with a vehicle speech system so that outputted speech by the vehicle speech system is played through the audio system. When a speech session begins, the audio system mutes any entertainment audio being played and outputs audio speech received from the vehicle speech system at an initial volume that is constrained to be between minimum and maximum initial volume settings. These initial volume settings are automatically adjusted by the audio system if it detects that the user has a tendency to repeatedly adjust the volume past one of these settings each time a speech session is carried out.

Vehicles today commonly come equipped with speech interfaces for the driver or other user. These speech interfaces can be used by automatic speech recognition (ASR) systems and/or by an onboard telematics unit to permit the user to carry on voice telephone calls. In some vehicles, both the ASR and telephony capabilities are integrated together into a single telematics unit having the speech interface. Telematics units that utilize these speech interfaces are commonly now offered as original equipment on many vehicles and in many cases come as standard equipment. OEM installation of such systems permits the manufacturer to integrate the telematics unit and its speech interface in with other vehicle systems. For example, the audio entertainment systems installed on these vehicles by the manufacturer can include traditional stereo components, satellite radio, as well as integration in with an on-board video entertainment. Operation of the telematics unit can be coordinated with the vehicle audio system so that, for example, the speech from the telematics unit's speech interface is played through one or more of the audio system speakers at a volume controllable by the radio volume knob. Then, when a call comes in to the telematics unit or when the user initiates a speech recognition session with the telematics unit, the radio can be automatically muted while the call or session is in effect and the volume of the caller or ASR system speech can be adjusted by the user via the radio's volume knob. As used herein, these telephone calls and speech recognition sessions are referred to generically as speech sessions.
In one known system that integrates the telematics unit audio output with the vehicle's audio system, each time a speech session is begun, the audio system volume is set back to its previous setting that existed at the end of the most recent speech session. Thus, if the user had finished his or her previous session with the volume set at one-third of maximum volume, then at the initiation of the next speech session, then regardless of the current audio system volume set by the user for music or other infotainment, the volume is automatically adjusted to that one-third setting. The exception to this approach is that the audio system is configured with a minimum volume setting, so that if the user had ended the last speech session with the volume turned all the way down, the new session will begin with the volume at some predetermined minimum volume above zero. In this way, the user will be certain to hear the ASR system or caller.

Adaptive initial volume settings for a vehicle audio system


A liquid crystal cell which minimizes disordered orientation occurring with temperature changes even across a wide range, to exhibit good contrast and high reliability, as well as a smectic liquid crystal composition for use the liquid crystal cell are provided. In smectic liquid crystal compositions having a layer construction in the liquid crystal molecular arrangement, it was found that antiferroelectric liquid crystal compositions resistant to variation in the layer spacing of the smectic phase due to temperature changes are resistant to disordered orientation. Specifically, if the antiferroelectric liquid crystal composition contains at lest 45 wt % of an antiferroelectric liquid crystal compound with roughly constant layer spacing in a temperature range from the temperature t.sub.1 which gives the minimum value for the layer spacing of the smectic C.sub.A * phase to -20.degree. C., no disordered liquid crystal orientation results even after cold/hot temperature cycles. An even greater effect is achieved if the spontaneous polarization at of the composition at temperature t.sub.1 is at least 160 nC/cm.sup.2.

1. Field of the Invention
The present invention relates to a liquid crystal composition and a liquid crystal display, and particularly it relates to a smectic liquid crystal composition which expresses a ferroelectric phase (hereunder abbreviated as "SmC* phase") or an antiferroelectric phase (hereunder abbreviated as "SmC.sub.A * phase") etc., and to a liquid crystal display which employs the smectic liquid crystal composition.
2. Description of the Related Art
Recently, liquid crystal cells have become widely used to take advantage of their characteristics such as thinness, light weight, low electricity consumption, etc., and most of these liquid crystal cells employ nematic liquid crystals.
Since nematic liquid crystals are driven based on the anisotropy of the dielectric constant of the liquid crystal, their speed of response is slow and they are therefore in need of improvement.
In contrast, liquid crystal cells employing liquid crystals exhibiting the chiralsmectic C phase (hereinafter abbreviated as "SmC* phase"), which is ferroelectric and was discovered by Meyer et al., have a high speed response and memory characteristics which are not attained by nematic liquid crystals. Thus, application of ferroelectric liquid crystals to ferroelectric liquid crystal cells, because of these characteristics, is being actively researched.
However, the good orientation and memory characteristics required for liquid crystal cells are difficult to realize in a real cell using the above-mentioned ferroelectric liquid crystals, because ferroelectric liquid crystals are not resistant to external shocks, etc. and thus have many remaining problems to be solved.
On the other hand, Chandani, et al. have recently discovered an antiferroelectric phase (hereinafter abbreviated as "SmC.sub.A * phase") which exhibits three stable states at the low temperature end of the SmC* phase. These antiferroelectric liquid crystals exhibit a thermodynamically stable phase wherein dipoles are arranged in anti-parallel at every adjacent layer, and this causes a field-induced phase transition between the antiferroelectric phase and the ferroelectric phase which is characterized by a clear threshold value and double hysteresis characteristics in response to an applied voltage. New methods of indication are beginning to be investigated using this switching behavior.
Liquid crystal compounds with antiferroelectric phases are already known as described in Japanese Unexamined Patent Publication Nos. 1-213390, 1-316339, 1-316367 and 2-28128, and with disclosures of new antiferroelectric liquid crystal compounds, their numbers are ever increasing.
In practical terms, most of the antiferroelectric liquid crystal compounds produced to date have high melting points and temperature ranges for the antiferroelectric phase which are much higher than room temperature. Normally, the liquid crystal materials used for ferroelectric or antiferroelectric liquid crystal cells are mixtures of 5 to 10 different types of liquid crystal compounds. The reason for this is that It is currently impossible to achieve satisfactory characteristics required for liquid crystal cells by using only one type of liquid crystal compound, while the required characteristics can be satisfied by using a mixture of liquid crystal compounds with different physical characteristics, to achieve a balance of characteristics as a whole.
Incidentally, one of the problems involved in applying smectic liquid crystal compositions including ferroelectric liquid crystal compositions and antiferroelectric liquid crystal compositions to liquid crystal cells is disordered orientation due to temperature changes in the liquid crystal cell.
When the temperature changes from a high to a low temperature, the phase of the liquid crystal composition generally changes from smectic A phase (SmA phase).fwdarw.smectic C* phase (SmC* phase).fwdarw.smectic C.sub.A * phase (SmC.sub.A * phase).fwdarw.smectic I* phase (SmI* phase) or smectic I.sub.A * (SmI.sub.A * phase). In accordance, the layer spacing of the layer structure in the smectic phase of the liquid crystal composition is drastically reduced from the SmA phase, the reduction becoming more moderate by the SmC.sub.A * phase and reaching a minimum at a certain temperature, but then when the temperature is further lowered, it increases again.
On the other hand, when the temperature is raised from a low temperature to a high temperature, the layer spacing undergoes a change opposite to the one described above. The disordered orientation occurs when a cold/hot temperature cycle is applied to the liquid crystal cell.
The reason is believed to be that structural defects occur in the smectic phase layer to absorb the changes in layer spacing during the cold/hot temperature cycle, and thus create the disordered orientation. As a result of this disordered orientation which results in shifting between the liquid crystal optical axis and the polarizing plate angle, light leakage occurs during dark indication periods, thus lowering the value for the contrast represented by the brightness ratio of light indication to dark indication and becoming an obstacle to achieving a clear screen display. In addition, the disordered orientation also tends to produce burning. Burning of the display is a phenomenon caused by the difference in orientation, or brightness, resulting from application of different voltages, such as white indication voltage and black indication voltage, to picture elements with disordered orientation.
For example, as an example of a ferroelectric liquid crystal with temperature dependency of the layer spacing, the display disclosed in Japanese Unexamined Patent Publication No. 2-40625 employs ferroelectric liquid crystals which undergo no change of the layer spacing between the crystalline phase and the smectic phase after crystallization.
However, according to studies by the present inventors, this ferroelectric liquid crystal composition also undergoes variation of the layer spacing with temperature changes within the temperature range of the smectic phase, and thus it has been found that temperature changes within that range cause the disadvantage of disordered orientation and thus a poor indicating function as a liquid crystal cell.
The present inventors have therefore posited that if the layer spacing of smectic liquid crystals is roughly constant throughout temperature changes, then layer structure defects in the smectic phase, as well as disordered orientation, will be suppressed.
Furthermore, as mentioned above, in the case of antiferroelectric liquid crystals, the required physical characteristics cannot be satisfied when only one type of antiferroelectric liquid crystal compound is used to form the liquid crystals in the liquid crystal cell. For example, many liquid crystals have practical problems, such as a temperature range of the antiferroelectric phase which is much higher than room temperature, or a long response time for changes between negative polarity and positive polarity when the driving voltage of the liquid crystal is 50 V or greater. Also, with only one type of liquid crystal compound even the initial orientation is such that the liquid crystal molecules fail to be oriented in the rubbing direction, or even when oriented they have a high degree of light leakage during dark indication periods, thus lowering the contrast.
On the other hand, in the case of liquid crystal compositions which are mixtures of many liquid crystal compounds, the state of orientation is improved, thus lowering the light leakage during dark indication periods.
Consequently, liquid crystal cells are preferably not constructed using only one type of antiferroelectric liquid crystal compound, and as already mentioned they usually require use of an antiferroelectric liquid crystal composition which is a mixture of at least a few types of antiferroelectric liquid crystal compounds. The same also applies to ferroelectric liquid crystals. Because they are used for liquid crystal cells, the compositions must have a low tendency to disordered orientation.
In light of these circumstances, it is an object of the present invention to provide a liquid crystal cell or liquid crystal display which exhibits good contrast by minimizing disordered orientation occurring with temperature changes within a wide range and which has no burnout and high reliability, as well as a smectic liquid crystal composition for use in the liquid crystal cell or liquid crystal display.

Smectic liquid crystal composition and liquid crystal display


A lawn chair with an incorporated solar light protective device that is designed to provide an outdoor place to sit down, while at the same time, provide a place to hide an individual from the potentially damaging rays of the sun. The device includes a sheet of flexible material, preferably canvas, that is mounted above a lawn chair. Some aspects of the sheet are adjustable to allow to be adjusted as needed for various users. The sheet is preferably placed over the head end of the lawn chair, protecting an individual's upper body while the individual is lying in the lawn chair.

The present invention concerns that of a new and improved lawn chair with an incorporated solar light protective device that is designed to provide an outdoor place to sit down, while at the same time, provide a place to hide an individual from the potentially damaging rays of the sun.

Lawn chair with incorporated solar light protective device


A frost free faucet having a spigot assembly including a drain conduit, a sleeve assembly including an elongated pipe, and a valve assembly. The valve assembly including a ¼ turn valve and a check valve. The ¼ turn valve includes a rotatable disc with an inlet and a stationary disc with a through hole. Each disc is formed of a ceramic material, wherein upon turning the rotatable disc 90 degrees in a first direction the inlet and the through-hole align to an open position and upon turning the rotatable disc 90 degrees in a second direction, the inlet and the through-hole misalign to a closed position.

Frost free faucets have long been in existence. These faucets characteristically have a shut-off valve located in the end of an elongated pipe or sleeve located within the wall or a warmer interior area of the building of which the wall is a part. This shut-off valve is operated by an elongated rod connected to an exterior handle. The frost free characteristics of the faucet are caused by the shut-off valve shutting off the flow of water at a point within the wall or building with the residual water in the elongated pipe flowing by gravity outwardly through the conventional outlet drain of the faucet. In this manner, the valve may be used in sub-freezing climates without requiring seasonal draining.
Conventional frost free faucets, however, utilize a valve design that is subject to deterioration during the lifetime of the faucet due to water impurities. The deterioration of the valve subjects the frost free faucet to backflow and leaks, which are undesirable. Furthermore, these conventional valve designs use of a multi-turn operation that is tiresome to operate.
It is desirable, therefore, to provide a frost free faucet that has an improved valve design. More particularly, it is desirable to provide a simple yet sophisticated valve design that enable an increased longevity, while maintaining sufficient backflow prevention. Furthermore, it is desirable to provide a valve design that allows ease of use.


A head lamp apparatus for a vehicle comprises a lamp housing mounted to a front portion of a vehicle body, a head lamp bulb disposed inside the lamp housing and adapted to radiate a light, a reflector for reflecting an irradiation light from the head lamp bulb in a direction forward of the vehicle body, and a position bulb disposed in front of the head lamp bulb inside the lamp housing.

The present invention relates to a head lamp apparatus for a vehicle having a position bulb in addition to a head lamp bulb for illuminating an area ahead of the vehicle.
FIG. 10 is a cross-sectional view of a head lamp apparatus for a motorcycle. The head lamp apparatus 101 is of the type disposed at a front head portion of a streamlined cowling 102 of the motorcycle and a head lamp bulb 104 and a reflector 105 are disposed inside a lamp housing 103. The lamp housing 103 is formed by covering a front surface of a housing body 106 molded by using synthetic resin with a transparent housing lens 107.
A bulb socket 108 disposed on a rear surface of the housing body 106 extends forward through a socket hole 109 defined in the reflector 105 and is defined at its tip end with a position bulb 110. The housing lens. 107 is not effected with a lens cutting operation and passes light as it is, but a lens cut portion 111 is formed only at a portion of the housing lens 107 in front of the position bulb 110.
In the head lamp apparatus 101, a forward irradiation light a from the position bulb 110 is amplified and diffused by the lens cut portion 111 and is radiated forward. An irradiation light b from the position bulb 110 radiated diagonally forward or sideways is reflected by a flange portion 105a formed at an edge portion of the reflector 105 and is radiated diagonally forward. As a result, the light from the position bulb 110 is then radiated forward with a wide angle.
In a head lamp apparatus 121 shown in FIG. 11, on the other hand, a bulb socket 108 is extended such that a position bulb 110 is close to a housing lens 107 and a lens cut portion 111 is formed only at a portion of the housing lens 107 in front of the position bulb 110. In a case of the head lamp apparatus 121, a forward irradiation light c from the position bulb 110 is amplified and diffused by the lens cut portion 111 and is radiated forward. An irradiation light d radiated diagonally forward or sideways is radiated forward with a wide angle without being reflected by the reflector 105 because the position bulb 110 is disposed close to the housing lens 107.
Visibility of the irradiation light from the position bulb 110 of the head lamp apparatus 101 shown in FIG. 10 is not good because the radiating light b reflected by the flange portion 105a of the reflector 105 is radiated diagonally forward and sideways and quantity of light of the irradiation light b is less than that of the radiating light a while the irradiation light a amplified by the lens cut portion 111 is radiated forward and quantity of light of the radiating light a is satisfactory. Moreover, visibility of the irradiation light from of the position bulb 110 is strongly influenced by a shape of the reflector 105 (flange portion 105a).
In this respect, in the head lamp apparatus 121 shown in FIG. 11, because the irradiation light d from the position bulb 110 radiated diagonally forward and sideways is radiated directly with the wide angle without being reflected by the reflector 105, satisfactory quantity of light can be obtained and an visibility of the radiating light from a diagonally front direction and from a side is favorable. However, because the bulb socket 108 projects from a reflecting surface of the reflector 105 by a very large length, the bulb socket 108 is conspicuous from outside through the housing lens 107 which passes light as it is, which becomes a cause of impairment of an outer appearance of the head lamp apparatus 121.
Moreover, because the bulb socket 108 is long, vibration of the body is greatly amplified to be transmitted to the position bulb 110 provided to the tip end of the bulb socket 108, which may cause early breaking of a wire of the position bulb 110. Furthermore, it is necessary to draw the bulb socket 108 rearward out of the lamp housing 103 to change the position bulb 110, but drawing out of the long bulb socket 108 requires a large space behind the lamp housing 103, which adversely affects a layout of other parts.
Furthermore, in any of the head lamp apparatus 101 and 121, the lens cut portion 111 for the position bulb, which is formed on the housing lens 107 which passes light as it is, is positioned at a position largely displaced from a center of the head lamp apparatus 101 or 121, which becomes a cause of impairment of an outer appearance of the head lamp apparatuses 101 and 121.
On the other hand, as another problem, an aiming plate or the like for adjusting an optical axis of a projector lamp can be seen from outside through the housing lens 107 if the projector lamp is disposed inside the head lamp apparatus 101 or 121 having the housing lens 107 which passes light as it is, thus significantly impairing the outer appearance.
It is a primary object of the present invention is to substantially eliminate defects or drawbacks encountered in the prior art mentioned above and to provide a head lamp apparatus for a vehicle capable of ensuring satisfactory quantity of light of a position bulb, improving a visibility of the head lamp apparatus by allowing an irradiation light from the position bulb to be radiated with a wide angle, and arranging the position bulb at a portion not close to one side to improve an outer appearance of the head lamp apparatus.
It is another object of the present invention to provide a head lamp apparatus for the vehicle capable of facilitating change of the position valve and preventing early breaking of a wire of the position bulb.
It is a further object of the present invention to provide a head lamp apparatus capable of efficiently diffusing the irradiation light from the position bulb and improving an anti-glare (glare-shielding) property of the head lamp apparatus when the head lamp bulb illuminates.
It is a still further object of the present invention to provide a head lamp apparatus for the vehicle capable of improving an outer appearance of the head lamp apparatus by hiding an aiming plate or the like of a projector lamp provided additionally in a lamp housing.
It is a still further object of the present invention to provide a head lamp apparatus for the vehicle for improving an anti-glare property of the head lamp apparatus by cutting a diffused light beam or the like radiated from the projector lamp provided additionally in the lamp housing.
These and other objects can be achieved according to the present invention by providing, in one aspect, a head lamp apparatus for a vehicle comprising:
a lamp housing mounted to a front portion of a vehicle body;
a head lamp bulb disposed inside the lamp housing and adapted to radiate a light;
a reflector for reflecting an irradiation light from the head lamp bulb in a direction forward of the vehicle body; and
a position bulb disposed in front of the head lamp bulb inside the lamp housing.
In a preferred embodiment of this aspect, the lamp housing is provided with a housing body and a transparent housing lens covering a front surface of the housing body and the head lamp bulb, the reflector and the position bulb are housed in the lamp housing, and the position bulb is disposed on an upper front side in the lamp housing.
The housing lens is provided with a lens cut portion at a position in front of the position bulb.
In another aspect, there is provided a head lamp apparatus for a vehicle comprising:
a lamp housing mounted to a front portion of a vehicle body;
a head lamp bulb disposed inside the lamp housing and adapted to radiate a light;
a reflector for reflecting an irradiation light from the head lamp bulb in a direction forward of the vehicle body; and
a projector lamp mounted to the lamp housing in adjacent to the reflector and having a projector lamp body and a projector lamp lens mounted to a front portion of the projector lamp body in the forward direction of the vehicle body,
the reflector being formed with an extension extending towards the projector lamp, the extension having a size covering the projector lamp except for the projector lamp lens.
In a preferred embodiment of this aspect, the extension has a tip end portion which is positioned further forward than a joint portion of the projector leans and the lamp body. The extension has a cutout for preventing the covering of the projector lamp lens.
An aiming plate is mounted to the housing body around the projector lamp body so as to adjust an axis of irradiation light.
According to the present invention of the structures mentioned above, because the position bulb is disposed in front of the head lamp bulb, the irradiation light from the head lamp bulb is not cut off, satisfactory quantity of light of the position bulb can be ensured, and the irradiation light from the position bulb can be caused to be radiated at a wide angle, thereby improving visibility. Furthermore, because the position bulb is positioned not close to one side, the outer appearance of the head lamp apparatus can be improved.
Furthermore, since the head lamp bulb, the reflector, and the position bulb are housed in the lamp housing having the housing body and the transparent housing lens covering the front surface of the housing body and the position bulb is disposed on the upper front side in the lamp housing, the change of the position bulb is facilitated and the early breaking of the wire of the position bulb can be prevented.
Still furthermore, since the lens cut portion is formed at the portion of the housing lens in front of the position bulb, the irradiation light from the position bulb can be efficiently diffused and the anti-glare property of the head lamp apparatus when the head lamp bulb illuminates can be improved.
Still furthermore, since the head lamp apparatus comprises the head lamp bulb, the reflector for reflecting the irradiation light from the head lamp bulb ahead of the vehicle, and the projector lamp disposed in adjacent to the reflector, and the reflector has the extension portion which extends towards the projector lamp and hides the projector lamp excluding the projector lens when the head lamp apparatus is viewed from a front side thereof, the aiming plate or the like provided to the projector lamp can be hidden by the extension portion to improve the outer appearance of the head lamp apparatus.
Still furthermore, since the tip end position of the extension portion is disposed further forward than the joint portion of the projector lens and the lamp body of the projector lamp when the head lamp apparatus is viewed from the side thereof, it is possible to cut off the diffused light beam or the like radiated by the projector lamp to improve the anti-glare property of the head lamp apparatus.
The nature and further characteristic features of the present invention will be made more clear from the following description made with reference to the accompanying drawings.


Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula

This invention relates to a new class of azole derivatives, methods for their use, and processes for their production. The compounds described herein are useful for the treatment of fungal infections in humans and other mammals. The present invention provides a compound represented by the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxy group, n is 0 or 1, and R1 and R2 are hydrogen, C1-C6 alkyl or C2-C6 alkenyl, said alkyl or alkenyl group being optionally substituted by a hydroxy or dimethylamino group, or R1 and R2 taken together with the nitrogen to which they are attached forms a heterocyclic group of the formula
where R7 is hydrogen, CHO, COR13 or C1-C6 alkyl in which the alkyl group may be optionally interupted by an oxygen atom or NR14 and may be substituted by hydroxy, R8, R9, R10, R11 and R12 are each independently hydrogen, hydroxy, CONH2, or C1-C6 alkyl, said alkyl group being optionally substituted by hydroxy, R13 is C1-C6 alkyl and R14 is hydrogen or C1-C6 alkyl; or a pharmaceutically acceptable salt thereof.
Triazole antifungal compounds are well known in the prior art. Of the several classes known, one particularly potent class contains a tertiary hydroxyl group. For example, U.S. Pat. No. 5,648,372 discloses that (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol has anti-fungal activity.
The utility of this class of compounds is limited by their low water solubility. One method of addressing this problem was disclosed in European Patent Application 829478, where the water solubility of an azole antifungal agent was increased by attaching a linked amino-acid to the azole portion of the molecule.
Alternatively, WO 97/28169 discloses that a phosphate moiety can be attached directly to the tertiary hydroxyl portion of the anti-fungal compound, e.g. the compound having the formula
Examples describing the use of N-N-dialkylaminomethyl benzoate derivatives as prodrugs can be found in H. Bundgaard et al, J. Med Chem. 32, 2503 (1989); E. Jensen et. al. Int. J. Pharmaceut. 58,143 (1990); and H. Bundgaard, Drugs of the Future 16, 443 (1991).
It has now been found that triazole anti-fungal compounds containing a secondary or tertiary hydroxyl group, including (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol, may be converted into prodrugs with superior properties to those previously disclosed by attaching an amino-containing moiety via a linking group. Specifically, the invention covers compounds of the formula:
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxy group, n is 0 or 1, and R1 and R2 are hydrogen, C1-C6 alkyl or C2-C6 alkenyl, said alkyl or alkenyl group being optionally substituted by a hydroxy or dimethylamino group, or R1 and R2 taken together with the nitrogen to which they are attached forms a heterocyclic group of the formula
where R7 is hydrogen, CHO, COR13 or C1-C6 alkyl in which the alkyl chain may be optionally interupted by either an oxygen atom or NR14 and may be substituted by a hydroxy group, R8, R9, R10, R11 and R12 are each independently hydrogen, hydroxy, CONH2 or C1-C6 alkyl, said R8, R9, R10, R11 or R12 alkyl group being optionally substituted by hydroxy, R13 is C1-C6 alkyl and R14 is hydrogen or C1-C6 alkyl; or a pharmaceutically acceptable salt thereof.
In a preferred embodiment, A represents the non-hydroxy portion of a triazole antifungal compound of the type containing a tertiary hydroxy group.
The various methylamine substituents of formula I may be attached in either an ortho, meta, or para relationship to the ester substituent, with the preferred attachment being either meta or para.
In a preferred embodiment A can be
wherein R3 represents phenyl substituted by one or more (preferably 1-3) halogen atoms;
R4 represents H or CH3;
R5 represents H, or taken together with R4 may represent xe2x95x90CH2;
R6 represents a 5- or 6 membered nitrogen containing ring which may be optionally substituted by one or more groups selected from halogen, xe2x95x90O, phenyl substituted by one or more groups selected from CN, (C6H4)xe2x80x94OCH2CF2CHF2 and CHxe2x95x90CHxe2x80x94(C6H4)xe2x80x94OCH2CF2CHF2, or phenyl substituted by one or more groups selected from halogen and methylpyrazolyl.
Nitrogen containing heterocycles which R6 may represent include triazolyl, pyrimidinyl, and thiazolyl.
Specific examples of A include, but are not limited to, the following:
In addition to the application of the present invention to structures containing a tertiary alcohol, it should also be understood that this discovery can be applied to anti-fungal agents which contain secondary alcohols. Some examples include, but are not limited to, the following:
Representative R1, R2 and n values are shown below:
(where A represents the non-hydroxy portion of a triazole anti-fungal compound of the type containing a tertiary or secondary hydroxyl group)
The term xe2x80x9cpharmaceutically acceptable saltxe2x80x9d as used herein is intended to include the non-toxic acid addition salts with inorganic or organic acids, e.g. salts with acids such as hydrochloric, phosphoric, sulfuric, maleic, acetic, citric, succinic, benzoic, fumaric, mandelic, p-toluene-sulfonic, methanesulfonic, ascorbic, lactic, gluconic, trifluoroacetic, hydroiodic, hydrobromic, and the like.
The term xe2x80x9chalogenxe2x80x9d includes chloro, bromo, fluoro and iodo, and is preferably chloro or fluoro, and most preferably fluoro.
The aliphatic xe2x80x9calkylxe2x80x9d and xe2x80x9calkenylxe2x80x9d groups may be straight or branched chains having the specified number of carbon atoms, e.g. in the case of C1-C6 alkyl, the alkyl group may have from 1 to 6 carbon atoms.
Preferred embodiments of the present invention, including in each case pharmaceutically acceptable salts thereof are:
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(N,N-diethylaminomethyl)benzoyloxy]methoxy]butane (compound of example 1)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(N,N-di-(2-hydroxyethyl)aminomethyl) benzoyloxy]methoxy]butane (compound of example 2)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(4-methyl-piperazinyl)methyl]benzoyloxy]methoxy]butane (compound of example 3)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(N,N-dimethylaminomethyl)benzoyloxy]methoxy]butane (compound of example 4)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(N-methyl-N-(2-hydroxyethyl)aminomethyl) benzoyloxy]methoxy]butane (compound of example 5)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(N-ethyl-N-butyl)aminomethyl]benzoyloxy]methoxy]butane (compound of example 6)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-(4-(2-hydroxyethyl)-1-piperazinylmethyl) benzoyloxy]methoxy]butane (compound of example 7)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(3RS-hydroxy)-1-piperidinylmethyl]benzoyloxy]methoxy]butane (compound of example 8)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4-(2RS-hydroxyethyl)-1-piperidinylmethyl]benzoyloxy]methoxy]butane (compound of example 9)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)2-[[p-[(4-formyl)-1-piperazinylmethyl]benzoyloxy]methoxy]butane (compound of example 10)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4RS-hydroxy)-1-piperidinylmethyl]benzoyloxy]methoxy]butane (compound of example 11)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4-ethyl)-1-piperazinylmethyl]benzoyloxy]methoxy]butane (compound of example 12)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4RS-methyl)-1-piperidinylmethyl]benzoyloxy]methoxy]butane (compound of example 13)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4RS-(N-piperadinyl)-1-piperidinylmethyl]benzoyloxy]methoxy]butane (compound of example 14)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(N,N-dipropyl)aminomethyl]benzoyloxy]methoxy]butane (compound of example 15)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(3RS-hydroxy)-1-pyrrolidinylmethyl]benzoyloxy]ethoxy]butane (compound of example 16)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(N,N-diallyl)aminomethyl]benzoyloxy]methoxy]butane (compound of example 17)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(2S,6R-dimethyl-1-piperidinyl)methyl]benzoyloxy]methoxy]butane (compound of example 18)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[N-ethyl-N-(2-dimethylaminoethyl) aminomethyl]benzoyloxy]methoxy]butane (compound of example 19)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(3-thiazolidinyl)methyl]benzoyloxy]methoxy]butane (compound of example 20)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(N-methyl-N-(3-dimethylaminopropyl) aminomethyl]benzoyloxy]methoxy]butane (compound of example 21)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(3RS-methyl-1-piperidinyl)methyl]benzoyloxy]methoxy]butane (compound of example 22)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[N-methyl-N-(2-dimethylaminoethyl) aminomethyl]benzoyloxy]methoxy]butane (compound of example 23)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[N,N-bis-(2RS-hydroxypropyl)aminomethyl]benzoyloxy]methoxy]butane (compound of example 24).
2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(1-piperidinyl)methyl]benzoyloxy]methoxy]butane (compound of example 25)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[p-[(4-morpholinyl)methyl]benzoyloxy]methoxy]butane (compound of example 26)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[m-[(4-morpholinyl)methyl]benzoyloxy]methoxy]butane (compound of example 27)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[m-(N,N-diethylaminomethyl)benzoyloxy]methoxy]butane (compound of example 28)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[m-[N,N-bis(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]butane (compound of example 29)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[m-[(4-methyl-1-piperazinyl)methyl]benzoyloxy]methoxy]butane (compound of example 30)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[p-[(4-morpholinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 31)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[p-[N,N-diethylaminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 32)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-morpholinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 33)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[p-[N,N-bis-(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 34)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[p-[(4-methyl-1-piperazinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 35)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[N,N-bis-(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 36)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-methyl-1-piperazinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 37)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[N,N-diethylaminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 38)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-(2xe2x80x2-hydroxyethoxy)ethyl-1-piperazinyl) methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 39)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[N-methyl-N-(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 40)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4xe2x80x2-hydroxy-4-piperidinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 41)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4xe2x80x2-carbamyl-4-piperidinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 42)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2[[[m-[(4-(2-hydroxyethyl)-1-piperazinyl) methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 43)
The more preferred embodiments of the present invention, including in each case pharmaceutically acceptable salts thereof are:
1,2,4-triazol-1-yl)-2-[[p-[(4-morpholinyl)methyl]benzoyloxy]methoxy]butane (compound of example 26)
1,2,4-triazol-1-yl)-2-[[[p-[N,N-diethylaminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 32)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-morpholiny)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 33)
1,2,4-triazol-1-yl)-2-[[[p-[N,N-bis-(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 34)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[N,N-b is-(2-hydroxyethyl)aminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 36)
1,2,4-triazol-1-yl)-2-[[[m-[N,N-diethylaminomethyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 38)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-(2xe2x80x2-hydroxyethoxy)ethyl-1-piperazinyl) methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 39)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[N-methyl-N-(2-hydroxyethyl)aminomethyl]enzoyloxy]methoxy]carbonyloxy]butane (compound of example 40)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4xe2x80x2-hydroxy-4-piperidinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 41)
(2R,3R)-3-t4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4xe2x80x2-carbamyl-4-piperidinyl)methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 42)
(2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-[[[m-[(4-(2-hydroxyethyl)-1-piperazinyl) methyl]benzoyloxy]methoxy]carbonyloxy]butane (compound of example 43).
The aforementioned preferred embodiments of the present invention are listed in the table below along with their observed molecular ions (M+ or MH+).
The compounds of the present invention can be made by conventional methods. Two suitable procedures are summarized by the following reaction schemes. In both methods, A represents the non-hydroxy portion of a triazole anti-fungal compound of the type containing a tertiary or secondary hydroxy group.
X=Cl, Br or I, preferably Cl
To elaborate on Method 1, the anti-fungal parent compound of interest is converted into ester 2 by reaction with chloride 1 in the presence of a suitable base, such as potassium hydride. The reaction can be carried out in THP or other appropriate solvent and the product is usually purified by column chromatography. Chloride 1 can be prepared by the general method of Iyer et al., Syn. Comm. 25, 2739, 1995 (see Method 1 below in the Illustrative Examples section) or by Method 2 shown below in the Examples). Ester 2 can be subsequently transformed into arylmethylamine 3 by reaction with the desired dialkyl amine in DMF. The reaction occurs between 25xc2x0 C. and 100xc2x0 C. and the resulting product can be purified by recrystallization or column chromatography. If an amine salt is used, it will be understood that one molar equivalent of an appropriate base should be added to facilitate the reaction.
The intermediates 2 of the formula
wherein the halomethyl substituent is in the ortho, meta or para position, preferably the meta or para position, X is chloro, bromo or iodo, preferably chloro, and A represents the non-hydroxyl portion of a triazole antifungal compound of the type containing a tertiary or secondary hydroxyl group are another aspect of the present invention. The preferred intermediates are those having the specific xe2x80x9cAxe2x80x9d groups mentioned above.
The intermediates 2 may be prepared by reacting a suitable halomethyl benzoic acid ester of the formula
wherein the halomethyl substituent of the phenyl ring is in the ortho, meta or para position, preferably the meta or para position, X is Cl, Br or I, and A represents the non-hydroxyl portion of a triazole antifungal compound of the type containing a tertiary or secondary hydroxyl group with an antifungal agent Axe2x80x94OH wherein A is as defined above in an inert organic solvent such as tetrahydrofuran and in the presence of base such as potassium hydride.
To elaborate on Method 2, the anti-fungal parent compound of interest is transformed into chloromethylformate 4 by reaction with commercially available chloromethylchloroformate (Aldrich Chemical Company) in the presence of an appropriate base in THF or other solvent at 0xc2x0 C. to 50xc2x0 C. Appropriate bases include potassium hydride and sodium hydride, among others, with the preferred base being potassium hydride. The product can be purified by column chromatography. Chloromethylformate 4 is converted to iodide 5 by reaction at elevated temperature with NaI in acetone. The crude product from this reaction can be used in the next step, or the product can be purified via column chromatography. In another aspect then, the present invention provides intermediates 4 of the formula
wherein X1 is Cl, Br or I and A is the non-hydroxy portion of a triazole antifungal compound of the type containing a tertiary or secondary hydroxyl group. The preferred intermediates of formula 4 are those having the specific xe2x80x9cAxe2x80x9d groups mentioned above. Intermediates 4 may be prepared by reacting chloromethylchloroformate with an antifungal agent Axe2x80x94OH in which A is as defined above in an inert organic solvent such as tetrahydrofuran. in the presence of base and, if desired, converting the so-produced chloromethylformate of formula 4 to the corresponding compound of formula 4 wherein X1 is Br or I by reaction with an alkali metal bromide or iodide. Iodide 5 is converted to the final product 7 by reaction with carboxylate salt 6 in acetonitrile or other appropriate organic solvent. The efficiency of the reaction can be increased by adding small amounts of 18-crown-6 or other appropriate crown ether. Carboxylate salt 6 can be prepared by the method disclosed in Lombardino et al in U.S. Pat. No. 4,623,486. The product can be purified by recrystallization or column chromatography. If an amine salt is used, it will be understood that one molar equivalent of an appropriate base should be added to facilitate the reaction. It is also possible to directly convert chloride 4 to the final product by reaction with carboxylate salt 6 at elevated temperatures.
It will be understood that where the substituent groups used in the above reactions contain certain reaction-sensitive functional groups such as amino or carboxylate groups which might result in undesirable side-reactions, such groups may be protected by conventional protecting groups known to those skilled in the art. Suitable protecting groups and methods for their removal are illustrated, for example, in Protective Groups in Organic Synthesis, Theodora W. Greene (John Wiley and Sons, 1991). It is intended that such xe2x80x9cprotectedxe2x80x9d intermediates and end-products are included within the scope of the present disclosure and claims.
The desired end-product of formula I may be recovered in the form of a pharmaceutically acceptable acid addition salt, e.g. by addition of the appropriate acid such as HCl, HI or methane-sulfonic acid to the amine.
It will be appreciated that certain products within the scope of formula I may have substituent groups which can result in formation of optical isomers. It is intended that the present invention include within its scope all such optical isomers as well as epimeric mixtures thereof, i.e. R- or S- or racemic forms.
The pharmaceutically active compounds of this invention may be used alone or formulated as pharmaceutical compositions comprising, in addition to the active triazole ingredient, a pharmaceutically acceptable carrier, adjuvant or diluent. The compounds may be administered by a variety of means, for example, orally, topically or parenterally (intravenous or intramuscular injection). The pharmaceutical compositions may be in solid form such as capsules, tablets, powders, etc. or in liquid form such as solutions, suspensions or emulsions. Compositions for injection may be prepared in unit dose form in ampules or in multidose containers and may contain additives such as suspending, stabilizing and dispersing agents. The compositions may be in ready-to-use form or in powder form for reconstitution at the time of delivery with a suitable vehicle such as sterile water.
Alternatively, the compounds of the present invention can be administered in the form of a suppository or pessary, or they may be applied topically in the form of a lotion, solution, or cream. Additionally, they may be incorporated (at a concentration up to 10%) into an ointment consisting of a white wax or soft, white paraffin base together with the required stabilizers and/or preservatives.
The compounds of the invention are useful because they possess pharmacological activities in animals, including particularly mammals and most particularly, humans. Specifically, the compounds of the present invention are useful for the treatment or prevention of topical fungal infections, including those caused by species of Candida, Trichophyton, Microsporum, or Epidermophyton. Additionally, they are useful for the treatment of mucosal infections caused by Candida albicans. They can also be used in the treatment of systemic fungal infections caused, for example, by species of Candida albicans, Cryptococcus neoformans, Aspergillus flavus, Aspergillus fumigatus, Coccidioides, Paracoccidiodes, Histoplasma, or Blastomyces.
Thus, according to another aspect of the invention, there is provided a method of treating a fungal infection which comprises administering a therapeutically effective amount of the compound to a host, particularly a mammalian host and most particularly a human patient. The use of the compounds of the present invention as pharmaceuticals and the use of the compounds of the invention in the manufacture of a medicament for the treatment of fungal infections are also provided.
The dosage to be administered depends, to a large extent, on the particular compound being used, the particular composition formulated, the route of administration, the nature and condition of the host and the particular situs and organism being treated. Selection of the particular preferred dosage and route of application, then, is left to the discretion of the physician or veterinarian. In general, however, the compounds may be administered parenterally or orally to mammalian hosts in an amount of from about 5 mg/day to about 1.0 g/day. These doses are exemplary of the average case, and there can be individual instances where higher or lower dosages are merited, and such dosages are within the scope of this invention. Furthermore, administration of the compounds of the present inventions can be conducted in either single or divided doses.
The in vitro evaluation of the antifungal activities of the compounds of the invention can be performed by determining the minimum inhibitory concentration (MIC). The MIC is the concentration of test compound which inhibits the growth of the test microorganism. In practice, a series of agar plates, each having the test compound incorporated at a specific concentration, is inoculated with a fungal strain and each plate is then incubated for 48 h at 37xc2x0 C. The plates are examined for the presence or absence of fungal growth, and the relevant concentration is noted. Microorganisms which can be used in the test include Candida albicans, Asperigillus fumigatus, Trichophyton spp., Microsporum spp., Epidermophyton floccosum, Coccidioides immitis, and Torulopsos galbrata. It should be recognized that, as prodrugs, some compounds of the invention may not be active in the in vitro test.
The in vivo evaluation of compounds of the present invention can be carried out at a series of dose levels by intraperitoneal or intravenous injection or by oral administration to mice which have been inoculated with a strain of fungus (e.g. Candida albicans). Activity is determined by comparing the survival of the treated group of mice at different dosage levels after the death of an untreated group of mice. The dose level at which the test compound provides 50% protection against the lethal effect of the infection is noted.
The compounds of the present invention substantially increase the solubility of the parent triazole antifungal compound and also release the bioactive parent compound (i.e. function as a prodrug) in both rat and human plasma. As shown in the table below, this is not the case with the triazole derivatives of WO 97/28169.

Water soluble prodrugs of azole compounds

Abstract: wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.


An example housing of a cabin air compressor assembly includes a main body portion and a motor outlet duct extending radially from the main body portion. The motor outlet duct interfaces with the main body portion at an interface area. A ratio of a radius of the interface area to an inner diameter of the motor outlet duct is from 0.113 to 0.162.

This disclosure relates to a compressor for use in supplying cabin air in an aircraft and, more particularly, to a housing for such a compressor.
Compressors that supply cabin air are known. Compressors typically include a motor driven to rotate a shaft and in turn drive a compressor rotor. The rotor moves a first supply of air into the compressor. This air is cooled and delivered to the cabin.
At least the motor is held within a housing. A second supply of air moves through the housing from an inlet to an outlet of the compressor. The air moves through the motor to cool the motor.


An electronic device includes a touch screen. When the electronic device wakes up and works in a locked state, a notification interface including a predetermined unlocking area is displayed on the touch screen. A user pattern formed by at least two fingers of a user located within the predetermined unlocking area is detected. The electronic device is unlocked if the user pattern matches a predetermined unlocking pattern.

1. Technical Field
Embodiments of the present disclosure relate to unlocking of electronic devices, and particularly, to an unlocking method of an electronic device.
2. Description of Related Art
Many electronic devices, such as smart phones and tablet computers, have locking functions to avoid unintended operations. Current unlocking methods include unlocking by gestures, passwords, and patterns, which are tedious. Therefore, an improved unlocking method of the electronic devices is needed.

Electronic device and unlocking method thereof

Fu Tai Hua Industry (Shenzhen) Co., Ltd.


A photoelectric conversion unit has first semiconductor regions and a second semiconductor region that is disposed between the first semiconductor regions being adjacently disposed in the unit. Impurity concentration profile in a depth direction of the first and semiconductor regions has a plurality of peaks. The impurity concentration peaks of the first semiconductor region include a first impurity concentration peak and a second impurity concentration peak being lower than the first impurity concentration peak. The impurity concentration peaks of the second semiconductor region include a third, a fourth, and a fifth impurity concentration peak. The fourth impurity concentration peak is higher than the third impurity concentration peak, and a fifth impurity concentration peak is higher than the third impurity concentration peak. The depth of the third impurity concentration peak is closer to the depth of the second impurity concentration peak than that of the first impurity concentration peak.

1. Field of the Invention
One disclosed aspect of the embodiments relates to a photoelectric conversion apparatus, and it particularly relates to a separation structure between photoelectric conversion elements.
2. Description of the Related Art
In the past, signals generated by a plurality of photoelectric conversion elements may have been processed as a signal from one pixel in a photoelectric conversion apparatus. For example, there is a technology that gathers light to a plurality of photoelectric conversion elements through one micro lens for performing phase difference focus detection. As disclosed in Japanese Patent Laid-Open No. 2001-250931, for example, signals obtained from photoelectric conversion elements that receive light passing through one micro lens are read independently for focus detection and combined into one signal for image processing.
When signals of a plurality of photoelectric conversion elements are processed as a signal of one pixel and if the plurality of photoelectric conversion elements differ in sensitivity and incident light quantity, it may be difficult to acquire a proper signal therefrom. Particularly, photoelectric conversion elements may be neighboring to various elements, and different separation structures may be used between those adjacent elements. In such a case, a proper signal may not be acquired.

Photoelectric conversion apparatus and imaging system having impurity concentration profile in a depth direction of the plural semiconductor regions


A self-aligned SiGe FinFET device features a relaxed channel region having a high germanium concentration. Instead of first introducing germanium into the channel and then attempting to relax the resulting strained film, a relaxed channel is formed initially to accept the germanium. In this way, a presence of germanium can be established without straining or damaging the lattice. Gate structures are patterned relative to intrinsic silicon fins, to ensure that the gates are properly aligned, prior to introducing germanium into the fin lattice structure. After aligning the gate structures, the silicon fins are segmented to elastically relax the silicon lattice. Then, germanium is introduced into the relaxed silicon lattice, to produce a SiGe channel that is substantially stress-free and also defect-free. Using the method described, concentration of germanium achieved in a structurally stable film can be increased to a level greater than 85%.

Technical Field
The present disclosure generally relates to techniques for fabricating an array of high performance FinFET devices.
Description of the Related Art
Advanced integrated circuits often feature strained channel transistors, silicon-on-insulator (SOI) substrates, FinFET structures, or combinations thereof, in order to continue scaling transistor gate lengths below 20 nm. Such technologies allow the channel length of the transistor to shrink while minimizing detrimental consequences such as current leakage and other short channel effects.
A FinFET is an electronic switching device in which a conventional planar semiconducting channel is replaced by a semiconducting fin that extends outward from the substrate surface. In such a device, the gate, which controls current flow in the fin, wraps around three sides of the fin so as to influence current flow from three surfaces instead of one. The improved control achieved with a FinFET design results in faster switching performance and reduced current leakage than is possible with a planar transistor. FinFETs are described in further detail in U.S. Pat. No. 8,759,874, and U.S. Patent Application Publication US2014/0175554, assigned to the same assignee as the present patent application.
Strained silicon transistors have been developed to increase mobility of charge carriers, i.e., electrons or holes, passing through a semiconductor lattice. Incorporating strain into the channel of a semiconductor device stretches the crystal lattice, thereby increasing charge carrier mobility in the channel so that the device becomes a more responsive switch. Introducing a compressive strain into a PFET transistor tends to increase hole mobility in the channel, resulting in a faster switching response to changes in voltage applied to the transistor gate. Likewise, introducing a tensile strain into an NFET transistor tends to increase electron mobility in the channel, also resulting in a faster switching response.
There are many ways to introduce tensile or compressive strain into transistors, for both planar devices and FinFETs. Such techniques typically entail incorporating into the device epitaxial layers of one or more materials having crystal lattice dimensions or geometries that differ slightly from those of the silicon substrate. The epitaxial layers can be made of doped silicon or silicon germanium (SiGe), for example. Such epitaxial layers can be incorporated into source and drain regions, into the transistor gate that is used to modulate current flow in the channel, or into the channel itself, which is a portion of the fin. For example, one way to introduce strain is to replace bulk silicon from the source and drain regions, or from the channel, with silicon compounds such as silicon germanium. Because Si—Ge bonds are longer than Si—Si bonds, there is more open space in a SiGe lattice. Electrons thus move more freely through a lattice that contains elongated Si—Ge and Ge—Ge bonds than through a lattice that contains shorter Si—Si bonds. The presence of germanium atoms having longer bonds tends to stretch the lattice, causing internal strain. Replacing silicon atoms with SiGe atoms can be accomplished, for example, during a controlled process of epitaxial crystal growth, in which a new SiGe crystal layer is grown from the surface of a bulk silicon crystal, while maintaining the same crystal structure of the underlying bulk silicon crystal. Alternatively, strain can be induced in the fin from below the device by using various types of SOI substrates. An SOI substrate features a buried insulator, typically a buried oxide layer (BOX) underneath the active area. SOI FinFET devices have been disclosed in patent applications assigned to the present assignee, for example, U.S. patent application Ser. No. 14/231,466, entitled "SOI FinFET Transistor with Strained Channel," which is hereby incorporated by reference in its entirety.

Method of using a sacrificial gate structure to make a metal gate FinFET transistor