Abstract:
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
Abstract translation:本发明提供了式I的半胱天冬酶抑制剂:其中Z是氧或硫; R 1是氢,-CHN 2,R 2,CH 2 OR,CH 2 SR或-CH 2 Y> Y; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US07442790-20081028-P00001.TIF“alt =”custom character“img-content =”character“img-format R 3和R 4之间的=“tif”/>表示单键或双键; Y是电负离子团; R 2是CO 2 H,CH 2 CO 2 H,或它们的酯,酰胺或等体醇; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4是氢或C 1-6烷基或R 3和R 4合在一起形成环 ; 环A和环B各自是杂环,R和R 5如说明书中所述。 这些化合物是凋亡和IL-1β分泌的有效抑制剂。
Abstract:
Images are analyzed by programmatic mechanisms for accessing one or more remote web pages to retrieve content on display at the remote web pages. The retrieved images may be analyzed to determine information about an object shown in a corresponding image of the content on display. At least a portion of the object shown in the corresponding image of the content on display may be made selectable and associated with the determined information. This determined information may subsequently be used, in for example, search applications.
Abstract:
In at least one aspect, the invention comprises constructing one or more hybrid adjustable rate mortgage aggregates based on one or more of: agency, program, coupon, and origination year; for each of one or more of the aggregates, constructing one or more sub-aggregates based on one or more of: rate-index, capitalization structure, and existence of interest-only feature; mapping pools of adjustable rate mortgages to the aggregates and sub-aggregates; constructing an index based on the mapping; and pricing the index.
Abstract:
A system and method is provided for synthesizing audio-visual content in a video image processor. A content synthesis application processor extracts audio features and video features from audio-visual input signals that represent a speaker who is speaking. The processor uses the extracted visual features to create a computer generated animated version of the face of the speaker. The processor synchronizes facial movements of the animated version of the face of the speaker with a plurality of audio logical units such as phonemes that represent the speaker's speech. In this manner the processor synthesizes an audio-visual representation of the speaker's face that is properly synchronized with the speaker's speech.
Abstract:
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract:
A catalyst and process for the production of acetic acid by the carbonylation of methanol and/or a reactive derivative thereof. The catalyst system comprises an iridium carbonylation catalyst, methyl iodide co-catalyst, optionally at least one of ruthenium, osmium, rhenium, zinc, gallium, tungsten, cadmium, mercury and indium and at least one non-hydrohalogenoic acid promoter. The non-hydrohalogenoic acid may be an oxoacid, a superacid and/or a heteropolyacid.
Abstract:
A rotor (14) is located within a rotor chamber (12) formed in a housing (24). A drive shaft (16) extends from a motor and couples to the drive shaft interconnect (46) at the center of the rotor (14). One side of the rotor (14) is provided with circumferentially spaced apart radial rows of mincing edges (20). These edges (20) are situated on concentric circles or on a spiral. They are elongated circumferentially and may be situated substantially on an arc and substantially on an arc or on a chord. During use, the rotor (14) is rotated after biopsy obtained tissue (10) has been placed in the rotor chamber (12) on the side of the rotor (14) that includes the mincing edges (20). A fluid is delivered into and out from the rotor chamber (12) as the rotor (14) is being rotated to mince the biopsy, lyse the cells, and release the cell nuclei from the obtained tissue. Cell nuclei are expelled from the chamber (12) and are moved through a filter (58). The cell nuclei are collected and then delivered to a flow cytometry apparatus to be analyzed.
Abstract:
This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2; and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Abstract translation:本发明描述了式IIIa的新型吡唑化合物:其中R 1是T环D,其中环D是5-7元单环或选自芳基,杂芳基,杂环基或碳环基的8-10元双环; R x,R y,R 2; 和R 2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂,特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症,糖尿病和阿尔茨海默病的疾病。
Abstract:
Genetic polymorphisms are identified in the human UGT2B4, UGT2B7 and UGT2B15 genes that alter UGT2B activity. Nucleic acids comprising the polymorphic sequences are used to screen patients for altered metabolism for UGT2B substrates, potential drug-drug interactions, and adverse/side effects, as well as diseases that result from environmental or occupational exposure to toxins. The nucleic acids are used to establish animal, cell and in vitro models for drug metabolism.
Abstract:
A plastic card transport apparatus and a plastic card inspection system. A group of lower support wheels is positioned with their circumferential surfaces aligned to define a card transport path having a plurality of card operation locations therealong. The wheels support a plastic card by its lower edge as the plastic card is transported along the card transport path from a first one of the card operation locations to a second one of the card operation locations. A drive source continuously drives selected ones of the lower support wheels to move the plastic card along the card transport path between card operation locations. A controller is responsive to a control signal to drive a selected one of the lower support wheel members, adjacent a first one of the card operation locations, to move the plastic card along the card transport path from that first one of the card operation locations to an adjacent one of the continuously driven lower support wheels, to transport the plastic card to a second one of the card operation locations. The plastic card inspection system includes such a plastic card transport apparatus to transport the plastic cards from a plastic card input location to a plastic card inspection location for inspection, and then to a plastic card output location selected on the basis of the inspection results. The cards are discharged to a tray having a fiber material on its side surfaces to align the cards as they are discharged.