发明名称 CASPASE INHIBITORS AND USES THEREOF
摘要 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; R3 is 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-1&bgr; secretion.
申请公布号 US2011144074(A1) 申请公布日期 2011.06.16
申请号 US201113012180 申请日期 2011.01.24
申请人 VERTEX PHARMACEUTICALS INCORPORATED 发明人 MORTIMORE MICHAEL;MILLER ANDREW;STUDLEY JOHN;CHARRIER JEAN-DAMIEN
分类号 A61K31/404;A61K31/58;A01N1/02;A61K31/4015;A61K31/403;A61K31/405;A61K31/407;A61K31/435;A61K31/437;A61K31/45;A61K31/473;A61K31/496;A61K31/498;A61K31/5025;A61K31/538;A61K31/54;A61K31/5415;A61K31/55;A61P1/00;A61P1/04;A61P1/16;A61P1/18;A61P3/00;A61P3/10;A61P7/00;A61P7/06;A61P9/00;A61P9/10;A61P11/00;A61P11/06;A61P13/00;A61P13/12;A61P17/00;A61P17/06;A61P19/00;A61P19/02;A61P19/08;A61P19/10;A61P21/00;A61P21/04;A61P25/00;A61P25/08;A61P25/14;A61P25/16;A61P25/28;A61P27/00;A61P29/00;A61P31/00;A61P31/04;A61P31/12;A61P31/18;A61P35/00;A61P37/00;A61P37/02;A61P37/06;A61P37/08;A61P39/02;A61P43/00;C07D209/86;C12N5/071 主分类号 A61K31/404
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