发明名称 Caspase inhibitors and uses thereof
摘要 This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R<SUP>1 </SUP>is hydrogen, CHN<SUB>2</SUB>, R, or -CH<SUB>2</SUB>Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R<SUP>2 </SUP>is CO<SUB>2</SUB>H, CH<SUB>2</SUB>CO<SUB>2</SUB>H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R<SUP>3 </SUP>is hydrogen, an optionally substituted C<SUB>1-6 </SUB>alkyl, F<SUB>2</SUB>, CN, aryl or R<SUP>3 </SUP>is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0-2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.
申请公布号 US7053057(B2) 申请公布日期 2006.05.30
申请号 US20010863649 申请日期 2001.05.23
申请人 VERTEX PHARMACEUTICALS INCORPORATED 发明人 GOLEC JULIAN M. C.;BEBBINGTON DAVID;BRENCHLEY GUY;KNEGTEL RONALD;MORTIMORE MICHAEL
分类号 A61K38/05;A61K31/445;A61K31/453;A61K31/4545;A61K31/47;A61K31/472;A61K31/496;A61P1/04;A61P1/16;A61P1/18;A61P3/10;A61P5/14;A61P7/00;A61P7/04;A61P7/06;A61P9/00;A61P9/04;A61P9/10;A61P11/00;A61P11/06;A61P13/12;A61P17/00;A61P17/02;A61P17/04;A61P17/06;A61P17/14;A61P19/02;A61P19/08;A61P19/10;A61P21/00;A61P21/04;A61P25/00;A61P25/08;A61P25/14;A61P25/28;A61P25/32;A61P27/02;A61P29/00;A61P31/00;A61P31/04;A61P31/06;A61P31/12;A61P31/18;A61P31/20;A61P35/00;A61P35/02;A61P35/04;A61P37/06;A61P39/02;A61P41/00;A61P43/00;C07D211/60;C07D215/48;C07D217/26;C07D401/12;C07D409/12;C07K5/078 主分类号 A61K38/05
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