发明名称 Caspase Inhibitors and Uses Thereof
摘要 This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
申请公布号 US2011003824(A1) 申请公布日期 2011.01.06
申请号 US20100883424 申请日期 2010.09.16
申请人 VERTEX PHARMACEUTICALS INCORPORDTED 发明人 CHARRIER JEAN-DAMIEN;BRENCHLEY GUY
分类号 A61K31/5025;A01N1/02;A61K31/437;A61K31/4745;A61K31/519;A61P1/04;A61P1/16;A61P1/18;A61P3/10;A61P5/14;A61P7/00;A61P7/04;A61P7/06;A61P7/08;A61P9/00;A61P9/04;A61P9/10;A61P11/06;A61P11/16;A61P13/12;A61P17/00;A61P17/02;A61P17/06;A61P17/14;A61P19/02;A61P19/08;A61P19/10;A61P21/00;A61P21/04;A61P25/00;A61P25/08;A61P25/14;A61P25/16;A61P25/28;A61P25/32;A61P27/02;A61P29/00;A61P31/00;A61P31/04;A61P31/06;A61P31/12;A61P31/14;A61P31/18;A61P31/20;A61P35/00;A61P35/02;A61P37/02;A61P37/06;A61P37/08;A61P43/00;C07D455/04;C07D471/04;C07D487/04;C07D487/14;C12N5/071 主分类号 A61K31/5025
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