Title:
【発明の名称】カスパーゼインヒビターおよびその使用
Document Type and Number:
Japanese Patent JP2003535865
Kind Code:
A
Abstract:
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.
Inventors:
Charliers, Jean-Damien
Bren Klee, Guy
Bren Klee, Guy
Application Number:
JP2002501900A
Publication Date:
December 02, 2003
Filing Date:
June 05, 2001
Export Citation:
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
International Classes:
A61K31/4745; A61K31/5025; 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; (IPC1-7): C07D455/04; A61K31/4745; A61K31/5025; 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; C07D471/04; C07D487/04; C07D487/14
Domestic Patent References:
| JPH10501244A | 1998-02-03 | |||
| JPH10504285A | 1998-04-28 | |||
| JP2000501428A | 2000-02-08 | |||
| JPS588082A | 1983-01-18 |
Foreign References:
| WO2000002903A1 | 2000-01-20 | |||
| WO1998016502A1 | 1998-04-23 | |||
| WO1998016505A1 | 1998-04-23 |
Attorney, Agent or Firm:
Shusaku Yamamoto (2 outside)