发明授权
- 专利标题: Caspase inhibitors and uses thereof
- 专利标题(中): 胱天蛋白酶抑制剂及其用途
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申请号: US09863649申请日: 2001-05-23
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公开(公告)号: US07053057B2公开(公告)日: 2006-05-30
- 发明人: Julian M. C. Golec , David Bebbington , Guy Brenchley , Ronald Knegtel , Michael Mortimore
- 申请人: Julian M. C. Golec , David Bebbington , Guy Brenchley , Ronald Knegtel , Michael Mortimore
- 申请人地址: US MA Cambridge
- 专利权人: Vertex Pharmaceuticals Incorporated
- 当前专利权人: Vertex Pharmaceuticals Incorporated
- 当前专利权人地址: US MA Cambridge
- 代理机构: Vertex Pharmaceuticals Incorporated
- 代理商 Lisa A. Dixon
- 主分类号: A61K38/05
- IPC分类号: A61K38/05 ; C07K5/078
摘要:
This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; 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; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 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.
公开/授权文献
- US20020061853A1 Caspase inhibtors and uses thereof 公开/授权日:2002-05-23
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