发明授权
- 专利标题： Carbamate caspase inhibitors and uses thereof
- 专利标题（中）： 氨基甲酸酯半胱天冬酶抑制剂及其用途
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申请号： US10645043申请日： 2003-08-21
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公开(公告)号： US07074782B2公开(公告)日： 2006-07-11
- 发明人: David Bebbington , Ronald Knegtel , Michael Mortimore , David Kay , Julian M. C. Golec
- 申请人： David Bebbington , Ronald Knegtel , Michael Mortimore , David Kay , Julian M. C. Golec
- 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 Michael C. Badia; Lisa A. Dixon
- 主分类号： C07D223/18
- IPC分类号： C07D223/18 ; C07D279/36 ; C07D405/00 ; C07D221/12 ; A61K31/55
摘要：
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; 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 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
公开/授权文献
- US20040053920A1 Carbamate caspase inhibitors and uses thereof 公开/授权日：2004-03-18
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