发明公开
- 专利标题: Carbamate caspase inhibitors and uses thereof
- 专利标题(中): 氨基甲酸酯衍生物如胱天蛋白酶抑制剂及其使用
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申请号: EP08001070.5申请日: 2001-03-29
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公开(公告)号: EP1923386A3公开(公告)日: 2008-05-28
- 发明人: Charrier, Jean-Damien , Bebbington, David , Kay, David , Knegtel, Ronald , Golec, Julian , Mortimore, Michael , Studley, John
- 申请人: Vertex Pharmceuticals Incorporated
- 申请人地址: 130 Waverly Street Cambridge, MA 02139-4242 US
- 专利权人: Vertex Pharmceuticals Incorporated
- 当前专利权人: Vertex Pharmceuticals Incorporated
- 当前专利权人地址: 130 Waverly Street Cambridge, MA 02139-4242 US
- 代理机构: Vossius & Partner
- 优先权: US192826P 20000329
- 主分类号: C07D209/86
- IPC分类号: C07D209/86 ; A61K31/395 ; A61P43/00 ; C07D209/88 ; C07D209/08 ; C07D279/30 ; C07D221/12 ; C07D223/22 ; C07D403/12
摘要:
This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R is hydrogen, -CHN2,R, CH2OR, CH2SR, or -CH2Y; Y is an electronegative leaving group; R is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R is a group capable of fitting into the S2 subsite of a caspase enzyme; R and R 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-1 beta secretion.
公开/授权文献
- EP1923386A2 Carbamate caspase inhibitors and uses thereof 公开/授权日:2008-05-21
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