发明名称 |
CASPASE INHIBITORS AND USES THEREOF |
摘要 |
This invention provides compounds of formula (I): wherein Z is oxygen or sulfu; R<1> is hydrogen, -CHN2, R, CH2OR, CH2SR, or -CH2Y; --- next to R<3> represents a single or double bond; Y is an electronegative leaving group; R<2> is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R<3> is a group capable of fitting into the S2 subsite or a caspase enzyme; R<4> is hydrogen or C1-6alkyl or R<3>and R<4> taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R<5> are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1 beta secretion. |
申请公布号 |
WO02094263(A3) |
申请公布日期 |
2003.03.27 |
申请号 |
WO2002US16353 |
申请日期 |
2002.05.23 |
申请人 |
VERTEX PHARMACEUTICALS INCORPORATED;MORTIMORE, MICHAEL;MILLER, ANDREW;STUDLEY, JOHN;CHARRIER, JEAN-DAMIEN |
发明人 |
MORTIMORE, MICHAEL;MILLER, ANDREW;STUDLEY, JOHN;CHARRIER, JEAN-DAMIEN |
分类号 |
A61K31/404;A61K31/4015;A61K31/403;A61K31/407;A61K31/435;A61K31/45;A61K31/498;A61K31/5025;A61K31/538;A61K31/54;A61K31/55;A61P1/00;A61P1/04;A61P1/16;A61P1/18;A61P3/00;A61P3/10;A61P7/00;A61P7/06;A61P9/00;A61P9/10;A61P11/00;A61P11/06;A61P13/00;A61P13/12;A61P17/00;A61P17/06;A61P19/00;A61P19/02;A61P19/08;A61P19/10;A61P21/00;A61P21/04;A61P25/00;A61P25/08;A61P25/14;A61P25/16;A61P25/28;A61P27/00;A61P29/00;A61P31/00;A61P31/04;A61P31/12;A61P31/18;A61P35/00;A61P37/00;A61P37/02;A61P37/06;A61P37/08;A61P39/02;A61P43/00;C07D209/86 |
主分类号 |
A61K31/404 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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