| 发明名称 |
CASPASE INHIBITORS AND USES THEREOF |
| 摘要 |
This invention provides compounds of formula (I): wherein Z is oxygen or sulfu; R1 is hydrogen, -CHN2, R, CH2OR, CH2SR, or -CH2Y; --- next to R3 represents a single or double bond; 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 or a caspase enzyme; R4 is hydrogen or C1-6alkyl or R3and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1.beta. secretion.
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| 申请公布号 |
CA2447999(C) |
申请公布日期 |
2011.04.26 |
| 申请号 |
CA20022447999 |
申请日期 |
2002.05.23 |
| 申请人 |
VERTEX PHARMACEUTICALS INCORPORATED |
发明人 |
MORTIMORE, MICHAEL;MILLER, ANDREW;STUDLEY, JOHN;CHARRIER, JEAN-DAMIEN |
| 分类号 |
A61K31/404;C07D209/86;A61K31/395;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;C07D209/08;C07D209/88;C07D221/06;C07D223/22;C07D241/46;C07D279/30;C07D403/12;C07D471/04;C07D471/14;C07D487/04;C07D495/04;C07D498/04;C07D513/04 |
主分类号 |
A61K31/404 |
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