发明名称 Carbamate caspase inhibitors and uses thereof
摘要 This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R<SUP>1</SUP>is hydrogen, -CHN<SUB>2</SUB>, R, CH<SUB>2</SUB>OR, CH<SUB>2</SUB>SR, or -CH<SUB>2</SUB>Y; Y is an electronegative leaving group; R<SUP>2 </SUP>is CO<SUB>2</SUB>H, CH<SUB>2</SUB>CO<SUB>2</SUB>H, or esters, amides or isosteres thereof; R<SUP>3 </SUP>is a group capable of fitting into the S2 subsite of a caspase enzyme; R<SUP>4 </SUP>and R<SUP>5 </SUP>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-1beta secretion.
申请公布号 AU4961901(A) 申请公布日期 2001.10.08
申请号 AU20010049619 申请日期 2001.03.29
申请人 VERTEX PHARMACEUTICALS INCORPORATED 发明人 DAVID BEBBINGTON;JEAN-DAMIEN CHARRIER;DAVID KAY;RONALD KNEGTEL;JULIAN GOLEC;MICHAEL MORTIMORE;JOHN STUDLEY
分类号 A61K31/403;A61K31/404;A61K31/473;A61K31/496;A61K31/5415;A61K31/55;A61K31/575;A61P9/00;A61P19/02;A61P19/08;A61P25/32;A61P29/00;A61P31/04;A61P31/12;A61P35/00;A61P37/06;A61P43/00;C07D209/04;C07D209/08;C07D209/82;C07D209/86;C07D221/12;C07D223/22;C07D223/26;C07D223/28;C07D279/30;C07D279/36;C07D403/12;C07J9/00 主分类号 A61K31/403
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