Title:
CARBAMATE CASPASE INHIBITORS AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO2001072707
Kind Code:
A3
Abstract:
This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R<1> is hydrogen, -CHN2,R, CH2OR, CH2SR, or -CH2Y; 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 of a caspase enzyme; R<4> and R<5> 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.
Inventors:
BEBBINGTON DAVID (GB)
CHARRIER JEAN-DAMIEN (GB)
KAY DAVID (GB)
KNEGTEL RONALD (GB)
GOLEC JULIAN (GB)
MORTIMORE MICHAEL (GB)
STUDLEY JOHN (GB)
CHARRIER JEAN-DAMIEN (GB)
KAY DAVID (GB)
KNEGTEL RONALD (GB)
GOLEC JULIAN (GB)
MORTIMORE MICHAEL (GB)
STUDLEY JOHN (GB)
Application Number:
PCT/US2001/010182
Publication Date:
May 23, 2002
Filing Date:
March 29, 2001
Export Citation:
Assignee:
VERTEX PHARMA (US)
BEBBINGTON DAVID (GB)
CHARRIER JEAN DAMIEN (GB)
KAY DAVID (GB)
KNEGTEL RONALD (GB)
GOLEC JULIAN (GB)
MORTIMORE MICHAEL (GB)
STUDLEY JOHN (GB)
BEBBINGTON DAVID (GB)
CHARRIER JEAN DAMIEN (GB)
KAY DAVID (GB)
KNEGTEL RONALD (GB)
GOLEC JULIAN (GB)
MORTIMORE MICHAEL (GB)
STUDLEY JOHN (GB)
International Classes:
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; (IPC1-7): C07D209/86; A61K31/395; A61P43/00; C07D209/88; C07D209/08; C07D279/30; C07D221/12; C07D223/22; C07D403/12
Domestic Patent References:
| WO1998016505A1 | 1998-04-23 | |||
| WO1999018781A1 | 1999-04-22 |
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