カスパーゼインヒビターおよびそれらの使用

Japanese Patent JP2004531558

A

This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 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 of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and 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-1β secretion.

Mortymore, Michael
Mirror, andrew
Studley, John
Charliers, Jean-Damien

JP2002590980A

October 14, 2004

May 23, 2002

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VERTEX PHARMACEUTICALS INCORPORATED

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; (IPC1-7): C07D209/86; A61K31/404; A61P1/04; A61P1/16; A61P1/18; A61P3/10; A61P7/06; A61P9/10; A61P11/00; A61P11/06; A61P13/12; A61P17/06; A61P19/02; A61P19/08; A61P19/10; A61P21/04; A61P25/08; A61P25/14; A61P25/16; A61P25/28; A61P29/00; A61P31/04; A61P31/12; A61P31/18; A61P35/00; A61P37/02; A61P37/06; A61P37/08; A61P39/02

Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita

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