Caspase inhibitors and uses thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C514S210200, C514S231500, C514S245000, C514S253130, C514S254010, C514S330000, C514S423000, C554S080000

Reexamination Certificate

active

10153971

ABSTRACT:
This invention provides compounds of formula I:wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y;next to R3represents a single or double bond; Y is an electronegative leaving group; R2is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4is a hydrogen or C1-6alkyl or R3and R4taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.

REFERENCES:
patent: 6800619 (2004-10-01), Charrier et al.
patent: WO98/16502 (1998-04-01), None
patent: WO99/56765 (1999-11-01), None
patent: WO 01/72707 (2001-10-01), None

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