Caspase inhibitors and uses thereof

Details Caspase inhibitors and uses thereof Caspase inhibitors and uses thereof

2011-01-25

2011-01-25

Sullivan, Daniel M (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C540S586000, C544S102000, C544S234000, C544S347000, C544S372000, C544S034000, C546S108000, C546S243000, C546S082000, C546S087000, C548S441000, C548S543000

Reexamination Certificate

active

07875712

ABSTRACT:
This invention provides caspase inhibitors of formula I:wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3and R4represents 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: 2003/0232846 (2003-12-01), Golec et al.
patent: WO 98/16502 (1997-10-01), None
patent: 98/16502 (1998-04-01), None
patent: 99/56765 (1999-11-01), None
patent: 01/72707 (2001-10-01), None

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