Caspase inhibitors and uses thereof

Details Caspase inhibitors and uses thereof Caspase inhibitors and uses thereof

2006-05-30

2006-05-30

Russel, Jeffrey Edwin (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C435S001100, C435S002000, C435S374000, C546S146000, C546S147000, C546S164000, C546S169000, C546S170000, C546S226000

Reexamination Certificate

active

07053057

ABSTRACT:
This invention provides caspase inhibitors having the formula:wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3is hydrogen, an optionally substituted C1-6alkyl, F2, CN, aryl or R3is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.

REFERENCES:
patent: 5866545 (1999-02-01), Hagmann et al.
patent: 6045990 (2000-04-01), Baust et al.
patent: 6136834 (2000-10-01), Ohmoto et al.
patent: WO 91/15577 (1991-10-01), None
patent: WO 99/18781 (1999-04-01), None
patent: WO 99/47154 (1999-09-01), None

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