Caspase inhibitors and uses thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C544S252000, C544S251000, C544S250000, C544S249000, C544S234000, C514S248000

Reexamination Certificate

active

07407964

ABSTRACT:
This invention provides novel caspase inhibitors of formula I:wherein R1is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3is independently selected from hydrogen or C1-6aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4alkyl, or C1-4alkoxy. The compounds are useful for treating caspase-mediated diseases.

REFERENCES:
patent: WO 95/33751 (1995-12-01), None
patent: WO 95/35308 (1995-12-01), None
patent: WO 98/11109 (1998-03-01), None
Wolft Manfred E. “Burger's Medicinal Chemistry, 5ed, Part 1”, John Wiley & Sons, 1995, pp. 975-977.
Banker, G.S. et al, “Modern Pharmaceutices, 3ed.”, Marcel Dekker, New York. 1996, pp. 451 and 596.

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