To provide a new compound useful as a caspase inhibitor and its pharmaceutically acceptable derivative.
The compound is expressed by general formula (I): where R1 is hydrogen, CN, CHN2, R or -CH2Y; R is an aliphatic group, substituted aliphatic group, aryl, substituted aryl, aralkyl, substituted aralkyl, nonaromatic heterocyclic group or substituted nonaromatic heterocyclic group; Y is an electronegative leaving group, -OR, -SR, -OC=O(R) or -OPO(R8)(R9); R8 and R9 are each independently selected from R and OR; R2 is CO2H, CH2CO2H, an ester, an amide or its isostere; R3 is hydrogen, a C1-6 straight-chain alkyl or C1-6 branched-chain alkyl; and ring A contains 0-2 double bonds, X groups are each independently selected from nitrogen and carbon, at least one X in the ring A is nitrogen, and ring A is as necessary substituted in a described manner and condensed with saturated or unsaturated 5 to 7-membered ring containing 0-3 heteroatoms, provided that when X3 is carbon, the substituent on X3 is an atom other than nitrogen.
CHARIFSON PAUL
CHARRIER JEAN-DAMIEN
BINCH HAYLEY
Takaaki Yasumura
Natsuki Morishita
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