| abstract |
The present invention relates to compounds of general formula for use as a caspase inhibitor, wherein R 1 is hydrogen, cyano, -CHN 2, R or -CH 2 Y; R is an optionally substituted aliphatic or aromatic group or a non-aromatic heterocyclic group; Y is a leaving group or -OR, -SR, -OC = O (R), or -OPO (R8) (R9); R 2 is carboxy, carboxymethyl, esters, amides or isosteres thereof; R 3 is hydrogen or alkyl: ring A contains a double bond, optionally fused to and optionally substituted with another ring; X1 and X3 are nitrogen or carbon, X2 is a bond, oxygen, sulfur, nitrogen or carbon, and any X is optionally substituted, provided that when X3 is substituted, its substituent is attached via a non-nitrogen atom; at least one x nitrogen; when R2 is carboxyl, X2 is methylene, and R1 is CH2Y, it is not Y-OC (= O) R; and when R 2 is carboxyl, X 2 is methylidene, R 3 is hydrogen, and R 1 is other than R -CH 2 -NHSO 2 (alkyl) - and -CH 2 -NHSO 2 - (cycloalkyl) - and a process for their preparation. The invention relates to pharmaceutical compositions containing the compounds and their use. SHE |