PYRIDAZINES AS INTERLEUKIN-1BETA CONVERTING ENZYME INHIBITORS.

摘要

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is halogen, oxygen linked leaving group including aromatic ether, aromatic ester, alkyl sulfonate, aryl sulfonate, alkyl phosphonate, aryl phosphonate, alkyl phosphate or aryl phosphate; R2 is OR5, NH(CHR5)m-COOR5, NH(CHR5)mCON(R5)R6, N(R5)R6 or NH(CHR5)nOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl or lower cycloalkyl; m = 1-6; and n = 2-6. pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1 beta protease activity in a mammal utilizing the compounds and compositions.