Pyridazines as interleukin-1.beta.-converting enzyme inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 237/24 (2006.01) A61K 31/50 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07D 401/02 (2006.01) C07D 401/04 (2006.01) C07D 403/02 (2006.01) C07D 403/04 (2006.01) C07D 405/02 (2006.01) C07D 409/02 (2006.01) C07D 413/02 (2006.01) C07D 417/02 (2006.01) C07F 9/547 (2006.01)

Patent

CA 2125359

ABSTRACT Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: Image (I) wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(=O)NH(CHR5)m-COOR5, NH(CHR5)mCON(R5)R6 C(=O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R 4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m = 0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta. protease activity in a mammal utilizing the compounds and compositions.

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