Thiol-carboxylic acid derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 323/41 (2006.01) A61K 31/22 (2006.01) C07C 327/30 (2006.01) C07D 209/20 (2006.01) C07D 295/185 (2006.01) C07K 5/06 (2006.01)

Patent

CA 1322073

ABSTRACT Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: Image (I) in which R1 is hydroxy; alkoxy; aryloxy; aralkyloxy; -NR6R7 where R6 and R7 are hydrogen or alkyl, or R6 and R7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; -NHCH(R8)COR9 where R8 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, -NR6R7, quanidine, CO2H, CONH2, SH, or S-alkyl; or CH2-AR where Ar is optionally substituted aryl; and R9 is hydroxy, alkoxy or -NR6R7. R2 is hydrogen or acyl. R3 is C3-6 alkyl. R4 is hydrogen; alkyl; -CH2R10 where R10 is optionally substituted phenyl or heteroaryl; or -CH(R12)O-R11 where R11 is hydrogen; alkyl; or -CH2Ph where Ph is optionally substituted phenyl; and R12 is hydrogen or alkyl. R5 is hydrogen; alkyl; or -CH(R13)COR14 where R13 is hydrogen or alkyl; and R14 is hydroxy, alkoxy or -NR6R7.

555081

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