abstract |
ABSTRACT COMPOUNDS Compounds of general formula I: (I) wherein: R1 represents a hydrogen atom or a C1-C6 alkyl, C1-C6 alkenyl, phenyl, phenyl(C1-C6)alkyl, C1-C6 alkyl-thiomethyl, phenylthiomethyl, substituted phenyl-thiomethyl, phenyl(C1-C6)alkylthiomethyl or heterocyclylthiomethyl group; or R1 represents -SRx wherein Rx represents a group ; R2 represents a hydrogen atom or a C1-C6 alkyl, C1-C6 alkenyl, phenyl(C1-C6)alkyl, cycloalkyl(C1-C6)alkyl, or cycloalkenyl(C1-C6)alkyl; R3 represents an amino acid residue with R or S stereochemistry or a C1-C6 alkyl, benzyl, (C1-C6)alkoxybenzyl or benzyloxy(C1-C6)alkyl group; R4 represents a hydrogen atom or a methyl group; n is an integer from 1 to 6; and A represents the group -NH2, a substituted acyclic amine or a heterocyclic base; or a salt and/or N-oxide and/or (where the compound is a thio-compound) a sulphoxide or sulphone thereof have collagenase inhibition activity and are useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumour invasion. |