Importance

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Abstract

Compounds of formula (I) have matrix metalloproteinase inhibitory activity, wherein R.sub.2 represents a group R.sub.6 --A-- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R.sub.6 represents hydrogen or an optionally substituted phenyl, cycloalkyl or cycloalkenyl group; R.sub.3 represents a group R.sub.7 --(B).sub.n --wherein n is 0 or 1, B represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R.sub.7 is --CONHOH, carboxyl, esterified or amidated carboxyl, cycloalkyl, cycloalkenyl, heterocyclyl, phenyl, naphtyl, or substituted phenyl or naphtyl in which the substituent(s) are selected from phenyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, benzyloxy, or R.sub.8 --(C.dbd.O)--(C.sub.1 -C.sub.6 alkyl)--O-- wherein R.sub.8 is hydroxy, amino, or an amino acid residue linked via an amide bond; or (except when n=0) R.sub.7 is hydrogen; R.sub.4 represents hydrogen or methyl; R.sub.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl or a group D-(C.sub.1 -C.sub.6 alkyl) wherein D represents hydroxy, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylthio, acylamino, optionally substituted phenyl, or a heterocyclic group, NH.sub.2, or a mono- or di-(C.sub.1 -NC.sub.6 alkyl) amine or a heterocyclic group; or R.sub.3 and R.sub.5 taken together represent a divalent, saturated or unsaturated hydrocarbon chain of from 8-14 C atoms, which may be interrupted by an O, S or N heteroatom, or a salt, solvate or hydrate thereof, provided that R.sub.3 is not the characteristic side chain of a natural alpha-amino acid, or the characteristic side chain of a natural alpha-amino acid in which any functional substituents are protected, any amino groups are acylated, and any carboxyl groups are esterified.

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First Claim