Hydroxamic acid based collagenase inhibitors

专利名称：Hydroxamic acid based collagenase

inhibitors

发明人：Colin Campion,Alan H. Davidson,Jonathan P.

Dickens,Michael J. Crimmin

申请号：US08/195818申请日：19940214公开号：US05530161A公开日：19960625

摘要：Compounds of general formula I: ##STR1## wherein: R.sup.1 represents aC.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C. sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6) alkylcarbonyl phenacyl or substitutedphenacyl group; or, when n=O, R.sup. 1 represents SR.sup.x, wherein R.sup.x represents agroup: ##STR2## R.sup. 2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1-C.sub. 6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6) alkyl orcycloalkenyl(C.sub.1 -C.sub.6)alkyl group;

R. sup.3 represents an amino acid residue with R or S stereochemistry or a C. sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C. sub.1 -C.sub.6 alkyl)group;

R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;

< P>R.sup.5 represents a hydrogen atom or a methyl group;

< P>n is an integer having the value 0, 1 or 2; and

A represents a C. sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or

more C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl groups;

< P>and their salts and N-oxides are collagenase inhibitors are and useful in themanagement of disease involving tissue degradation and/or the promotion of woundhealing. Diseases involving tissue degradation include arthropathy (particularly

rheumatoid arthritis) , inflammation, dermatological diseases, bone resorption diseasesand tumor invasion.

申请人：BRITISH BIO-TECHNOLOGY LIMITED

代理机构：Banner & Allegretti, Ltd.

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