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US 5,514,677 AGranted
Hydroxamic acid based collagenase inhibitors
AssigneeBritish Biotech Pharmaceuticals Limited
InventorsAlan H. Davidson, Jonathan P. Dickens, Michael J. Crimmin
Life of this patent
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Abstract
Compounds of general formula I: ##STR1## wherein: A represents the group --NH.sub.2, a substituted acyclic amine or a heterocyclic base; 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.
Claims8
A compound of general formula IV wherein:
- ##STR67## R.sup.1 represents a hydrogen atom;
- R.sup.2 represents a C.sub.3 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6) alkyl, cycloalkyl (C.sub.1 -C.sub.6) alkyl, or cycloalkenyl (C.sub.1 -C.sub.6)alkyl;
- R.sup.3 represents a hydrogen, para-hydroxybenzyl, hydroxymethyl, 1-hydroxyethyl, HSCH.sub.2, CH.sub.3 SCH.sub.2 CH.sub.2, NH.sub.2 COCH.sub.2, NH.sub.2 COCH.sub.2 CH.sub.2, NH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2, NH.sub.2 C(NH)NHCH.sub.2 CH.sub.2 CH.sub.2, (COOH)CH.sub.2 CH.sub.2, (COOH)CH.sub.2, ##STR68## C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6)alkoxybenzyl, benzyloxy(C.sub.1 -C.sub.6)alkyl or benzyloxy benzyl group;
- R.sup.4 represents a hydrogen atom or a methyl group;
- n is an integer from 1 to 6;
- and
- A represents the group --NH.sub.2, a substituted acyclic amine of the form --N(R.sup.A)R.sup.B, wherein one of R.sup.A and R.sup.B is a C.sub.1 -C.sub.6 alkyl group and the other is hydrogen or a C.sub.1 -C.sub.6 alkyl group or A represents the group pyridyl, imidazolyl, oxazolyl, thiazolyl, benzthiazolyl, benzoxazolyl, morpholinyl, pyrrolininyl or piperidinyl;
- or a salt or N-oxide thereof.
5 more elements
Dependencies are inferred from the claim text.