British Biotech Pharmaceuticals Limited

Fionna Mitchell Martin

Mark Whittaker

Raymond Paul Beckett

Andrew Miller

Richard Simon Todd

Christopher Norman Lewis

Zoe Marie Spavold

Stephen Arthur Bowles

Philip Huxley

Compounds of formula (I) are matrix metalloprotemase inhibitors wherein X represents a carboxylic acid group &mdash;COOH, or a hydroxamic acid group &mdash;CONHOH;R represents a radical of formula (II): R &mdash;(ALK) &mdash;(Q) &mdash;(ALK) ., and W represents a cyclic amino radical of formula (IIIA) or (IIIB):

Hydroxamic acid derivatives as proteinase inhibitors

Metalloproteinase inhibitors

The present invention relates to therapeutically active hydroxamic acid, N-formyl-N-hydroxyamino and carboxylic acid derivatives, their preparation, and pharmaceutical compositions containing them. These compounds are useful in the inhibition of metalloproteases, such as stromelysin, gelatinase, matrilysin, and collagenase. These compounds are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

Succinyl hydroxamic acid, N-formyl-N-hydroxy amino carboxylic acid and

Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.

Preparation of allyl succinate derivatives and starting materials

The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.

Matrix metalloproteinase inhibitors

L-tert-leucine-2-pyridylamide or an acid addition salt thereof.

Compound of formula (I) ##STR1## wherein Ar represents an optionally substituted phenyl or heteroaryl group, m is 1 or 2, n is 0, 1, 2, 3 or 4, X represents --COOH or --CONHOH and R.sub.1, R.sub.3 and Y are as defined in the specification,are inhibitors of metalloproteinases involved in tissue degradation.

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Oxford, United Kingdom

Fionna Mitchell Martin