Ucb Pharma, S.a.

Celltech R&d Limited

Smithkline Beecham Corporation

Stuart Bailey

Stephen Brand

Julien Alistair Brown

John Robert Porter

John Clifford Head

James Andrew Johnson

Derek R Buckle

Rikki Peter Alexander

Daniel Christopher Brookings

Alan Findlay Haughan

Andrew Sharpe

Timothy John Norman

Christopher Lowe

David Glynn Smith

Andrew Faller

William Ross Pitt

Stephen Robert Mack

Pavandeep Singh Aujla

Marianna Dilani Richard

Laura Jane Tait

Natasha Kinsella

A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Fused thiophene derivatives as kinase inhibitors

Phenylalanine enamide derivatives of formula (1) are described: wherein in which R is a carboxylic acid (&#x2014;COH) or a derivative or biostere thereof; The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

Phenylalanine enamide derivatives

Phenylalanine enamide derivatives of formula (1) are described:   The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

Compounds of formula (1) are described: in which X is an &#x2014;O&#x2014; or &#x2014;S&#x2014; atom or &#x2014;N(R)&#x2014; group and Ris a group ArLArAlk- in which Aris an optionally substituted aromatic or heteroaromatic group, Lis a covalent bond or a linker atom or group, Aris an optionally substituted bicyclic heteroarylene group and Alk is a chain &#x2014;CH&#x2014;CH(R)&#x2014;, &#x2014;CH&#x2550;C(R)&#x2014;, OR&#x2014;CH(CHR)&#x2014; in which R is a carboxylic acid (&#x2014;COH) or a derivative or biostere thereof. The compounds are selective inhibitors of alpha 4 integrins such as &#x3b1;&#x3b2;and are of use in modulating cell adhesion for the prophylaxis or treatment of inflammatory diseases or disorders, such as rheumatoid arthritis, in which the extravasculation of leukocytes plays a role. 

Bicyclic heteroaromatic alanines

Phenylalanine enamide derivatives of formula (1) are described:wherein The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

Phenylalanine enamide derivatives of formula (1) are described:wherein Ris a &#x2014;CH, &#x2014;(CH)CH, &#x2014;CHCHOH, &#x2014;CHCHOCH, &#x2014;CHCHOCHCHOH, &#x2014;CHCHOCHCHOCH,group;and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of &#x3b1;4 integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.

Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.

Inhibitors of the production of S-CD23 and the secretion of TNF

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Dorking, United Kingdom

Stuart Bailey