Ucb Pharma, S.a.

Celltech R&d Limited

John Wyeth Brother, Limited

Celltech Therapeutics Limited

Ucb Biopharma Sprl

Barry John Langham

Daniel Christopher Brookings

Sarah Catherine Archibald

Jeremy Martin Davis

Graham John Warrellow

Rikki Peter Alexander

John Robert Porter

John Clifford Head

Janeen Marsha Linsley

Judi Charlotte Neuss

Martin Clive Hutchings

James Andrew Johnson

Roger Crossley

Alan C White

Robin G Shepherd

Timothy John Norman

Albert Opalko

Richard Jeremy Franklin

Andrew James Ratcliffe

Brian Woodside Hutchinson

Rachel Jane Cubbon

Julien Alistair Brown

James Thomas Reuberson

Joanna Rachel Quincey

Daniel James Ford

Mezher Hussein Ali

Peter J Meade

Manisha Naik

Joanna Rachel Thorne

Emma Louise Trown

Andrew Harry Parton

Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, 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. The compounds are of general formula (I): 

Quinoline derivatives as kinase inhibitors

A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.

Thieno-pyridine derivatives as MEK inhibitors

Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.

Bicyclic heteroaromatic derivatives of formula (1) are described: F(1) where: the dashed line joining A and C(R) is present and represents a bond and A is a &#x2014;N&#x2550; atom or a &#x2014;C(R)&#x2550; group, or the dashed line is absent and A is a &#x2014;N(R)&#x2014;, or &#x2014;C(R)(R)&#x2014; group; X is an &#x2014;O&#x2014;, &#x2014;S&#x2014; or substituted nitrogen atom or a &#x2014;S(O)&#x2014;, &#x2014;S(O)&#x2014; or &#x2014;NH-group; Y is a nitrogen or substituted carbon atom or a &#x2014;CH&#x2550; group; n is zero or the integer 1; Alkis an optionally substituted aliphatic or heteroaliphatic chain Lis a covalent bond or a linker atom or group; Cyis a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders. 

Bicyclic heteroaromatic derivatives

A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

Bicyclic heteroaromatic compounds as kinase inhibitors

A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

Thienopyridone derivatives as kinase inhibitors

A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 5-oxo-4,5-dihydro-1H-pyrrolo[3,2-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(R) is present and represents a bond and A is a &#x2014;N&#x2550; atom or a &#x2014;C(R)&#x2550; group, or the dashed line is absent and A is a &#x2014;N(R)&#x2014;, or &#x2014;C(R)(R)&#x2014; group; X is an &#x2014;O&#x2014;, &#x2014;S&#x2014; or substituted nitrogen atom or a &#x2014;S(O)&#x2014;, &#x2014;S(O)&#x2014; or &#x2014;NH-group; Y is a nitrogen or substituted carbon atom or a &#x2014;CH&#x2550; group; n is zero or the integer 1; Alkis an optionally substituted aliphatic or heteroaliphatic chain Lis a covalent bond or a linker atom or group; Cyis a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders. 

Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors

Compounds of formula (1) are described in which Rand Ris each independently a hydrogen atom or a group R, or Rand Rtogether form an oxo (&#x2550;O) or thio (&#x2550;S) group; X is a N atom or an optionally substituted CH group: Y is a &#x2014;O&#x2014; or &#x2014;S&#x2014; atom or &#x2014;SO&#x2014; or &#x2014;SO&#x2014; group or an optionally substituted &#x2014;CH&#x2014; or &#x2014;NH&#x2014; group with the proviso that when Rand Rtogether form an oxo (&#x2550;O) or thio (&#x2550;S) group Y is an optionally substituted &#x2014;CH&#x2014; or &#x2014;NH-group; Lis a covalent bond or a linker atom or group; p is zero or the integer 1; Alkis an optionally substituted Caliphatic or Cheteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted &#x2014;CH&#x2014; group; Ar is an optionally substituted Caromatic or Cheteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R, Rand Rare hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

Pyridine and pyrimidine derivatives

Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a &#x2014;N&#x2550; atom or a &#x2014;N(R)&#x2014;, &#x2014;C(R)&#x2550; or &#x2014;C(R)(R)&#x2014; group; R, Rand Ris each independently a hydrogen atom or an optionally substituted Calkyl group; X is an &#x2014;O&#x2014; or &#x2014;S&#x2014; atom or &#x2014;NH&#x2014; group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alkis an optionally substituted aliphatic or heteroaliphatic chain Lis a covalent bond or a linker atom or group; Cyis a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase mediated diseases or disorders, such as rheumatoid arthritis 

Bicyclic oxopyridine and oxopyrimidine derivatives

Enamine derivatives

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Reading, United Kingdom

Barry John Langham