Glaxo Group Limited

Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Stephen Barry Guntrip

George Stuart Cockerill

Kathryn Jane Smith

Malcolm Clive Carter

Brian Edgar Looker

Keith Biggadike

Panayiotis Alexandrou Procopiou

Diane Mary Coe

Karen Elizabeth Lackey

Rajnikant Patel

Dean David Edney

Rebecca Jane Moore

Michael John Monteith

Abigail Halton

Julie Nicole Hamblin

Paul Spencer Jones

Alan T Hudson

Colin David Eldred

Michael David Barker

Karl Witold Franzmann

Alison Judith Redgrave

Christopher James Lunniss

Brian Evans

Ian Robert Baldwin

Paul Barraclough

Michael David Woodrow

Sadie Vile

Anthony William Dean

Stuart Holman

John Edward Robinson

Martin John Page

Tracy Jane Redfern

Alan Michael Chapman

Rita Field

Mika Kristian Lindvall

Sharon Lisa Gough

Stephen Carl McKeown

There are provided according to the invention novel compounds of formula (I)  or pharmaceutically acceptable salts thereof, wherein R, RRRand Rare as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Quinoline derivatives as phosphodiesterase inhibitors

The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Methods using phenethanolamine derivatives for treatment of respiratory diseases

The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Phenethanolamine derivative for the treatment of respiratory diseases

Phenethanolamine derivatives for treatment of respiratory diseases

A process for the preparation of a compound of formula (I) comprising the steps:  

Heterocyclic compounds

The present invention relates to novel compounds of formula (I), to a process for their menufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases

Formailide derivatives as beta2-adrenoreceptor agonists

Substituted heteroaromatic compounds, and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR and V is N; or Y is N and V is CR ; or Y is CR and V is CR ; or Y is CR and V is CR ; R represents a group CH SO CH CH NHCH &mdash;Ar&mdash;, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C alkyl or C alkoxy groups; R is selected from the group comprising hydrogen, halo, hydroxy, C alkyl, C alkoxy, C alkylamino and di&lsqb;C alkyl&rsqb;amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R group and optionally substituted by at least one independently selected R group; R is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R represents a group of formula (a) wherein each R is independently selected from halogen, C alkyl, C alkoxy; and n is 0 to 3; each R is independently hydroxy, halogen, C alkyl, C alkenyl, C alkynyl, C alkoxy, amino, C alkylamino, di&lsqb;C alkyl&rsqb;amino, C alkylthio, C alkylsulphinyl, C alkylsulphonyl, C alkylcarbonyl, carboxy, carbamoyl, C alkoxycarbonyl, C alkanoylamino, N-(C alkyl)carbamoyl, N,N-di(C alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O) , wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O) atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O) , wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R group and is optionally substituted by at least one independently selected R group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Protein tyrosine kinase inhibitors

The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.

Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH ), (CH )W, or W, in which W is O, S(O) wherein m is 0, 1 or 2, or NR wherein R is hydrogen or a C alkyl group; R represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O) , wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O) atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R being optionally substituted by one or more R ;groups; P&equals;0 to 3; U, R , R are as defined in the application.

Fused heterocyclic compounds as protein tyrosine kinase inhibitors

Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds in which one ring is a pyridine or pyrimidine of formula (I) are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O),, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O),atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O),, wherein m is 0, 1 or 2 and wherein the ring system is substituted by at least one independently selected R,group and is optionally substituted by at least one independently selected R,group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Growing community of inventors

Stevenage, United Kingdom

Stephen Barry Guntrip