Smithkline Beecham Corporation

Glaxo Group Limited

Smithkline Beechum P.l.c.

David Kenneth Dean

Andrew Kenneth Takle

David Matthew Wilson

Mark James Bamford

Antoinette Naylor

Jason Witherington

Daryl Simon Walter

Lee James Beeley

Sanjeet Singh Sehmi

Giancarlo Trani

Jorge Munoz-Muriedas

Rachel Elizabeth Anne Thewlis

Jon Graham Anthony Steadman

Mairi Sime

Mervyn Thompson

Paul John Beswick

Robert William Ward

Ian David Wall

Nigel Paul King

Robert James Gleave

John Michael Berge

Nikesh R Kotecha

Susan Roomans

Alessandra Gaiba

Peter John Lovell

Andrew Peter Moses

Laura J Chambers

David John Davies

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, Calkyl, Ccycloalkyl, Calkoxy, Calkoxy Calkyl, Cfluoroalkyl, halogen, NRR, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R, R, R, R, R, Rand Rare as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.

5,6,7,8-tetrahydroimidazo[1,2-A]pyrazine derivatives as P2X7 modulators

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, Calkyl, Ccycloalkyl, Calkoxy, Calkoxy Calkyl, Cfluoroalkyl, halogen, NRR, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R, R, R, R, R, Rand Rare as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators

The present invention relates to novel benzazepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Benzazepine derivatives for the treatment of neurological disorders

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

Imidazolidine carboxamide derivatives as P2X7 modulators

Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.

Pyridine derivatives as Raf kinase inhibitors

Pyridylfurans and pyrroles as Raf kinase inhibitors

The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, Rand Y are as defined in the specification. The compounds are partial or full agonists at the growth hormone secretagogue (GHS) receptors. Pharmaceutical compositions comprising the compounds methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.

Piperazine derivatives useful for the treatment of gastrointestinal disorders

Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CHCO, S or NH, or the moiety X&#x2014;Ris hydrogen; Yand Yindependently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of Xand Xis selected from O, S or NRand the other is CH, wherein Ris hydrogen, Calkyl, aryl or arylCalkyl.

Pyridine substituted furan derivatives as Raf kinase inhibitors

Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors

The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, use as Raf Kinase Inhibitors and treatment methods for neurotraumatic diseases and cancer.

Imidazole-2-carboxamide derivatives as Raf kinase inhibitors

Novel compounds (I) and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy wherein Ar is a group of formula a) or b).

Imidazole derivatives as Raf kinase inhibitors

Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Pleuromutilin derivatives with antimicrobial activity

Compounds of formula (I) wherein X is O, CH, S or NH, or the moiety X&#x2014;Ris hydrogen; V is CH or N; Y is NRR, NRC(Z)NRR, NRCOORor NRSOR; Ar is phenyl or a 5- or 6-membered heteroaryl ring either of which may be optionally substituted; n is 0, 1, 2, 3 or 4; and R, R, R, R, Rand Rhave the meanings given in the description; and pharmaceutically acceptable salt thereof.

Compounds

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Harlow, United Kingdom

David Kenneth Dean