Glaxo Group Limited

Daryl Simon Walter

David Kenneth Dean

Robert James Gleave

Giancarlo Trani

Jon Graham Anthony Steadman

Rachel Elizabeth Anne Thewlis

Mairi Sime

Jorge Munoz-Muriedas

Alan Naylor

Paul John Beswick

Emmanuel Hubert Demont

Steven James Stanway

Ian David Wall

David Robert Vesey

Stefan Senger

Peter Henry Milner

Andrew Faller

David Timothy Macpherson

Susan Roomans

David George Hubert Livermore

Laura J Chambers

Andrew Peter Moses

Sally Redshaw

Laura Jane 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 oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.

Receptor antagonists and their methods of use

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: Rrepresents hydrogen, halogen, Calkyl, Carylmethyl-, Calkenyl, Calkynyl or Ccycloalkylmethyl-; and any of said Calkyl, Carylmethyl-, Calkenyl, Calkynyl or Ccycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and Rrepresents hydrogen, fluorine or methyl;or Rand Rtogether with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of Calkyl, Calkenyl and Calkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.

Pyrrole and isoindole carboxamide derivatives as P2X7 modulators

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

The present invention relates to novel hydroxyethylamine compounds having Asp2 (&#x3b2;-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated &#x3b2;-amyloid levels or &#x3b2;-amyloid deposits, particularly Alzheimer's disease.

Hydroxyethylamine derivatives for the treatment of Alzheimer's disease

Growing community of inventors

Harlow, United Kingdom

Daryl Simon Walter