Novartis Ag

Emma Budd

Catherine Howsham

Lee Edwards

Kamlesh Jagdis Bala

Katrin Spiegel

Glyn Alan Hughes

Urs Baettig

Ian Bruce

Stephen Paul Collingwood

Nichola Smith

Peter Hunt

Gurdip Bhalay

Paul Joseph Oakley

Graham Charles Bloomfield

Darren Mark Legrand

Thomas Anthony Hunt

Andrew Dunstan

Darren Mark LeGrand

Peter Gedeck

Judy Fox Hayler

Darren Mark Le Grand

Barbara Valade

Roger John Taylor

Bernard Cuenoud

Brian Cox

Thomas Hugo Keller

Cathy Ritchie

Nicola Press

Gaynor Elizabeth Pilgrim

Glyn Hughes

Julia Doris Ida Hatto

Paul Oakley

Lee Edward

The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

Pyridine and pyrazine derivative for the treatment of chronic bronchitis

Pyridine and pyrazine derivative for the treatment of CF

A compound of Formula I in free or salt or solvate form, where R, R, R, R, R, R, R, R, R, Rand Rhave the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives

A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

N-substituted heterocyclyl carboxamides

The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R, R, Ar', A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.

Pyrazine compounds as PI3 kinase inhibitors

Compounds of formula I in free or salt form, wherein R, R, Rand Rhave the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Inhibitors of phosphatidylinositol 3-kinase

Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme

Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel

The present invention concerns a compound of formula Ia wherein: Ris hydrogen or C-C-alkyl; Ris &#x2014;(C-C-alkylene)-Y&#x2014;C-C-haloalkyl or &#x2014;(C-C-alkylene)-Y&#x2014;C-C-hydroxyalkyl; Y represents &#x2014;CONH&#x2014; or a five membered heteroaryl group. Ris C-C-alkyl or halogen; Ris halo, &#x2014;SO&#x2014;CH, &#x2014;SO&#x2014;CF, carboxy, &#x2014;CO&#x2014;NH, &#x2014;CO-di(C-C-alkyl)amino, or a 5- or 6-membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C-C-cycloalkyl, C-C-alkylcarbonyl, C-C-alkoxy optionally substituted by aminocarbonyl, or C-C-alkyl optionally substituted by hydroxy, C-C-alkoxy, C-C-alkylamino or di(C-C-alkyl)amino; Ris hydrogen, halo, &#x2014;SO&#x2014;CH, nitrile, C-C-haloalkyl, imidazolyl, C-C-alkyl, &#x2014;NRR, or &#x2014;SO&#x2014;NRR; and Ris hydrogen, halogen or C-C-alkyl; Rand Rare independently hydrogen, amino, C-C-alkylamino, di(C-C-alkyl)amino, or CC-C-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase. 

5-phenyl-thiazol-2-yl-urea derivatives and use as PI3 kinase inhibitors

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Horsham, United Kingdom

Emma Budd