Novartis Ag

Other

Irm LLC

Darren Mark Legrand

Ian Bruce

Stephen Paul Collingwood

David C Tully

Catherine Howsham

Yves Auberson

Emma Budd

Lee Edwards

Urs Baettig

Kamlesh Jagdis Bala

Judy Fox Hayler

David Andrew Sandham

Roger John Taylor

David Beattie

Brian Cox

Jeffrey McKenna

Stéphanie Monnier

Thomas Anthony Hunt

Katrin Spiegel

Christopher Thomson

Vikki Furminger

Glyn Alan Hughes

James Dale

Emily Stanley

Berndt Oberhauser

Christopher G Thomson

Rebecca Butler

David William Pearce

Oliver Ross Steward

Andrew Stuart Lister

Barbara Valade

Jean-Louis Reber

Julia Doris Ida Hatto

Silvia Heuerding

Jennifer Leslie Harris

Juergen Roettele

Dilraj Singh

Emmanuelle Briard

Edward Charles Hall

Jeffrey Mckenna

Owen Hughes

Lee Edward

Glyn Hughes

Henry L Danahay

Janet C Maas

The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin. 

Autotaxin inhibitors

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 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 CF

Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.

Organic compounds

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

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

Compounds of formula I in free or salt form, wherein Ar, X, Y and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Azetidine derivatives as CCR-3 receptor antagonist

Compounds of formula I in free or salt form, wherein Ar, R, R, R, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Piperazine derivatives with CCR-3 inhibiting activity

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Horsham, United Kingdom

Darren Mark Legrand