Novartis Ag

Gurdip Bhalay

Stephen Paul Collingwood

Catherine Howsham

Lee Edwards

Nichola Smith

Peter Hunt

Andrew Dunstan

Emma Budd

Paul Joseph Oakley

Graham Charles Bloomfield

Thomas Anthony Hunt

Peter Gedeck

Trevor John Howe

Robin Alec Fairhurst

David Andrew Sandham

Darren Mark Le Grand

Sylvie Felicite Gomez

Clive McCarthy

Urs Baettig

Brian Cox

Reto Naef

Jeffrey McKenna

Christopher Thomson

Thomas Storz

James Dale

Nicholas James Devereux

Clive Victor Walker

Alessandro Mazzacani

Ameet Vijay Ambarkhane

Ahmed Hamadi

Martin Beckett

Angela Glen

Ret Naef

Paul Oakley

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

Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, R, R, R, and Rhave the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Pyrazine derivatives as ENaC blockers

The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.

3-spirocyclic piperidine derivatives as ghrelin receptor agonists

Pyrazine derivatives as enac blockers

Compounds of formula I in salt or zwitterionic form wherein, wherein R, R, R, and Rhave the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Quinuclidine derivatives binding to mucarinic M3 receptors

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

Compounds of formula I in free or salt form, wherein T, X, Y, U, R, R, m, n and p have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Pyrrolidine derivatives acting as CCR3-receptor antagonists

This invention relates to organic compounds of formula I, in which Aris unsubstituted phenyl substituted by one or more halogen atoms; Aris unsubstituted phenyl or phenyl substituted by one or more substituents selected from the group consisting of halogen, cyano and C-C-alkoxy; Ris hydrogen or methyl optionally substituted by hydroxy; Ris hydrogen or hydroxy; and pharmaceutically acceptable salts thereof. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.

Derivatives of 3-phenyl-n-(2-(4-benzyl)-piperidin-1-yl)-ethyl)-acrylamid with ccr-3-receptor antagonistic activity for use in the treatment of inflammations and allergic conditions

Compounds of formula (I) in free or salt form, where Aris phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C&#x2013;C-alkyl optionally substituted by cyano or halogen, Aris phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C&#x2013;C-alkyl, C&#x2013;C-haloalkyl, C&#x2013;C-alkoxy or C&#x2013;C-alkoxycarbonyl, Ris C&#x2013;C-alkyl substituted by hydroxy, C&#x2013;C-alkoxy, acyloxy, &#x2014;N(R)R, halogen, carboxy, C&#x2013;C-alkoxycarbonyl, phenyl-C&#x2013;C-alkoxycarbonyl, &#x2014;CON(R)Ror by a monovalent cyclic organic group, Rand R?3are each independently hydrogen or C&#x2013;C-alkyl, or Ris hydrogen and Ris acyl or SOR, or Rand Rtogether with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, Rand Rare each independently hydrogen, C&#x2013;C-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C&#x2013;C-alkyl, halogen, cyano or C&#x2013;C-alkoxy, or Rand Rtogether with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R?6is C&#x2013;C-alkyl, C&#x2013;C-haloalkyl, or phenyl optionally substituted by C&#x2013;C-alkyl, and n is 1, 2, 3 or 4. The compounds are useful as pharmaceuticals.

N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists

A compound of formula (I):Ris hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, Ris hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, Ris hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, Ris hydrogen or alkyl, Ris a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula &#x2014;N(R)R, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and Rand Rare each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of Rand Ris hydrogen and the other is acyl, or Rand Rtogether with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors

A compound of formula (I)Ris hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, Ris hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, Ris hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, Ris hydrogen or alkyl, Ris a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula &#x2014;N(R)R, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and Rand Rare each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of Rand Ris hydrogen and the other is acyl, or Rand Rtogether with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors

Piperidine compounds for use as ccr-3 inhibitors

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Horsham, United Kingdom

Gurdip Bhalay