Actelion Pharmaceuticals Ltd

Idorsia Pharmaceuticals Ltd

Eva Caroff

Kurt Hilpert

Sylvia Richard-Bildstein

Emmanuel Meyer

Francis Hubler

Dorte Renneberg

Heinz Fretz

Thierry Kimmerlin

Volker Breu

David Lehmann

Anja Fecher

Matthias Steger

Thomas Giller

Oliver Valdenaire

Emmanuel Meyers

Olivier Houille

Marcel Keller

Rémy Castro

Loïc Jacob

Alexia Chavanton-arpel

Oliver Allemann

Andrew Croxford

Remy Castro

The invention relates to compounds of Formula (I) wherein X, Y, R, R, R, Rand Rare as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

1-(piperazin-1-yl)-2-([1,2,4]triazol-1-yl)-ethanone derivatives

The invention relates to compounds of Formula (I) wherein n, X, Rand Rare as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

Hydroxyalkyl-piperazine derivatives as CXCR3 receptor modulators

The invention relates to compounds of Formula (I) wherein Rand Rare as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

(R)-2-methyl-piperazine derivatives as CXCR3 receptor modulators

The invention relates to compounds of Formula (I) wherein R, R, R, Rand Rare as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor. 

8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives

The invention relates to compounds of Formula (I), wherein ring A, X, (R), R, R, R, R, R, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives

The present invention relates to thiazole derivatives of formula I and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. 

Thiazole derivatives and their use as P2Y12 receptor antagonists

The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I). 

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The present invention relates to 2-phenyl-4-cyclopropyl-pyrimidine derivatives and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

2-phenyl-4-cyclopropyl-pyrimidine derivatives

The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidines

The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis. 

2-aminocarbonyl-pyridine derivatives

The present invention relates to compounds of formula I wherein R, R, R, R, R, R, n, W and Z are as defined in the application, their preparation and their use as P2Yreceptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

Substituted 2-phenyl-pyridine derivatives

The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Yreceptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

Pyrimidine derivatives and their use as P2Y12 receptor antagonists

The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Yreceptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (I). 

2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor

The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by &#x2014;N(R')&#x2014; or &#x2014;O&#x2014; and R&#x2032; is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments. 

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Allschwil, Switzerland

Eva Caroff