Actelion Pharmaceuticals Ltd

Other

Ralf Koberstein

Hamed Aissaoui

Thierry Sifferlen

Christoph Boss

Markus Gude

Martine Clozel

Thomas Weller

Walter Fischli

Wolfgang Skranc

Romain Siegrist

David Lehmann

Daniel Trachsel

Zarghun Nazir

Michael Stanek

Cornelia Zumbrunn Acklin

Christoph Imboden

Wilhelm Tschebull

Michael W Cappi

Doris Domin

Matthias Helms

David Lehman

Andreas Hendrikus De Vries

Gerardus Karel Verzijl

Andreas Hendrikus Maria De Vries

Gerardus Karel Maria Verzijl

Walter Actelion Pharmaceuticals Ltd Fischli

The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and Rare as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists. 

2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists

The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and Rare as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists. 

2-aza-bicyclo[3.3.0]octane derivatives

The invention relates to compounds of formula (I) wherein Y, A, N and Rare as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to the use of such compounds as medicaments, especially as orexin receptor antagonists. 

Pyrrolidines and piperidines as orexin receptor antagonists

The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and Rare as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.

2-aza-bicyclo[2.2.1]heptane derivatives

The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and Rare as described in the description and their use as medicaments, especially as orexin receptor antagonists. 

Thiazolidine derivatives as orexin receptor antagonists

The invention relates to piperidine compounds of formula (I): wherein X&#x2014;Rrepresents &#x2014;N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C)alkyl or halogen, or X&#x2014;Rrepresents &#x2014;NH&#x2014;C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di- or tri-substituted wherein the substituents are independently selected from (C)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C)alkyl, (C)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.

3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors

The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R, R, R, and A are as described in the description and their use as orexin receptor antagonists. 

3-aza-bicyclo[3.3.0]octane compounds

The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and Rare as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists. 

Trans-3-aza-bicyclo[3.1.0]hexane derivatives

The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.

N-glycinsulfonamide derivatives and uses as orexin receptor antagonists

The invention relates to novel azetidine compounds of formula (I), wherein R, R, and X are as described in the description and their use as orexin receptor antagonists. 

Azetidine compounds as orexin receptor antagonists

The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.

Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists

The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to a mammal.

Substituted 1,2,3,4-tetrahydroisoquinoline derivatives

The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists. General Formula (I) wherein X and R-Rare as defined in the description 

Quinoxalin-3-one derivatives as orexin receptor antagonists

The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.

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Lorrach, Germany

Ralf Koberstein