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

US8133901B2 · kind B2 · utility

Assignee

• Actelion Pharmaceuticals Ltd. · CH

Inventors

• Hamed Aissaoui · Allschwil, CH
• Christoph Boss · Allschwil, CH
• Markus Gude · Allschwil, CH
• Ralf Koberstein · Bad Kötzting, DE
• Thierry Sifferlen · Allschwil, CH

Key dates

• Filing date: Nov 29, 2007
• Grant date: Mar 13, 2012
• Expiry date: Oct 18, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to piperidine compounds of formula (I):wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X—R1 represents —NH—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 (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)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 (C1-4)alkyl, (C1-4)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.