Smithkline Beecham Corporation

Clive Leslie Branch

Christopher Norbert Johnson

Geoffrey Stemp

Roderick Alan Porter

Amanda Johns

David John Nash

Wai Ngor Chan

Kevin Thewlis

Riccardo Novelli

Rachel Elizabeth Anne Stead

Jean-Pierre Pilleux

Steven Coulton

Alexander B Smith

Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.

N-aroyl cyclic amine derivatives as orexin receptor antagonists

Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.

N-aroyl cyclic amines

This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NRor a group (CH), wherein n represents 1, 2 or 3; Y represents CH, CO, CH(OH), or CHCH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Arrepresents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists. 

This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein:

This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.

N-aroyl piperazine derivatives as orexin receptor antagonists

Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same.

Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor

This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C&#x2550;O, SO, or CH&#x2550;CH&#x2014;; Aris aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Arrepresents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by Rand further optional substituents; or Arrepresents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; Rrepresents optionally substituted (C)alkoxy, halo, optionally substituted (C)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; Rrepresents hydrogen, optionally substituted (C)alkyl, optionally substituted (C)alkanoyl, optionally subtituted (C)alkanoxycarbonyl or optionally substituted aryl(C)alkyloxycarbonyl; and their use as orexin receptor-antagonists.

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This invention relates to morpholine derivatives of formula (I) and their use as antagonists of orexin receptors.

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Harlow, United Kingdom

Clive Leslie Branch