Smithkline Beecham Corporation

David John Nash

Geoffrey Stemp

Christopher Norbert Johnson

Clive Leslie Branch

Amanda Johns

Roderick Alan Porter

Wai Ngor Chan

Riccardo Novelli

Rachel Elizabeth Anne Stead

Jean-Pierre Pilleux

Michael S Hadley

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

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 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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Harlow, United Kingdom

David John Nash