Smithkline Beecham Corporation

Beecham Group Plc

Glaxo Group Limited

Smithkline Beegham P.l.c.

Geoffrey Stemp

Christopher Norbert Johnson

Clive Leslie Branch

David John Nash

John M Evans

Amanda Johns

Roderick Alan Porter

Frederick Cassidy

Wai Ngor Chan

Kevin Thewlis

Mervyn Thompson

Riccardo Novelli

Rachel Elizabeth Anne Stead

Jean-Pierre Pilleux

Michael S Hadley

Susan Marie Westaway

Gordon Burrell

Jonathan Thomas Seal

Steven Coulton

Gregor James MacDonald

Stephen Allan Smith

Steven James Stanway

David G Smith

Andrew Lightfoot

Harshad Kantilal Rami

Darren Jason Mitchell

Gordon Bruton

Neil Upton

Robert N Willette

David Timothy Macpherson

Antonio Kuok Keong Vong

Charles D Nicholson

Dieter Angersbach

Alexander B Smith

Antonio Keuok Keong Vong

Phillip Jeffrey

Barry Sidney Orlek

The present invention relates to novel benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders. 

Benzylpiperazine derivatives and their medical use

The invention relates to compounds of formula (I): processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.

Process for preparing piper azine derivatives

Benzylpiperazine derivatives as motilin receptor agonists

Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. 

Piperazinyl-sulfonamide derivatives useful in the treatment of GPR38 receptor mediated diseases

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:

The invention provides compounds of formula (I): wherein: Rand Rindependently represent various substituents; Rand Rindependently represent H, F, Cl, Br, Calkyl, Calkoxy, OH, CN, or NO; B represents a sulfur atom or a &#x2014;CH-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof. Preferably, A is selected from one of the groups (i), (ii) or (iii): wherein Xand Xare independently N or CR, and Xis NR, O or S; Yand Yare independently N or CR, and Yis NR, O or S; Zis NR, O or S, and Zand Zare independently N or CR; R, R, and Rare as herein defined, and Ris H, a halogen atom, OH, cyano, nitro, Calkyl, Calkoxy, Calkylenedioxy, Calkanoyl, or Calkylsulfonyl, an optionally substituted 3-, 4-, 5- or 6-membered cycloalkyl ring, or a group of the formula (a), (b), (c) or (d) as defined by the formulas (a), (b), (c) or (d). The compounds are modulators of dopamine Dreceptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.

Tetrahydrobenzazepine derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents)

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

Growing community of inventors

Harlow, United Kingdom

Geoffrey Stemp