Smithkline Beecham Corporation

Glaxo Group Limited

Smithkline Beegham P.l.c.

Wai Ngor Chan

Roderick Alan Porter

Amanda Johns

Christopher Norbert Johnson

Riccardo Novelli

Geoffrey Stemp

Rachel Elizabeth Anne Stead

Clive Leslie Branch

David John Nash

Jean-Pierre Pilleux

John M Evans

Mervyn Thompson

Robert N Willette

Neil Upton

Hugh Jonathan Herdon

Jeffrey Clifford Jerman

Simon Edward Ward

Mythily Vimal

Daniel Marcus Bradley

Helen Kate Morgan

Nicolas Bertheleme

Kuok Keong Vong

Jaqueline Sandra Scott

Kevin Michael Thewlis

Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; Ris selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from Calkyl and halogen; and Ris selected from H and CHwhen n is 1 and Ris H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed. 

Compounds which potentiate the AMPA receptor and uses thereof in medicine

This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Piperidine compounds for use as orexin receptor antagonist

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. 

A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Piperidine compounds for use as orexin receptor antagoinst

Disclosed are phenyl-alkylene benzamides useful as orexin antagonists 

Benzamide derivatives as antagonists of orexin receptors

Receptor that binds anti-convulsant compounds

This invention relates to substituted benzopyran amides useful in treating certain medical conditions and to processes for preparing these compounds.

Benzopyrans and their use as therapeutic agents

Screening methods to identify anti-convulsant compounds

A compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR1## wherein either Y is N and R.sub.2 is hydrogen, or Y is C--R.sub.1 ; where either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of hydrogen, C.sub.3-8 cycloalkyl, C.sub.1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C.sub.1-6 alkoxy or substituted arminocarbonyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF.sub.3 S, or a group CF.sub.3 --A--, or a group CF.sub.2 H--A'--, trifluoromethoxy, C.sub.1-6 alkylsulphinyl, perfluoro C.sub.2-6 alkylsulphonyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino, C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl; or R.sub.1 and R.sub.2 together are --(CH.sub.2).sub.4 -- or --CH.dbd.CH--CH.dbd.CH--, or form an optionally substituted triazole or oxadiazole ring; R.sub.3 to R.sub.9 represent various substituent groups; and X is oxygen or NR.sub.10 where R.sub.10 is hydrogen or C.sub.1-6 alkyl.

Pharmaceutical composition containing bicyclic type compounds

Bicyclic compounds with pharmaceutical activity

The invention relates to certain cis and trans benzopyrans having substituted benzamides at position C-4 and to their use in treating and/or preventing certain CNS disorders.

Treatment

Growing community of inventors

Harlow, United Kingdom

Wai Ngor Chan