Beecham Group Plc

Smithkline Beecham Corporation

Glaxo Group Limited

Barry S Orlek

Michael S Hadley

Steven Mark Bromidge

Gordon Bruton

Paul Adrian Wyman

John David Harling

Harry J Wadsworth

Desmond John Best

Laramie Mary Gaster

Steven Dabbs

Kishore Kalidas Rana

Mervyn Thompson

Richard E Faulkner

Howard E Rosenberg

Anthony Huxley

Thomas H Brown

Sarah Margaret Jenkins

Sing Yeung Mak

Geracimos Rassias

Pamela Joan Theobald

Richard E Faulkner, Deceased

Vicky Johnstone

The present invention relates to novel diazepanyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

1-benzoyl substituted diazepine derivatives as selective histamine H3 receptor agonists

The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.

Piperazine derivative having affinity for the histamine H3 receptor

The present invention relates to novel diazepanyl derivatives of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

The present invention relates to novel methylene dipiperidine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Methylene dipiperidine derivatives

The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Piperazine derivates and their use for the treatment of neurological and psychiatric diseases

The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Bicyclic benzamide compound as histamine H3 receptor ligand useful in the treatment of neurological diseases

A compound of formula (I): useful in the treatment and prophylaxis of conditions mediated by s-CD23 

Quinoline derivatives, process for preparing them and use for the treatment of diseases mediated by s-CD23

A compound of formula (I) useful in the treatment and prophylaxis of conditions mediated by s-CD23

Sulfone derivatives and their use in the treatment of autoimmune diseases and allergies

Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R,is hydrogen, C,alkyl (optionally substituted by hydroxy or C,alkoxy), C,alkenyl, C,alkynyl, C,alkylCO&mdash;, formyl, CF,CO&mdash; or C,alkylSO,&mdash;; R,is hydrogen or up to three substituents selected from halogen, NO,, CN, N,, CF,O&mdash;, CF,S&mdash;, CF,CO&mdash;, trifluoromethyldiazirinyl, C 1-6&quest;alkyl, C,alkenyl, C,alkynyl, C,perfluoroalkyl, C,cycloalkyl, C,cycloalkyl-C,alkyl-, C,alkylO&mdash;, C,alkylCO&mdash;, C,cycloalkylO&mdash;, C,cycloalkylCO&mdash;, C,cycloalkyl-C,alkylO&mdash;, C,cycloalkyl-C,alkylCO&mdash;, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C,alkyl-, C,alkylS&mdash;, C,alkylSO,&mdash;, (C,alkyl),NSO,&mdash;, (C,alkyl)NHSO,&mdash;, (C,alkyl),NCO&mdash;, (C,alkyl)NHCO&mdash; or CONH,; or &mdash;NR,R,where R,is hydrogen or C,alkyl, and R,is hydrogen, C,alkyl, formyl, &mdash;CO,C,alkyl or &mdash;COC,alkyl; or two R,groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by &mdash;OH or &boxH;O; and the two R,groups and the two R,groups are each independently hydrogen or C,alkyl or the two R,groups and/or the two R,groups together form a C,spiroalkyl group provided that at least one R,and R,group is not hydrogen, are useful in the treatment and prophylaxis of epilepsy and other disorders.

Anti-convulsant isoquinolyl-benzamide derivatives

Substituted benzamide derivatives and their use as anticonvulsants

A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises zero, one or two nitrogen atoms, Q being optionally C-substituted by a group R.sub.1 selected from halogen, CN, OR.sub.2, SR.sub.2, N(R.sub.2).sub.2, NHCOR.sub.2, NHCOOCH.sub.3, NHCOOC.sub.2 H.sub.5, NHOR.sub.2, N.sub.3, NHNH.sub.2, NO.sub.2, COR.sub.2, COR.sub.3, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, cyclopropyl or C.sub.1-2 alkyl optionally substituted with OR.sub.2, N(R.sub.2).sub.2, SR.sub.2, CO.sub.2 R.sub.2, CON(R.sub.2).sub.2 or one, two or three halogen atoms, in which each R.sub.2 is independently hydrogen or C.sub.1-2 alkyl and R.sub.3 is OR.sub.2, NH.sub.2 or NHR.sub.2 ; r represents an integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0 or 1; R.sub.a and R.sub.b each represent hydrogen or, when X is hydrogen, optionally together represent a bond; with the proviso that when Y is hydrogen s is 1.

N-linked azabicyclic heterocycles useful for treating dementia

Enantiomers of 1-(3,4-dichlorobenzyl)-2-methylaminoindane

Substituted cycloalkylamine derivatives and their use as calcium channel

Indane and tetrahydronaphthalene derivatives as calcium channel

Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a group ##STR2## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.1 and the other is nitrogen or CR.sub.2, or A.sub.2 is oxygen or sulphur, A.sub.1 is CH and A.sub.3 is CR.sub.1, where R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1-2 alkyl, with the proviso that when r is 2, R.sub.1 and R.sub.2 are hydrogen or methyl. The novel compounds of this invention may be used to treat or to prevent dementia in mammals.

Growing community of inventors

Harlow, United Kingdom

Barry S Orlek