Merck Sharp + Dohme Corp.

Merck Sharpe & Dohme Corp.

Francine Sternfeld

Leslie Joseph Street

Angus Murray MacLeod

Austin John Reeve

Tamara Ladduwahetty

Kevin John Merchant

William Robert Carling

Raymond Baker

Richard Alexander Jelley

Jose Luis Castro Pineiro

Kevin William Moore

Victor G Matassa

Victor Giulio Matassa

Janusz Jozef Kulagowski

Andrew Madin

Jason Matthew Elliott

Mark Stuart Chambers

Sarah Christine Hobbs

Alexander Richard Guiblin

Christopher John Swain

Andrew Pate Owens

Neil Roy Curtis

Graham A Showell

Duncan Edward Shaw

Michael Geoffrey Russell

Piotr Antoni Raubo

Sylvie Bourrain

Ian Thomas Huscroft

James Michael Crawforth

Ruth McKernan

Helen Routledge

Caroline Henry

Olivier Dirat

The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R, R, R, R, R, R, R, R, R, Rand Rare defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Tetrahydropyran compounds as tachykinin antagonists

The invention provides compounds of formula I: which are inhibitors of &#x3b3;-secretase and hence useful in the treatment or prevention of Alzheimer's disease.

Sulphones for inhibition of gamma secretase

The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group Rand the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups Rand R; one of Rand Ris hydrogen; either all of W, W, Wand Ware carbon or one of W, W, Wand Wis nitrogen and the rest are carbon; and Rand Rare, independently, a small group, heteroaromatic ring or a 4&#x2013;7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.

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A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAreceptors of formula Iwhich are partial or full inverse agonists of an &#x3b1;5 receptor subunit while being relatively free of activity at &#x3b1;1 and/or &#x3b1;2 and/or &#x3b1;3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.

Imidazolophthalazine derivatives as ligands for GABAA receptors

A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAreceptors of formula I:which are partial or full inverse agonists of an &#x3b1;5 receptor subunit while being relatively free of activity at &#x3b1;1 and/or &#x3b1;2 and/or &#x3b1;3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.

A class of 1,2,3a,4,x-pentaaza-cyclopenta&lsqb;a&rsqb;naphthalene compounds (x&equals;6, 7, 8 or 9) is described. The compounds have a high affinity for the GABA &agr;5 receptors and show inverse agonist activity thereat. The compounds are useful in therapy where cognition enhancement is required.

Pentaaza-cyclopental&lsqb;a&rsqb;naphthalene derivatives as ligands for GABAa &agr;5 receptors

Substituted triazolo pyridazine derivatives as inverse agonists of the GABAA&agr;5 receptor subtype

A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.

Substituted 1,2,4-triazolo&lsqb;3,4-A&rsqb;phthalazine derivatives as GABA&agr;5 ligands

Triazolopyridazine Derivatives for treating anxiety and enhancing cognition

Substituted 1,2,4-Triazolo&lsqb;3,4-A&rsqb;phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula:

Precursor compounds to substituted 1,2,4-triazolo&lsqb;3,4,-a&rsqb;phathalazine GABA alpha 5 ligands

A compound of formula I, or a salt or prodrug thereof:

Triazolopyridazine derivatives for treating anxiety and enhancing cognition

Substituted 1,2,4-Triazolo&lsqb;3,4-A&rsqb;phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula

Substituted 1,2,4-triazolo&lsqb;3,4-a&rsqb;phthalazine derivatives as GABA alpha 5 ligands

Azetidine, pyrrolidine and piperidine derivatives as 5HT1 receptor

Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha.

Triazole derivatives

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London, United Kingdom

Francine Sternfeld