Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Merck Sharpe & Dohme Corp.

Tamara Ladduwahetty

Angus Murray MacLeod

Kevin John Merchant

Francine Sternfeld

Sander G Mills

Shrenik K Shah

Conrad P Dorn

Jeffrey John Hale

Malcolm MacCoss

Timothy Harrison

Paul E Finke

Brian John Williams

Leslie Joseph Street

Mark Stewart Chambers

William Robert Carling

Kevin William Moore

Mark Stuart Chambers

Alexander Charles Humphries

Myra Gilligan

Jose Luis Castro Pineiro

Christopher John Swain

Kevin J Wilson

Monique Bodil Van Niel

Peter Alan Hunt

Laura Catherine Cooper

Amanda Louise Boase

Andrew Madin

Eileen Mary Seward

Richard Thomas Lewis

Neil Roy Curtis

Michael Rowley

Malcolm Maccoss

Austin John Reeve

Sarah Christine Hobbs

Ian Churcher

Robert James Maxey

Linda Elizabeth Keown

Richard Alexander Jelley

Michela Bettati

Emanuela Gancia

Reymond Baker

Angus Murray Macleod

Monique B Van Niel

Abdul Quddus

Kevin Wilson

Compounds of formula (I) are potent and selective 5-HTantagonists, useful in treatment of a variety of adverse conditions of the CNS. 

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Compounds of formula I: are potent and selective antagonists of the human 5-HTreceptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Diarylsulfones as 5-HT2A antagonists

Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease. 

Gamma-secretase inhibitors

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.

The present invention relates to compounds of formula I:

Cognition enhancing derivatives of isoxazole triazoloindane GABA-A &#x3b1;5 receptor subunit ligands

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.

Morpholine and thiomorpholine tachykinin receptor antagonists

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 heterocycles of the general structural formula:

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

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London, United Kingdom

Tamara Ladduwahetty