Merck Sharp + Dohme Corp.

Merck Sharpe & Dohme Corp.

Merck + Co., Inc.

Angus Murray MacLeod

Kevin John Merchant

Tamara Ladduwahetty

Leslie Joseph Street

Francine Sternfeld

Mark Stewart Chambers

Monique Bodil Van Niel

Richard Thomas Lewis

Philip Jones

Raymond Baker

Jose Luis Castro Pineiro

William Robert Carling

Graham A Showell

Austin John Reeve

Graeme Irvine Stevenson

Christopher John Swain

Kevin William Moore

Sarah Christine Hobbs

Robert James Maxey

Sylvie Bourrain

Timothy Harrison

Kevin J Wilson

Michael Rowley

Stephen Robert Fletcher

Mark Stuart Chambers

Helen Jane Szekeres

Peter Alan Hunt

Eileen Mary Seward

Andrew Pate Owens

Martin Richard Teall

Frank Burkamp

Peter Blurton

Laura Catherine Cooper

Alexander Charles Humphries

Helen Jane Bryant

Richard Alexander Jelley

Susan Koon-Fung Cheng

Myra Gilligan

Daniel Spinks

Andrew Madin

Brian John Williams

Paul E Finke

Ian James Collins

Neil Roy Curtis

Wesley Peter Blackaby

David James Hallett

Jason Matthew Elliott

Simon Charles Goodacre

John Saunders

Christopher Richard Moyes

Howard Barff Broughton

Victor Giulio Matassa

Michela Bettati

Jackson B Gibbs

Gerard Raphael Dawson

Joseph George Neduvelil

Kenneth S Koblan

Ruth McKernan

Amanda Louise Boase

Guy Ralph Seabrook

Richard J Lewis

The present invention discloses a compound of formula (I): wherein: Ris an aryl or heteroaryl ring; Ris hydroxy, Calkoxy, Calkyl, amino, NR'R&#x2033; or Calkyl-NR&#x2032;R&#x2033; where R&#x2032; and R&#x2033; are independently chosen from hydrogen and Calkyl and where R&#x2032; and R&#x2033;, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR&#x2032;R&#x2033; as defined above or Ris Calkoxy substituted by NR&#x2032;R&#x2033; as defined above; Ris hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, aryl or aryl Calkyl; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, aryl, aryl Calkyl or Calkoxycarbonyl; or Rand R, together with the nitrogen atom to which they are attached, form a C-Cmono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF, halogen and Calkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome. 

Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands

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

A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Pyridazine derivatives as ligands for GABA receptors

The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.

Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of Alzheimer's disease

The present invention provides a compound of formula (I) in which Ris generally hydrogen or CF, Ris generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y&#x2014;X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them 

Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition

Compounds of formula I: are antagonists of the human 5-HTreceptor, and hence useful in treatment or prevention of a variety of neurological conditions.

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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.

A class of imidazo[1,2-&#x3b1;]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAreceptors, in particular having good affinity for the &#x3b1;2 and/or &#x3b1;3 and/or &#x3b1;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Imidazo-pyrimidine derivatives as ligands for GABA receptors

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.

The present invention provides a compound of formula (I) wherein A is an optionally substituted Calkylidene group or a bond, Rand Rare hydrogen, alkyl groups or heterocyclic groups, Rand Rare small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is Calkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition

A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

Phenylsulphonyl derivatives as 5-HT receptor ligands

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Bishops Stortford, United Kingdom

Angus Murray MacLeod