Merck Sharp + Dohme Corp.

Robert James Maxey

Mark Stewart Chambers

Philip Jones

Angus Murray MacLeod

Leslie Joseph Street

David James Hallett

Simon Charles Goodacre

Neil Roy Curtis

Helen Jane Szekeres

Jose Luis Castro Pineiro

Ian James Collins

Richard Thomas Lewis

Michael Rowley

Wesley Peter Blackaby

Tamara Ladduwahetty

Kevin John Merchant

Kevin William Moore

Mark Stuart Chambers

Michael Geoffrey Neil Russell

Linda Elizabeth Keown

Alexander Charles Humphries

Helen Jane Bryant

Myra Gilligan

Emanuela Gancia

Angus Murray Macleod

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

[object Object]

A class of imidazo[1,2][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAreceptors, in particular having good 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.

Imidazo-triazine derivatives as ligands for gaba receptors

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.

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 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 substituted or 6,7-ring fused &lsqb;1, 2, 3&rsqb;triazolo&lsqb;1,5-&agr;&rsqb;-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Triazolo-pyrimidine derivatives as ligands for gaba receptors

3-(Piperidin-4-yl)-1H-indole derivatives bearing an optionally substituted phenyl moiety at the 2-position of the indole ring system and an alkyl or aryl-alkyl substituent on the nitrogen atom of the piperndine ring are selective antagonists of the human 5-HT,receptor.

Phenylindole derivatives as 5-HT2A receptor antagonists

Growing community of inventors

Amersham, United Kingdom

Robert James Maxey