Merck Sharp + Dohme Corp.

Merck & Dohme Limited

Paul David Leeson

Janusz Jozef Kulagowski

Neil Roy Curtis

Ian James Collins

Michael Rowley

Martin Richard Teall

Mark Peter Ridgill

Timothy Harrison

William Robert Carling

Stephen Robert Fletcher

Kevin William Moore

Graham A Showell

Alan John Nadin

Christopher Richard Moyes

Timothy Jason Sparey

Ian M Mawer

Andrew Pate Owens

Sylvie Bourrain

Joseph George Neduvelil

Compounds according to Formula (I) or a salt thereof are selective ligands for GABA receptors useful for treatment of disorders of the central nervous system:

Substituted 1H-pyridinyl-2-ones as GABAA alpha 2/3 ligands

Substituted 1H-Pyridinyl-2-ones are useful as GABA,-Alpha 2/3 ligands.

Substituted 1H-pyridinyl-2-ones as GABAA-&agr; 2/3 ligands

Five-membered heteroaromatic compounds as dopamine receptor subtype

A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Tetrahydropyridine derivatives as dopamine receptor subtype ligands

A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Indole derivatives as dopamine D4 antagonists

Pyrmidine derivatives

A class of pyrrolo�2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.

Pyrrolo-pyridine derivatives

A class of substituted furo�2,3-b!pyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Furopyridine derivatives

Isoxazole and pyrazole derivatives as dopamine receptor subtype ligands

The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo�b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo�b!furan moiety by a methylene group, which are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 receptor subtype and having a selective affinity for the D.sub.4 subtype over other dopamine receptor subtypes, possess advantageous qualities in terms of their improved aqueous solubility relative to the corresponding free base and, as such, provide for greater ease of formulation and display enhanced pharmacokinetic properties, including oral absorption.

Methanesulfonate salts of antipsychotic benzofuran derivatives

Benzofuran derivatives as D.sub.4 receptor antagonists

Morpholine derivatives as dopamine receptor subtype ligands

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Monmouth Junction, NJ, United States of America

Paul David Leeson