Merck Sharp + Dohme Corp.

Andrew Mitchinson

Leslie Joseph Street

William Robert Carling

Michael Geoffrey Russell

Jose Luis Castro Pineiro

Kevin William Moore

Gayle Scott

A class of [1,8] naphthyridine analogues which are substituted in the 4-position by a substituted phenyl ring. These compounds are ligands for GABAreceptors and useful in the therapy of deleterious mental states such as anxiety.

(1,8) naphthyridines as gaba ligands, their pharmaceutical compositions and uses

A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAreceptors, in particular having high affinity for the &#x3b1;2 and/or &#x3b1;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.

Pyrazolo-triazine derivatives as ligands for gaba receptors

1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and a chloro at the 8-position are selective ligands for GABAZ receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.

Triazolo-pyridazine derivatives as ligands for GABA receptors

A class of pyrido&lsqb;2,3-d&rsqb;pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position, and a range of substituents at the 3-position, are selective ligands for GABA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;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.

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Sawbridgeworth, United Kingdom

Andrew Mitchinson