Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Merck Sharpe & Dohme Corp.

Kevin William Moore

William Robert Carling

Leslie Joseph Street

Jose Luis Castro Pineiro

Michael Geoffrey Russell

Angus Murray MacLeod

Richard Thomas Lewis

David James Hallett

Kevin John Merchant

Simon Charles Goodacre

Alexander Richard Guiblin

Philip Jones

Andrew Madin

Mark Stewart Chambers

Tamara Ladduwahetty

Francine Sternfeld

Gayle Scott

Timothy Harrison

Ian James Collins

Paul D Leeson

Michael Rowley

Wesley Peter Blackaby

Paul David Leeson

Andrew S Jennings

Janusz Jozef Kulagowski

Andrew Pate Owens

Neil Roy Curtis

Martin Richard Teall

Stephen Robert Fletcher

Graham A Showell

Victor G Matassa

Austin John Reeve

Christopher Richard Moyes

Sarah Christine Hobbs

Howard Barff Broughton

Helen Jane Szekeres

Robert James Maxey

Michael Geoffrey Neil Russell

Alexander Charles Humphries

Andrew Mitchinson

Michael Reader

Sarah Margaret Kelly

Robert William Carling

A class of 8-fluoro-3-phenylimidazo[1,2-&#x3b1;]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a &#x2014;NH&#x2014; or &#x2014;OCH&#x2014; linkage, being selective ligands for GABAreceptors, 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.

Imidazo-pyridine derivatives as ligands for GABA receptors

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 compound (I) is a GABAreceptor ligand, functionally selective for the &#x3b1;2 and/or &#x3b1;3 subunit, and is useful in the treatment of deleterious mental states, in particular anxiety.

7-Tert-butyl-3-(2-fluorophenyl)-6-(2H-(1,2,4)triazol-3-ylmethoxy)-(1,2,4)triazolo (4,3b) pyridazine for the treatment of anxiety and convulsions

The present invention is directed to compounds comprising a triazolo[4,3-b]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Inhibitors of Akt activity

A class of 3-phenylimidazo[1,2-&#x3b1;]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a &#x2014;NH&#x2014; linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, 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

A class of substituted 1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-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-pyridazine derivatives as ligands for GABA receptors

A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a &mdash;NH&mdash; linkage; Z represents an optionally substituted aryl or heteroaryl group; R represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, &mdash;OR , &mdash;SR , &mdash;SOR , &mdash;SO R , &mdash;SO NR R , &mdash;NR R , &mdash;NR COR , &mdash;NR CO R , &mdash;COR , CO R , &mdash;CONR R or &mdash;CR &boxH;NOR ; and R and R independently represent hydrogen, hydrocarbon or a heterocyclic group.), substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a &mdash;NH&mdash; linkage, are selective ligands for GABA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 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.

3-Phenyl-imidazo-pyrimidine derivatives as ligands for GABA receptors

A class of substituted 1,2,4-triazolo&lsqb;4,3-&rsqb;pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-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.

Imidazo-triazine derivatives as ligands for GABA receptors

1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-alkoxy moiety at the 6-position, are selective ligands for GABA 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.

1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.

Triazolo-pyridazine derivatives as ligands for gaba receptors

Pyrazolo-triazine derivatives as ligands for GABA receptors

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

1,2,4-triazolo&lsqb;4,3-b&rsqb;pyridazine derivatives are ligands for GABA,receptors useful in the treatment of disorders of dementing illnesses.

Therapeutically active 1,2,4-triazolo&lsqb;4.,3-B&rsqb; pyridazine derivatives as ligands for GABA receptors

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

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, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABA,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.

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Buntingford, United Kingdom

Kevin William Moore