Merck Sharp + Dohme Corp.

Other

Merck + Co., Inc.

Dohme Ltd.

Merck Sharp

Gregory John Hollingworth

Jason Matthew Elliott

Christopher John Swain

Janusz Jozef Kulagowski

Brian John Williams

Neil Roy Curtis

Philip Stephen Jackson

Timothy Harrison

Raymond Baker

Nadia Melanie Rupniak

Eileen Mary Seward

Duncan Edward Shaw

Kevin Dinnell

Jose Luis Castro Pineiro

Eileen May Seward

Lihu Yang

Kevin Tyler Chapman

Stephen Robert Fletcher

Matthew John Lindon

Christopher Richard Moyes

A Brian Jones

Christopher Alan Willoughby

Frank Burkamp

Peter Blurton

Edward Giles McIver

Steven Michael Hutchins

Rebecca Elizabeth Brown

Jason Matthew Elliot

Lauren Rogers

Victoria Alexandra Doughty

Tracy Bayliss

The present invention provides a compound of formula (I): wherein V represents NR, O, S, SO or S(O); W and X each independently represent CH or N; Y represents N, CH or C&#x2014;Ar, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C&#x2014;Ar, with the proviso that when Y is N or CH then Z is C&#x2014;Ar, and with the further proviso that when Y is C&#x2014;Arthen Z is CH; Arrepresents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Arrepresents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; Rrepresents halogen, hydroxy, oxo, Calkyl, Calkenyl, Calkynyl, haloCalkyl, hydroxyCalkyl, Calkoxy, haloCalkoxy, hydroxyCalkoxy, Ccycloalkyl, Ccycloalkoxy, CcycloalkylCalkyl, cyano, nitro, SR, SOR, SOR, COR, NRCOR, CONRR, NRSOR, SONRR, &#x2014;(CH)carboxy, esterified &#x2014;(CH)carboxy or &#x2014;(CH)NRR; Rrepresents hydrogen, halogen, hydroxy, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy, haloCalkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy or haloCalkoxy; Rand Rare each independently hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl or fluoroCalkyl; or Rand Rand the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or Calkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O), or NR; Rrepresents hydrogen, Calkyl, hydroxyCalkyl or CalkoxyCalkyl; Rrepresents hydrogen, Calkyl, fluoroCalkyl, Ccycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy or haloCalkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it. 

Amino-heterocycles as VR-1 antagonists for treating pain

The present invention provides compounds of formula (I); pharmaceutically acceptable salts and N-oxides thereof in which A, B, D and E are C or N with the proviso that one or more are N, R, R, R, R, Rand Rare simple substituents, n is 0-3 and y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; as VR-1 antagonists for treating conditions or diseases in which pain and/or inflammation predominates; the use of the same for manufacturing medicaments, pharmaceutical compositions comprising them and methods of treatment utilizing them 

Heteroaromatic urea derivatives as VR-1 receptor modulators for treating pain

The present invention relates compounds of the formula (I): wherein R, R, R, R, R, R, R, R, Rand Rrepresent a variety of substituents, ring A is a phenyl or pyridyl ring; d is zero, 1 or 2; and pharmaceutically acceptable salts and N-oxides thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia 

Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents

The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia. 

Cyclohexane derivatives and their use as therapeutic agents

The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R, R, R, R, R, R, R, R, R, R, R, R?17, R, R, Rand Rare as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Cyclohexyl derivatives and their use as therapeutic agents

The present invention provides methods for the treatment of major depressive disorders comprising oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

Use of NK-1 receptor antagonists for treating major depressive disorders

2-aryl indole derivative as antagonists of tachykinins

Azaindole derivatives and their use as therapeutic agents

The present invention provides methods for the treatment or prevention of cognitive disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

Use of NK-1 receptor antagonists for treating cognitive disorders

The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I):

Spiro-azacyclic derivatives and their use as therapeutic agents

The present invention provides methods for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

The present invention provides a method for the treatment or prevention of schizophrenic disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

Use of NK-1 receptors antagonists for treating schizophrenic disorders

The present invention provides methods for the treatment or prevention of amnestic disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist.

Use of NK-1 receptor antagonists for treating amnestic disorders

The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.

Use of NK-1 receptor antagonists for treating stress disorders

Spiro-piperidine derivatives and their use as therapeutic agents

Growing community of inventors

Brentwood, United Kingdom

Gregory John Hollingworth