Merck Sharp + Dohme Corp.

Galapagos Nv

Merck Sharpe & Dohme Corp.

Merck & Dohme Limited

Stephen Robert Fletcher

Frank Burkamp

Mark Stewart Chambers

Luke Jonathan Alvey

Victor G Matassa

Gregory John Robert Newsome

Peter Blurton

Frédéric Gilbert Labéguère

Laurent Raymond Maurice Sanière

Angus Murray MacLeod

Monique Bodil Van Niel

Martin Richard Teall

Christel Jeanne Marie Menet

Christopher Richard Moyes

Alastair James Hodges

Koen Kurt Smits

Javier Blanc

Luc Juliaan Corina Van Rompaey

Susan Koon-Fung Cheng

Nolwenn Jouannigot

Timothy Harrison

Ian James Collins

Michael Rowley

Graham A Showell

Alan John Nadin

Paul David Leeson

Timothy Jason Sparey

Edward Giles McIver

A Brian Jones

Daniel Spinks

Mark G Bock

Leslie Joseph Street

Jose Luis Castro Pineiro

William Robert Carling

Kevin J Wilson

Richard Thomas Lewis

Wesley Peter Blackaby

Kevin William Moore

Gregory John Hollingworth

Paul Joseph Oakley

Michael Geoffrey Russell

Sarah Christine Hobbs

Stephen John Lewis

Sylvie Bourrain

Edward Giles Mciver

Andrew S Jennings

Elizabeth Mary Naylor

Joanne Thomson

Laurent Raymond Maurice Saniére

Graham David Checksfield

Lauren Rogers

Frédéric Gilbert Labéguére

Laurent Raymond Maurice SANIÈRE

Frédéric Gilbert LABÉGUÈRE

Frédéric LABÉGUÈRE

Gregory Newsome

Laurent SANIÈRE

A compound according to Formula Ia: wherein L, G, and Rare as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

Dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

[1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

Compounds useful for the treatment of degenerative and inflammatory diseases

A compound according to Formula (Ia), wherein Cy, L, G, and Rare as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

Dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (GPR84 antagonists)

Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease. 

Tetrahydroindole derivatives for treatment of alzheimer's disease

The present invention provides compounds of formula (I), wherein both p's are one or two, Ris generally heteroaryl or cycloalkyl, Ris Ccycloalkyl or phenyl and Ris heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation. 

Piperidine and azetidine derivatives as GlyT1 inhibitors

Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1). 

Indazol-3-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (VR1)

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

A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, 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.

Pyridazine derivatives as ligands for GABA receptors

The present invention provides a compound of formula (I): in which Ar and Rare phenyl or a heteroaromatic group, Ris generally hydrogen, Ris hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammation 

Substituted-1-phthalazinamines as vr-1 antagonists

A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine ring are selective antagonists of the human 5-HTreceptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and other psychotic disorders.

Phenylsulphonylipiperazinyl derivatives as 5-HT receptor ligands

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Bishops Stortford, United Kingdom

Stephen Robert Fletcher