Glaxo Group Limited

Glaxosmithkline Intellectual Property Development Limited

Smithkline Beecham Corporation

The University of Edinburgh

Dr. Falk Pharma Gmbh

Kynos Therapeutics Limited

John Liddle

Ann Louise Walker

David Matthew Wilson

Deirdre Mary Bernadette Hickey

Michael David Barker

Alan D Borthwick

Andrew McMurtrie Mason

Neil Stuart Garton

Clement Douault

Stephen John Atkinson

Christopher Roland Wellaway

Anne Marie Jeanne Bouillot

Matthew Campbell

Robert John Sheppard

Hawa Diallo

Olivier Mirguet

Alexis Denis

Paul Graham Wyatt

Neil Derek Miller

Steven Leslie Sollis

David George Hubert Livermore

Fabrizio Nerozzi

Richard Jonathan Hatley

Deidre Mary Bernadette Hickey

Anne Louise Walker

Robert John Ife

Stephen Allan Smith

Paul Bamborough

Anna Katrin Szardenings

Francis Louis Atkinson

Robert William Ward

Jason Witherington

Dominique Amans

David Glynn Smith

David Haigh

Stephen Garland

Jessica Fanny Renaux

Vipulkumar Kantibhai Patel

Colin Andrew Leach

Steven James Stanway

Ivan Leo Pinto

Jeremy John Payne

John Martin Pritchard

Caroline Whitworth

Sebastien Andre Campos

Richard Peter Charles Cousins

Heather Hobbs

Paul Faulder

Duncan Stuart Holmes

Alexander George Steven Preston

Christopher Wellaway

Ann Walker

Deirdre Mary B Hickey

Stephen Allen Smith

Michael John Johnston

A compound of formula (I) or a salt thereof are provided: wherein R, X and Rare defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

3-(5-chloro-2-oxobenzo[d]oxazol-3(2H)-yl) propanoic acid derivatives as KMO inhibitors

Compounds of formula (I): wherein X, Y, Rand R-Rare as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis. 

Benzoimidazole derivatives as PAD4 inhibitors

The present invention relates to methods and/or uses for treating pancreatitis, kidney diseases and other various disorders as described herein, for conditions or disorders mediated by KMO inhibitors, which comprises administering 6-chlorobenzoxazine compounds of Formula (I): orpharmaceutically acceptable salts and/or corresponding pharmaceutical compositions thereof.

Method of treating pancreatitis using 1,4-benzoxazine derivatives

The present invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, which are Kynurenine monooxygenase (KMO) inhibitors, which are useful in the treatment of various disorders, which may include, but are not limited to, for diseases such as, for example: acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

3-(6-alkoxy-5-chlorobenzo[D]isoxazol-3-YL)propanoic acid useful as kynurenine monooxygenase inhibitors

3-(6-chloro-3-oxo-3,4-dihydro-(2H)-1,4-benzoxazin-4-yl) propanoic acid derivatives and their use as KMO inhibitors

Compounds of formula (I) wherein; Ris hydrogen or Calkyl; Ris hydrogen, Calkyl, perhalomethylCalkyl-O&#x2014;, or Calkoxy; Ris hydrogen, Calkyl, or CalkoxyCalkyl; Ris hydrogen, Calkyl, perhalomethylCalkyl; or unsubstituted CcycloalkylCalkyl; A is C&#x2014;Ror N; B is C&#x2014;Ror N; D is C&#x2014;Ror N; with the proviso that at least one of A, B, and D, is N; Ris hydrogen or Calkyl; Ris hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkoxy, or hydroxy; Ris hydrogen or Calkyl, with the proviso that one of Rand Ris hydrogen; Ris hydrogen or hydroxy; Ris hydrogen or Calkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

2-(azaindol-2-yl) benzimidazoles as PAD4 inhibitors

3-(6-alkoxy-5-chlorobenzo[d]isoxazol-3-yl)propanoic acid useful as kynurenine monooxygenase inhibitors

Compounds of formula (I) wherein; Ris hydrogen or Calkyl; Ris hydrogen, Calkyl, perhalomethylCalkyl-O&#x2014;, or Calkoxy; Ris hydrogen, Calkyl, or CalkoxyCalkyl; Ris hydrogen, Calkyl, perhalomethylCalkyl; or unsubstituted CcycloalkylCalkyl; A is C&#x2014;Ror N; B is C&#x2014;Ror N; D is C&#x2014;Ror N; with the proviso that at least one of A, B, and D, is N; Ris hydrogen or Calkyl; Ris hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkoxy, or hydroxy; Ris hydrogen or Calkyl, with the proviso that one of Rand Ris hydrogen; Ris hydrogen or hydroxy; Ris hydrogen or Calkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis. 

2-(azaindol-2-yl) benz imidazoles as PAD4 inhibitors

Compounds of formula (1) wherein Ris 2-indanyl, Ris 1-methylpropyl, Ris 2-methyl-1,3-oxazol-4-yl and Rand Rtogether with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.

Substituted diketopiperazines and their use as oxytocin antagonists

A compound of formula (I): or a salt thereof;which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.

Compounds

Compounds of formula (I) wherein Ris 2-indanyl, Ris 1-methylpropyl, Ris a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, Rrepresents methyl and Rrepresents hydrogen or methyl or, Rand Rtogether with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.

2-(azaindol-2-yl)benzimidazoles as PAD4 inhibitors

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John Liddle