Janssen Pharmaceutica Nv

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Other

University of Utah Research Foundation

The University of North Carolina at Chapel Hill

Dana-farber-cancer Institute Inc.

Whitehead Institute for Biomedical Research

Illumina Corporation

Li Liu

Mark E McDonnell

Mark J Macielag

Bin Benjamin Zhu

Yue-Mei Zhang

Haiyan Bian

Shu-Chen Lin

Philip Michael Pitis

Sui-Po Zhang

Jose Clemente

Kristen Chevalier

John Mabus

Chris Flores

Pete Connolly

Scott L Dax

Bart L DeCorte

Peter J Connolly

Steven J Coats

Wei He

James J McNally

Henry Joseph Breslin

Bart L De Corte

Min Shen

Matthew Brian Boxer

Chaozhong Cai

Ashis Kumar Saha

David William End

Kyle Ryan Brimacombe

Steve Coats

Jason Matthew Rohde

Bart Lieven Daniel De Corte

Bruce E Maryanoff

William Alvin Kinney

Xiaodong Wang

Christopher M Flores

Anton Simeonov

Gilles C Bignan

Ajit Jadhav

Martin J Walsh

Shyamali Ghosh

Stephen M Prouty

Andrew Louis McIver

Matthew J Todd

Douglas S Auld

Tamara A Miskowski

Rajan Pragani

Mindy Irene Emily Davis

Marina I Nelen

Erica L Nulton

Kent Lai

Manshu Tang

Surendra Karavadhi

Cordelle D Tanega

Mark E Mcdonnell

Kristen M Chevalier

Steven A Rosenberg

John R Carson

Richard A Morgan

Min-Jui Richard Shen

Donald William Ludovici

Dana L Johnson

Madhavan Nair

David Sabatini

Matthew E Hall

Mark J Schulz

Daniel Jason Urban

Edward A Berger

Xun Li

Richard William Connors

Barna Dey

Ganesha Rai Bantukallu

Natalia Martinez

Michael Pacold

Bhavik Patel

Jim McNally

Mark MacIelag

Yuhong Fang

Wei Zhao

Mustafa H Ghanem

Jonathan Toung

Ruoyu Zhang

Mark M McDonnell

Andrew Louis Mciver

Mindy Irene Davis

Matthew Hall

Mark Mcdonnell

The present invention provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.

Inhibitors of phosphoglycerate dehydrogenase (PHGDH) and uses thereof

A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; Rand Rare each independently a halogen, CN, CF, CHF, CHF, a C-C10alkyl group, a C1-Calkoxy group, a di(C-Calkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.

Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer

Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X, X, Rand Rare disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed. 

Mutant IDH1 inhibitors useful for treating cancer

Disclosed are inhibitors of human galactokinase of formula (I) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I). 

Galactokinase inhibitors for the treatment and prevention of associated diseases and disorders

Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I). 

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R, Y, R, R, and Rare defined herein.

Phenoxy-substituted pyrimidines as opioid receptor modulators

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R, R, R, R, and Y are defined herein.

4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: 

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R, R, R, and L, A, and Rare defined herein.

Pyrimidine compounds as delta opioid receptor modulators

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Doylestown, PA, United States of America

Li Liu