Novartis Ag

Aventis Pharmaceuticals Inc.

Constellation Pharmaceuticals, Inc.

Aventis Pharma Deutschland, Gmbh

Julian Roy Levell

Young Shin Cho

Yaping Wang

Gang Liu

Qian Zhao

Martin Sendzik

James Clifford Sutton

Cynthia Shafer

Michael David Shultz

Abran Q Costales

Thomas Raymond Caferro

Zhuoliang Chen

Fan Yang

Yong Mi Choi-Sledeski

James R Manning

Mark Czekaj

Yong Gong

Jonathan E Wilson

Michael Luzzio

Victor S Gehling

Bharat Lagu

Lawrence Blas Perez

Christopher Thomas Brain

Gregory Bernard Poli

Alan Collis

Peter Charles Astles

John William Giraldes

Avinash Khanna

Roy J Vaz

Paul R Eastwood

Heinz Pauls

William R Ewing

Heinz W Pauls

Keith Bruce Pfister

Kent W Neuenschwander

Troy Douglas Smith

Mark G Palermo

Bakary-Barry Toure

Jeffrey N Barton

Mark Gabriel Palermo

Alexandre Côté

Michael R Becker

Francois Lenoir

Huangshu Lei

Daniel Michael Green

Ludivine Moine

Francois Brucelle

Olivier Houille

Guyan Liang

Jehrod Burnett Brenneman

James R Pribish

Kennedy Taveras

Anna Gardberg

Alan John Collis

Jehrod B Brenneman

Simon Cornelis Van Der Plas

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

Modulators of TREX1

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compostions thereof, which are useful for treating a variety of conditions associated with methyl modifying enzymes. 

Modulators of methyl modifying enzymes, compositions and uses thereof

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT). 

P300/CBP hat inhibitors

P300/CBP HAT inhibitors

The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R, R, Rand R-Rare herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH

The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R, R, R, R-R, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Pyrrolopyrimidine compounds as inhibitors of CDK4/6

The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R-Rare defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer. 

The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R, R, R, R-R, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. 

The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R, P, Pand Pare as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.

Substituted propane phosphinic acid derivatives

This invention relates to compounds of formula which inhibit Factor Xa or tryptase, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa or tryptase.

1-aroyl-piperidinyl benzamidines

Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.

Chemical compounds

The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds

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Arlington, MA, United States of America

Julian Roy Levell