Schering Corporation

Jiangsu Hengrui Medicine Company Ltd.

Shanghai Hengrui Pharmaceutical Co., Ltd.

Merck Gmbh

Merck Sharp + Dohme Corp.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Rumin Zhang

William T Windsor

Vincent Stewart Madison

Corey Strickland

Gerald Wayne Shipps, Jr

Yaolin Wang

Jose S Duca

Paul Reichert

Shahriar Shane Taremi

Thomas E Hesson

Feng He

Yao Ma

Suxing Liu

Weikang Tao

M Arshad Siddiqui

Minsheng Zhang

Yongqi Deng

Lianyun Zhao

Hung V Le

Fengqi Zhang

Yinfa Yan

Patrick J Curran

David Parry

Charles W McNemar

Todd W Mayhood

Emma M Lees

Anthony F Mannarino

Gaolian Xie

James P Durkin

Ronald J Doll

F George Njoroge

Linghang Zhuang

Stephane L Bogen

Janeta Popovici-Muller

Jian Liu

Matthew Ernst Voss

Zhuyan Guo

Alan W Hruza

Dong Liu

Thierry Olivier Fischmann

Craig R Gibeau

Patricia C Weber

Latha G Nair

Weidong Pan

Brian M Beyer

Heping Wu

Yuan Tian

Bruce A Malcolm

Lata Ramanathan

Shelby P Umland

Jun Zou

Brian Robert Lahue

Mark A McCoy

Philip W Mui

Rong Liu

Michael G Murray

Feng X Zhu

Rong Kong

Elise M Siegel

David A Parry

Charles Wayne Mcnemar

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORγ) and pharmaceutical use thereof

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (ROR&#x3b3;) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of ROR&#x3b3;-mediated diseases or disorders. 

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (ROR&#x3b3;) and pharmaceutical uses thereof

This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers. 

CD73 inhibitors and therapeutic uses thereof

The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes.

Polynucleotides encoding soluble, stable forms of human double minute 2 polypeptides

The present invention relates to HDM2 polypeptides and mutants thereof which are complexed with various compounds, e.g., HDM2 inhibitors.

HDM2 polypeptides

In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.

Substituted piperidines that increase P53 activity and the uses thereof

HDM2 Polypeptides

Soluble, stable form of HDM2, crystalline forms thereof and methods of use thereof

The present invention provides, inter alia, peptide compositions and methods for treating and preventing Flaviviridae virus (e.g., hepatitis C virus) infections.

Peptide viral entry inhibitors

Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

High affinity quinoline-based kinase ligands

Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

High affinity thiophene-based and furan-based kinase ligands

The present invention discloses peptide substrates of a proteolytic ADAM33 polypeptide. The present invention also discloses methods of identifying additional substrates of a proteolytic ADAM33 polypeptide. Furthermore, the present invention discloses methods of identifying compounds that inhibit the proteolytic activity of a proteolytic ADAM33 polypeptide.

Peptide substrates of a proteolytic ADAM33 polypeptide and assays using the same

Azapeptides useful in the treatment of Hepatitis C

Novel chromogenic, fluorogenic and fluorescence polarization substrates which are useful in HCV NS3 protease and inhibitor assays.

Peptide substrates for HCV NS3 protease assays

An inhibitor of the HCV NS3 protease. The inhibitor is a subsequence of a substrate of the NS3 protease or a subsequence of the NS4A cofactor. Another inhibitor of the present invention contains a subsequence of a substrate linked to a subsequences of the NS4A cofactor. In another embodiment the inhibitor is a bivalent inhibitor comprised of a subsequence, a mutated subsequence or a mutated full-length of a substrate of the NS3 protease linked to a subsequence, a mutated subsequence or a mutated full-length suquence of the HCV NS4A cofactor.

Synthetic inhibitors of hepatitis C virus NS3 protease

Growing community of inventors

Edison, NJ, United States of America

Rumin Zhang