Merck Sharp + Dohme Corp.

Msd R&d (china) Co., Ltd.

Jiangsu Hengrui Medicine Company Ltd.

Shanghai Hengrui Pharmaceutical Co., Ltd.

Merck + Co., Inc.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Msd R&d Co., Ltd.

Fengqi Zhang

Jianming Bao

Michael Man-Chu Lo

Robert D Mazzola, Jr

Xiaolei Gao

Sandra Lee Knowles

John J Acton, Iii

Chunsing Li

Melissa S Egbertson

Ling Tong

David M Tellers

Scott T Harrison

Oleg B Selyutin

Feng He

Emma R Parmee

Minsheng Zhang

Michael T Rudd

Songnian Lin

Timothy J Henderson

Qiaolin Deng

Petr Vachal

Rumin Zhang

Zhaoyang Meng

Guizhen Dong

Vincent Colandrea

Yinfa Yan

Debra L Ondeyka

Ronald Dale Ferguson, Ii

Suxing Liu

Meng Na

Andrew William Stamford

Weikang Tao

Zhijian Lu

Yuan Cheng

Rui Liang

David Askin

Kevin Tyler Chapman

James R Tata

Richard John Varsolona

Lin Chu

Milana M Maletic

Dong Liu

Subharekha Raghavan

Rajan Anand

James Francis Dropinski

Takao Suzuki

Xibin Liao

Joseph Leslie Duffy

James J Mulhearn

Nancy J Kevin

John E Stelmach

Deyou Sha

R Scott Hoerrner

Thomas A Rano

Feng Ye

Edward Metzger

Zhiqiang Yang

Libo Xu

Yi Zang

Kake Zhao

Vanessa L Rada

Jonathan E Wilson

Alexander J Kim

Joseph D Armstrong, Iii

Jeffrey W Schubert

Sunita V Dewnani

Robert M Purick

Brian Anthony Kirk

Daniel E Petrillo

Fred Fleitz

Christian P Stevenson

Aaron Zwicker

Tracy Huening

Maud Reiter

John J Iii Acton

Vincent J Colandrea

Robert D Mazzola

Ronald Iii Ferguson

Sandra L Knowles

Scott Timothy Harrison

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 is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor

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

The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention relates to bicyclic himbacine derivatives of the formula  and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.

Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists

Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. 

Cyclic amine substituted heterocyclic CETP inhibitors

Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. 

Substituted benzopiperazines as CETP inhibitors

Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

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Edison, NJ, United States of America

Fengqi Zhang