Merck Sharp + Dohme Corp.

Other

Schering Corporation

Wei Zhou

Xianhai Huang

Christopher W Boyce

Phieng Siliphaivanh

Anandan Palani

Robert G Aslanian

David James Witter

Kevin J Wilson

Joseph A Kozlowski

Jongwon Lim

Milana M Maletic

Jun Qin

Xiaohong Zhu

William J Greenlee

Amjad Ali

Dong Xiao

Kevin D McCormick

Hongjun Zhang

Younong Yu

David L Sloman

Joey Lee Methot

Purakkattle J Biju

Umar Faruk Mansoor

Matthew H Daniels

Yeon-Hee Lim

Salem Fevrier

Danielle Falcone

Brendan O'Boyle

Zhaoning Zhu

Michael Berlin

Robert D Mazzola, Jr

Raman Kumar Bakshi

Ashwin Umesh Rao

Junying Zheng

Jiayi Xu

Chad E Bennett

Thomas A Bara

Mihirbaran Mandal

Elizabeth Helen Kelley

Li Dong

Troy McCracken

Rachel Nicola MacCoss

Ning Shao

Hua Zhou

Andrew William Stamford

Brian Alexander McKittrick

Duane A Burnett

John W Clader

Hubert B Josien

Lei Chen

Dong-Ming Shen

Scott D Edmondson

Jason D Brubaker

Joseph Michael Kelly

Ying Huang

Ling Tong

Michael Man-Chu Lo

Pauline C Ting

Daniel M Solomon

Joshua Close

Cheng Zhu

David Joseph Guerin

Ying-Duo Gao

Dmitri A Pissarnitski

Hongmei Li

Rongze Kuang

Santhosh Francis Neelamkavil

Joon Jung

Alessia Petrocchi

Rajan Anand

Wanying Sun

Xiao Chen

John P Caldwell

Eric Mertz

Qiaolin Deng

Tao Yu

Manuel De Lera Ruiz

Christian Fischer

John W Butcher

Zhong-Yue Sun

Catherine M White

Jayaram R Tagat

Paul Tempest

Weiguo Liu

Haiqun Tang

Zhiqiang Zhao

Qin Jiang

Ron Ferguson

Heping Wu

Nicolas Zorn

Corey E Bienstock

Xiaoxiang Liu

Walter Won

Mwangi W Mutahi

Gang Zhou

Henry A Vaccaro

Michelle Martinez

Bart Harper

Meng Yang

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).

Compounds that are ERK inhibitors

The present invention provides a compound of Formula (I) and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds and said stereoisomers, and pharmaceutical compositions thereof, and methods for using said compounds and compositions for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein. 

Factor XIA inhibitors

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). 

Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). 

Disclosed are compounds of Formula A: (structurally represented) where 'RG1', 'RG2a', &#x201c;RG4&#x201d;, &#x201c;RG5&#x201d;, &#x201c;MG1&#x201d;, &#x201c;n&#x201d; and &#x201c;m&#x201d; are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. 

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The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

Substituted isoquinolines as CRTH2 receptor modulators

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). 

Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). 

This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTHreceptor. 

In many embodiments, the present invention provides novel heterocyclic compounds which are modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compositions.

Gamma secretase modulators

The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X, R, R, R, R, R, and Rare as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder. 

Fused tricyclic compounds for the treatment of inflammatory disorders

The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R, R, R, R, R, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction.

This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

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Scotch Plains, NJ, United States of America

Wei Zhou