Merck Sharp + Dohme Corp.

Schering Corporation

Opko Health, Inc.

Other

Msd Italia S.r.l.

Schering-Plough Corporation

Merck Sharp & Dohme LLC

Anandan Palani

Dong Xiao

Xianhai Huang

Robert G Aslanian

Ashwin Umesh Rao

John W Clader

Neng-Yang Shih

Hubert B Josien

Cheng Wang

Hon-Chung Tsui

Sunil Paliwal

Jun Qin

Ravi P Nargund

Brian Alexander McKittrick

Michelle Laci Wrobleski

Michael W Miller

Xing Dai

Peng Li

Shuwen He

Xiao Chen

Xuanjia Peng

Kevin D McCormick

Hongjun Zhang

Ying Huang

Hong Liu

Wei Zhou

Nicolas Zorn

Ning Shao

William J Greenlee

Bernard R Neustadt

Stuart W McCombie

Casey Cameron McComas

Christopher W Boyce

Richard Soll

Gregory A Reichard

Jayaram R Tagat

Susan F Vice

Li Dong

Symon Gathiaka

Sapna S Shah

Bahige M Baroudy

Ruo Steensma

Zhaoning Zhu

Qun Dang

Elizabeth M Smith

David L Sloman

Elisabetta Bianchi

Salem Fevrier

Zhong Lai

Mark D McBriar

Mark A Laughlin

Pawan Dhondi

Juan D Arredondo

Jared N Cumming

Jack D Scott

Younong Yu

Phieng Siliphaivanh

Eric J Gilbert

Antonello Pessi

Robert D Mazzola, Jr

Qiaolin Deng

Marc A Labroli

Chad E Bennett

Federica Orvieto

Xiaohong Zhu

Paul E Carrington

Jie Wu

Sylvia Joanna Degrado

Nigel J Liverton

Hao Wu

Yongxin Han

Duane A Burnett

Michael Berlin

Pauline C Ting

Joey Lee Methot

Thomas H Graham

Ryan D Otte

Purakkattle J Biju

Derun Li

Rongze Kuang

Jing Su

Hongmei Li

Abdelghani Achab

Walter Won

Timothy J Henderson

Jianhua Chao

Charles A Lesburg

Zhong-Yue Sun

Manuel De Lera Ruiz

Frank Narjes

Uwe Koch

Junying Zheng

Haiqun Tang

Min Lu

Ruo Xu

Joerg Habermann

Henry M Vaccaro

Troy McCracken

Indu T Bharathan

Elisabeth Hennessy

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, R, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Small molecule inhibitors of KRAS G12C mutant

Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

Arginase inhibitors and methods of use

Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, Rand the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

Long-acting co-agonists of the glucagon and GLP-1 receptors

Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases. 

Insulin dimers conjugated to peptides having at least one incretin activity are disclosed.

Insulin dimer-incretin conjugates

Co-agonists of the glucagon and GLP-1 receptors are described.

Co-agonists of the glucagon and GLP-1 receptors

Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NKreceptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

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In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I):  or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R, R, R, R, R, R, ring A, R, m, -L-, and Rare as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use

A NKantagonist having the formula (I), wherein Arand Arare optionally substituted phenyl or heteroaryl, Xis an ether, thio or imino linkage, Rand Rare not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

Growing community of inventors

Bridgewater, NJ, United States of America

Anandan Palani