Merck Sharp + Dohme Corp.

Schering Corporation

Other

Merck Canada Inc.

Thomas A Bara

Hubert B Josien

John W Clader

Duane A Burnett

Dmitri A Pissarnitski

Zhiqiang Zhao

Ruo Xu

Hongmei Li

Murali Rajagopalan

Wen-Lian Wu

Thavalakulamgara K Sasikumar

Chad E Bennett

Martin Domalski

Mark D McBriar

Anandan Palani

Cheng Zhu

Jing Su

Santhosh Francis Neelamkavil

Theodros Asberom

Wei Zhou

Haiqun Tang

Chad E Knutson

Li Qiang

David James Cole

William J Greenlee

Samuel Chackalamannil

Zhaoning Zhu

Amjad Ali

Yongxin Han

Robert G Aslanian

Qun Dang

Bin Hu

Xianhai Huang

Barbara A Pio

Michael W Miller

Scott D Edmondson

Dong-Ming Shen

Dong Xiao

Srikanth Venkatraman

Yan Xia

Jason M Cox

Zhuyan Guo

Ying-Duo Gao

John S Debenham

Patrick A Pinto

Jesse K Wong

Harry R Chobanian

Yan Guo

Wanying Sun

Mariappan Chelliah

Eric Mertz

Yeon-Hee Lim

Shouwu Miao

Christopher W Plummer

Linda Brockunier

Francisco Velazquez

Weiguo Liu

Unmesh G Shah

Jiayi Xu

Martin C Clasby

Jun Qin

Ping Lan

Austin Chen

Xiaohong Zhu

Sathesh P Bhat

Zhong Lai

Mihirbaran Mandal

Bart Harper

Paul E McNamara

Shengjian Li

Troy McCracken

Mary Ann Caplen

Meng Yang

Xian Liang

Hyunjin M Kim

Jinglai Hao

Zhongxiang Sun

Cangming Yang

Pawan Dhondi

Dipshikha Biswas

Charles Jayne

W Michael Seganish

Karen M Marcantonio

Chunrui Sun

Pradeep B Pushpavanam

Sherry A Shapiro

Zhe Feng

Mary Anne Caplen

Yan Jin

Vince J Colandrea

Martin S Domalski

Paul Mcnamara

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included. 

Hydroxy isoxazole compounds useful as GPR120 agonists

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

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 

Antidiabetic bicyclic compounds

The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

HCV NS3 protease inhibitors

Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)&#x2014;O&#x2014;C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)&#x2014;O&#x2014;C(O)-heteroaryl and a basic tertiary amine. 

Tetrahydropyranochromene gamma secretase inhibitors

This invention discloses novel gamma secretase inhibitors of the formula: Rand R, or Rand R, or Rand R, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein Ris a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I). 

Gamma secretase modulators

This invention discloses novel gamma secretase inhibitors of the formula: Rand R, or Rand R, or Rand R, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Disclosed are novel gamma secretase inhibitors of the formula:  Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).

Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors

The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentrating hormone (MCH). In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of the invention generally have the structure: where the substituents are as defined herein.

MCH antagonists for the treatment of obesity

Growing community of inventors

Linden, NJ, United States of America

Thomas A Bara