Merck Sharp + Dohme Corp.

Intervet Inc.

Duane E DeMong

Michael W Miller

Andrew William Stamford

Christopher W Plummer

Xing Dai

Jack D Scott

Kallol Basu

Jared N Cumming

Ping Liu

Matthew A Larsen

William J Greenlee

Hong Liu

Harry R Chobanian

Yan Guo

Zhiyong Hu

Amjad Ali

Kun Liu

Barbara A Pio

Dong Xiao

Thomas H Graham

Thomas J Greshock

Helen Y Chen

Umar Faruk Mansoor

Qiaolin Deng

Marc Poirier

Paul Tempest

Yonglian Zhang

Joel M Harris

Jianping Pan

Elisabeth Hennessy

Huijun Wang

Wei Li

Aaron Sather

Uma Swaminathan

Michael D Altman

John A McCauley

Ashok Arasappan

Scott D Edmondson

Steven L Colletti

Robert R Wilkening

Iyassu Sebhat

Eric J Gilbert

Harold B Wood

Ryan D Otte

Andrew M Haidle

Wanying Sun

James Patrick Jewell

De-Yi Yang

Benjamin Wesley Trotter

Scott B Hoyt

Min Lu

Brandon D Cash

Andrew J Hoover

Joseph A Kozlowski

John M Sanders

Bernard R Neustadt

William K Hagmann

Ravi P Nargund

Paul E Finke

Bin Hu

Wensheng Yu

Jongwon Lim

Brian J Lavey

Gregori J Morriello

Bowei Wang

Cheng Zhu

Milana M Maletic

Michael K C Wong

Rajan Anand

Guowei Zhou

Timothy J Henderson

Matthew Lloyd Childers

Linda Brockunier

Liping Wang

Quang T Truong

Brandon Mitsuo Taoka

William Bert Geiss

Lehua Chang

Yuping Zhu

Anilkumar G Nair

Kevin D Dykstra

Vincent Colandrea

Ronald K Chang

Zhiqiang Guo

Nam Fung Kar

Alejandro Crespo

Jason W Szewczyk

Joie Garfunkle

Kake Zhao

Christopher R Moyes

Cangming Yang

Heather E Stevenson

Karen M Marcantonio

Yong Huang

Chander Shekher Celly

Jonathan T Kern

Matthew J H Clements

Marc Poirer

Megan Macala

Sarah W Li

In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use

In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, Rand Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2and/or A2receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2receptor and/or the adenosine A2receptor.

9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use

Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R, R, R, R, R, R, R, A, X, X, and Xare defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

Aza-benzothiophene compounds as STING agonists

In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, Rand Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

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 Formula (I). 

Antidiabetic bicyclic compounds

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. 

The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R9, and A are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved. 

Compounds inhibiting leucine-rich repeat kinase enzyme activity

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I):  and ring B, n, R, R, R, R, and Rare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer. 

Sting agonist compounds

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2&#x2014;negative allosteric modulators, compositions, and their use

[7,6]-fused bicyclic antidiabetic compounds

[5,6]&#x2014;fused bicyclic antidiabetic compounds

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 compounds

Growing community of inventors

Hanover, MA, United States of America

Duane E DeMong