Merck Sharp + Dohme Corp.

Schering Corporation

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

Merck Sharp & Dohme LLC

Msd R&d Co., Ltd.

Umar Faruk Mansoor

M Arshad Siddiqui

Jongwon Lim

Phieng Siliphaivanh

Joseph A Kozlowski

David L Sloman

John M Sanders

Jared N Cumming

Amjad Ali

Michael D Altman

Xianhai Huang

David James Witter

Kun Liu

Vincent Stewart Madison

Jason D Brubaker

Kevin J Wilson

Alan B Northrup

Thomas H Graham

Thierry Olivier Fischmann

Ling Tong

Ping Liu

Christopher W Boyce

Solomon D Kattar

Duane E DeMong

Neng-Yang Shih

Wensheng Yu

Janeta Popovici-Muller

Dansu Li

Joey Lee Methot

Bandarpalle B Shankar

Raman Kumar Bakshi

Milana M Maletic

Vinay M Girijavallabhan

Peter Orth

Brian M Andresen

Michael K C Wong

Seong Heon Kim

Hua Zhou

Wei Liu

Yimin Qian

Lei Chen

Matthew H Daniels

Panduranga Adulla P Reddy

Craig R Gibeau

Charles A Lesburg

Qiaolin Deng

Yonglian Zhang

Chaoyang Dai

Anthony Donofrio

Matthew A Larsen

Brendan O'Boyle

Christian Fischer

Matthew Lloyd Childers

Christopher W Plummer

Lianyun Zhao

Wei Zhou

Jianping Pan

Luis E Torres

Salem Fevrier

Graham Frank Smith

Danielle Falcone

Shuyi Tang

Kathryn Ann Lipford

Gerald Wayne Shipps, Jr

Brian J Lavey

Zhuyan Guo

Guowei Zhou

De-Yi Yang

Kristin E Rosner

David Benjamin Belanger

Corey E Bienstock

Liping Yang

Patrick J Curran

Duan Liu

Alan B Cooper

Joseph Michael Kelly

David Joseph Guerin

Rongze Kuang

Jianmin Fu

Alessia Petrocchi

Yongqi Deng

Xiaolei Gao

Catherine M White

Yeon-Hee Lim

Jayaram R Tagat

Andrew J McRiner

Binyuan Sun

Hakan Gunaydin

Zhaoyang Meng

Ron Ferguson

Sobhana Babu Boga

Mehul F Patel

Hugh Y Zhu

Liang Zhu

Xiaohua Huang

Elizabeth Helen Kelley

Gerald W Shipps

Adam J Schell

Yang Nan

In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): and, and pharmaceutically acceptable salts thereof, wherein, R, n, R, and 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 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.

Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use

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

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.

The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors. 

KDM5 inhibitors

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting 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). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I). 

ERK inhibitors

The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

Inhibitors of IRAK4 activity

The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

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). 

Compounds that are ERK inhibitors

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). 

The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R, R, R, R, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.

Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors

The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. 

Heterocyclic compounds as ERK inhibitors

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Framingham, MA, United States of America

Umar Faruk Mansoor