Merck Sharp + Dohme Corp.

Schering Corporation

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

Jianping Pan

Jared N Cumming

Guoqing Li

Andrew William Stamford

Ying Huang

Ulrich Iserloh

Corey Strickland

John P Caldwell

William J Greenlee

Zhaoning Zhu

Tao Guo

Yusheng Wu

Lingyan Wang

Zhong-Yue Sun

Brian Alexander McKittrick

Elizabeth M Smith

Suresh D Babu

Robert D Mazzola, Jr

Kurt William Saionz

Yuanzan C Ye

Yuefei Shao

Rachael Catherine Hunter

Michelle Lee Morris

Gang Qian

Huizhong Gu

Dawit Tadesse

Gaifa Lai

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Amjad Ali

Kun Liu

Ping Liu

Thomas H Graham

Duane E DeMong

Umar Faruk Mansoor

Jing Su

Johannes H Voigt

Qiaolin Deng

Christopher W Plummer

Weidong Pan

Yonglian Zhang

Xiaoxiang Liu

Mihir Mandal

Matthew A Larsen

Shu-Wei Yang

Elisabeth Hennessy

Johannes H Voight

Huijun Wang

Aaron Sather

Uma Swaminathan

Thuy X E Le

Christina B Madsen-Duggan

Marc A Labroli

Ginny Dai Ho

Sookhee Nicole Ha

Christine Yang

Zheng Tan

Sandra J Koseoglu

Sang Ho Lee

Terry Roemer

Christopher Michael Tan

Hao Wang

Andrew J Hoover

Xiaoiang Liu

William K Hagmann

Alexander Pasternak

Haifeng Tang

Fa-Xiang Ding

Douglas Walsh Hobbs

Li Xiao

Shuzhi Dong

Haiqun Tang

Dexi Yang

Thuy X H Le

Yuhua Huang

Jeffrey F Lowrie

Reynalda DeJesus

Thuy Xe Le

Brian Mckittrick

Robert D Mazzola

Thuy X Le

Rachael C Hunter

Michelle L Morris

Reynalda Dejesus

Jr Robert D Mazzola

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

Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic.

Benzimidazoles and indoles as taro inhibitors

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 inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic. 

The present invention relates to compounds of formula I that are metallo-&#x3b2;-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with &#x3b2;-lactam antibiotics for overcoming resistance. 

Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Heterocyclic aspartyl protease inhibitors

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein  Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I. Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

Cyclic amine bace-1 inhibitors having a heterocyclic substituent

Cyclic amine BACE-1 inhibitors having a heterocyclic substituent

Growing community of inventors

Monmouth Junction, NJ, United States of America

Jianping Pan