Millennium Pharmaceuticals Limited

Merck Sharp + Dohme Corp.

Schering Corporation

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

Cor Therapeutics, Inc.

Lingyan Wang

Andrew William Stamford

Jared N Cumming

Ulrich Iserloh

William J Greenlee

Zhaoning Zhu

John P Caldwell

Zhong-Yue Sun

Robert M Scarborough

Penglie Zhang

Bing-Yan Zhu

Brian Alexander McKittrick

Yonghong Song

Tao Guo

Elizabeth M Smith

Corey Strickland

Yusheng Wu

Suresh D Babu

Erick A Goldman

Wenrong Huang

Kurt William Saionz

Yuanzan C Ye

Wenhao Li

Jingmei Zuckett

Rachael Catherine Hunter

Gang Qian

Michelle Lee Morris

Dawit Tadesse

Robert D Mazzola, Jr

Johannes H Voigt

Huizhong Gu

Thuy X H Le

Ying Huang

Guoqing Li

Jianping Pan

Yuefei Shao

Gaifa Lai

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Xiaoxiang Liu

Robert Mazzola

Johannes H Voight

Thuy X E Le

Jack D Scott

Eric J Gilbert

Xiaoiang Liu

Frank W Bennett

Ann E Weber

Stephane L Bogen

Younong Yu

Gabor Butora

Ian W Davies

Vinay M Girijavallabhan

Quang T Truong

Angela Dawn Kerekes

Yuhua Huang

Wei Li

Quang Truong

Thuy Xe Le

Rachel C Hunter

Thuy X Le

Rachael C Hunter

Michelle L Morris

Brian Mckittrick

Anne E Weber

Jr Robert D Mazzola

Robert D Mazzola

The present invention relates to 2'-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2&#x2032;-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2&#x2032;-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 

2'-alkynyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as 'ring B') of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or 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 Alzheimer's disease, are also disclosed. 

Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use

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 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.

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Benzamides and related inhibitors of factor Xa

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.

In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R, R, R, R, R, R, ring A, ring B, ring C, m, n, p, q, -L-, -L-, L-, and L- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. 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 in treating pathologies associated with amyloid beta (A&#x3b2;) protein, including Alzheimers Disease, are also disclosed. 

Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use

Benzamides and related inhibitors of factor XA

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 compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, U, X, R, R, R, and Rare as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds to inhibit aspartyl protease and to treat a variety of disease or disorders, including cardiovascular diseases, cognitive and neurodegenerative diseases. 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 antagonist

Growing community of inventors

East Brunswick, NJ, United States of America

Lingyan Wang