Merck Sharp + Dohme Corp.

Schering Corporation

Other

Schering-plough Corporation

Chad E Bennett

Duane A Burnett

Wen-Lian Wu

Hongmei Li

Chad E Knutson

William J Greenlee

Anandan Palani

Hubert B Josien

Troy McCracken

Zhaoning Zhu

John W Clader

Xianhai Huang

Dmitri A Pissarnitski

Theodros Asberom

Zhiqiang Zhao

Ruo Xu

Thomas A Bara

Jun Qin

David James Cole

Monica L Vicarel

Andrew William Stamford

Jared N Cumming

Brian Alexander McKittrick

Robert G Aslanian

Jack D Scott

Elizabeth M Smith

Jing Su

Zhong-Yue Sun

Wei Zhou

Haiqun Tang

Thavalakulamgara K Sasikumar

Joel M Harris

Xiaoxiang Liu

Xiaohong Zhu

Mihirbaran Mandal

Martin Domalski

Li Qiang

Mark D McBriar

Hyunjin M Kim

Pawan Dhondi

Murali Rajagopalan

Eugenia Y Kiselgof

Dong Xiao

Younong Yu

Malcolm Maccoss

Deen Tulshian

Eric J Gilbert

Tin-Yau Chan

Xuanjia Peng

Henry M Vaccaro

Mary Ann Caplen

Yonggang Chen

Gioconda V Gallo

Peter Korakas

Thavalakulamgara K Sasiskumar

Mary Anne Caplen

Troy Mccracken

Martin S Domalski

Troy M Mccracken

Thomas Bara

Thavalakulamgar K Sasikumar

The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be 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 uses, including Alzheimer's disease, are also disclosed. 

5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): 

2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use

The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved. 

Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions. 

Gamma secretase modulators

In many embodiments, the present invention provides novel heterocyclic compounds which are modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compositions.

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). 

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.

The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

Azetidinone derivatives and methods of use thereof

In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J-J, X, Z, and R-Rare as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease. 

Fused tricyclic mGluR1 antagonists as therapeutic agents

In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J-J, X, Z, and R, R, and Rare as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease. 

Pyridothienopyridazinone derivatives as mGluR1 antagonists

Disclosed are compounds of the formula: and compounds of the formula: wherein R, R, R, R, R, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.

Azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism

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Metuchen, NJ, United States of America

Chad E Bennett