Schering Corporation

Merck Sharp + Dohme Corp.

Li Qiang

Thavalakulamgara K Sasikumar

Duane A Burnett

Wen-Lian Wu

Martin Domalski

Jing Su

Deen Tulshian

Haiqun Tang

Lisa S Silverman

Julius J Matasi

Peter Korakas

Brian Alexander McKittrick

John W Clader

Hubert B Josien

Dmitri A Pissarnitski

Hongmei Li

Theodros Asberom

Zhiqiang Zhao

Ruo Xu

Chad E Bennett

Thomas A Bara

Chad E Knutson

Mark D McBriar

Murali Rajagopalan

David James Cole

William J Greenlee

Zhaoning Zhu

Yuanzan C Ye

Robert Mazzola

Mary Ann Caplen

Mary Anne Caplen

Martin S Domalski

Thomas Bara

Thavalakulamgar K Sasikumar

Sasikumar K Thavalakulamgara

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 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.

In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J-J, X, 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. 

mGluR1 antagonists as therapeutic agents

The present invention provides compounds, which, are novel antagonists for D/Dreceptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D/Dreceptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

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The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. Compounds of the invention generally have the structure: where the substituents are as defined herein.

Biaryltetrahydroisoquinoline piperidines as selective MCH receptor antagonists for the treatment of obesity and related disorders

In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J-J, X, and R&#x2014;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. 

The present invention discloses compounds of formula I wherein m, n, p, R, Rand X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Heterocyclyls as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders

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Edison, NJ, United States of America

Li Qiang