Schering Corporation

Merck Sharp + Dohme Corp.

Other

Madera Therapeutics, LLC

Ruo Xu

John W Clader

Hubert B Josien

Dmitri A Pissarnitski

Hongmei Li

Theodros Asberom

Duane A Burnett

Zhiqiang Zhao

Thomas A Bara

Wen-Lian Wu

Thavalakulamgara K Sasikumar

Mark D McBriar

William J Greenlee

Zhaoning Zhu

Anandan Palani

Xianhai Huang

Jing Su

Zhong-Yue Sun

Haiqun Tang

Chad E Bennett

Martin Domalski

David James Cole

Andrew William Stamford

Jun Qin

Xiaohong Zhu

Chad E Knutson

Li Qiang

Gioconda V Gallo

Murali Rajagopalan

Yueqing Hu

Samuel Chackalamannil

Malcolm Maccoss

Robert D Mazzola, Jr

Jesse K Wong

Johannes H Voigt

Yuguang Wang

Xiaoxiang Liu

Paul E McNamara

Mary Ann Caplen

Troy McCracken

Xian Liang

Pawan Dhondi

Monica L Vicarel

Mary Anne Caplen

Yan Jin

Yunyong Liu

Martin S Domalski

Paul Mcnamara

Thomas Bara

Thavalakulamgar K Sasikumar

Compounds of formula (I), imidazopyrimidine ketones, as well as preparations and applications thereof. Compounds and pharmaceutically acceptable salts thereof which stimulate the body to produce tumor necrosis factor-related apoptosis-inducing ligands, while avoiding the drawbacks of existing cancer treatments based on recombinant proteins and antibodies. Thus, they can provide novel options for the treatment of related tumors. 

Imidazo-pyrimidone compounds, and preparation method and application thereof

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

Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)&#x2014;O&#x2014;C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)&#x2014;O&#x2014;C(O)-heteroaryl and a basic tertiary amine. 

Tetrahydropyranochromene gamma secretase inhibitors

Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L, n, X, Ar, Y, Z, Q, and Qare as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0. 

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

In its many embodiments, the present invention provides a novel class of heterocyclic compounds 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 diseases 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.

The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, 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 diseases 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 substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Disclosed are novel gamma secretase inhibitors of the formula:  Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).

Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors

The present invention discloses compounds which, are 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.

MCH antagonists for the treatment of obesity

A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological disorders: A representative example is:

Polycyclic guanine phosphodiesterase V inhibitors

A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:

Polycyclic guanine derivative phosphodiesterase V inhibitors

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Watchung, NJ, United States of America

Ruo Xu