Merck Sharp + Dohme Corp.

Schering Corporation

Pharmacopeia Drug Discovery, Inc.

Schering-plough Corporation

Schering Coporation

Pharmacopeia Inc.

Junying Zheng

Robert G Aslanian

Christopher W Boyce

Kevin D McCormick

Younong Yu

Michael Berlin

Jianhua Chao

Manuel De Lera Ruiz

Walter Won

Pauline C Ting

Xianhai Huang

Rongze Kuang

Mwangi W Mutahi

Neng-Yang Shih

Purakkattle J Biju

Pietro Mangiaracina

Salem Fevrier

John J Baldwin

Arthur G Taveras

Anandan Palani

Dong Xiao

Daniel M Solomon

Wing C Tom

Ashwin Umesh Rao

Henry A Vaccaro

Xiaohong Zhu

J Robert Merritt

Ning Shao

Li Dong

Andrew William Stamford

Amjad Ali

Stuart B Rosenblum

Michael Man-Chu Lo

Rajan Anand

Qiaolin Deng

Yeon-Hee Lim

Paul Tempest

Wei Zhou

Nicolas Zorn

Heping Wu

Bo Liang

Joseph Michael Kelly

Ying Huang

Deping Wang

Philippe G Nantermet

Liangqin Guo

Thomas J Greshock

Ronald M Kim

Guoqing Li

Anthony J Roecker

Timothy J Henderson

Tao Yu

Jayaram R Tagat

Tony Priestley

Jie Wu

Chia-Yu Huang

Gang Zhou

Cynthia J Aki

Jae-Hun Kim

Gioconda V Gallo

James J Mulhearn

Ting Zhang

Edward Metzger

Daniel Lundell

Gaifa Lai

Hongwu Wang

Ruiyan Liu

Jay S Fine

Rong-qiang Liu

Minglang Wu

Lisa Guise-Zawacki

Stephanie Louise Ciesla

Youngong Yu

Angelo Reggiani

Walter S Won

Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: 'Z', Rand Rare defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease. 

Aminopyrazine compounds with A2A antagonist properties

Disclosed are compounds of Formula A, or a salt thereof: wherein R, R, and E are defined herein, which compounds have properties for inhibiting Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels

Disclosed are compounds of Formula G1: where 'R'. 'R' to &#x201c;R&#x201d;, &#x201c;n&#x201d;, &#x201c;m&#x201d;, &#x201c;p&#x201d;, &#x201c;W&#x201d;, &#x201c;X&#x201d;, &#x201c;Y&#x201d;, and &#x201c;Z&#x201d; are defined herein, which compounds are antagonists of Areceptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which Areceptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A anatagonist properties

Disclosed are compounds of Formula A: (structurally represented) where 'RG1', 'RG2a', &#x201c;RG4&#x201d;, &#x201c;RG5&#x201d;, &#x201c;MG1&#x201d;, &#x201c;n&#x201d; and &#x201c;m&#x201d; are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. 

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In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of &#x3b1;2C adrenergic receptor agonists, 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 conditions associated with the &#x3b1;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Biaryl-spiroaminooxzaoline analogues as alpha 2C adrenergic receptor modulators

In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of &#xff;2C adrenergic receptor agonists, 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 conditions associated with the &#xff;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Functionally selective alpha2C adrenoreceptor agonists

Biaryl spiroaminooxazoline analogues as Alpha2C adrenergic receptor modulators

In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as &#x3b1;2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the &#x3b1;2C adrenergic receptors using such compounds or pharmaceutical compositions.  

Derivatives and analogs of chroman as functionally selective ALPHA2C adrenoreceptor agonists

In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.

In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of &#x3b1;2C adrenergic receptor agonists, 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 conditions associated with the &#x3b1;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Biaryl-spiroaminooxazoline analogues as alpha 2C adrenergic receptor modulators

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: 

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Thiadiazoles as CXC- and CC- chemokine receptor ligands

In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as &#x3b1;2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the &#x3b1;2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

&#x3b1;2C adrenoreceptor agonists

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Isothiazole dioxides as CXC- and CC-chemokine receptor ligands

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein:

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New Providence, NJ, United States of America

Junying Zheng