Merck Sharp + Dohme Corp.

Maze Therapeutics, Inc.

Walter Won

Junying Zheng

Pauline C Ting

Christopher W Boyce

Robert G Aslanian

Xianhai Huang

Michael Berlin

Younong Yu

Rongze Kuang

Kevin D McCormick

Deping Wang

Liangqin Guo

Ronald M Kim

Rajan Anand

Jianhua Chao

Ting Zhang

Gang Zhou

Anandan Palani

Dong Xiao

Philippe G Nantermet

Mark E Layton

Thomas J Greshock

Anthony J Roecker

Manuel De Lera Ruiz

Ashwin Umesh Rao

James J Mulhearn

Salem Fevrier

Li Dong

Ning Shao

Jie Wu

Andrew William Stamford

Amjad Ali

Michael Man-Chu Lo

Qiaolin Deng

Yeon-Hee Lim

Paul Tempest

Michael J Kelly, Iii

Heping Wu

Nicolas Zorn

Tianying Jian

Jae-Hun Kim

Gioconda V Gallo

David John Morgans, Jr

Joseph Michael Kelly

Jian Liu

James J Perkins

Jason M Cox

Christopher S Burgey

Hong Liu

Guoqing Li

Helen Y Chen

Timothy J Henderson

Tao Yu

Jayaram R Tagat

Wei Zhou

Christopher James Bungard

John E Stelmach

Kevin T Mellem

Mehul F Patel

Mwangi W Mutahi

Edward Metzger

Hongwu Wang

Patrick Sang Tae Lee

Christopher Joseph Sinz

Hannah L Powers

Youngong Yu

Michael J Iii Kelly

Disclosed are compounds of Formula (I), Formula (II), or a salt thereof: Formula (I) Formula (II) which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (I), Formula (II) or their salts, and methods of treating pain disorders, cough, and itch using the same.

4-amino or 4-alkoxy-substituted aryl sulfonamide compounds with selective activity in voltage-gated sodium channels

Provided herein are compounds of formula (I'): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y, Y, L, L, X, X, X, X, X, Q, R, R, R, R, and Rare as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I&#x2032;). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

Inhibitors of glycogen synthase 1 (GYS1) and methods of use thereof

Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and Rto Rare defined herein, which compounds have properties for blocking 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 cough, itch, acute pain and neuropathic pain disorders using the same. 

Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels

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, where Q, X, R1 and R2 are as 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 (acute, post-operative, neuropathic), or cough or itch disorders using the same. 

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

Biaryl spiroaminooxazoline analogues as Alpha2C adrenergic receptor modulators

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.

Functionally selective alpha2C adrenoreceptor agonists

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

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Alpine, NJ, United States of America

Walter Won