Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Msd K.k.

Other

Merck Sharp & Dohme LLC

Mark E Layton

Michael J Kelly, Iii

Philip E Sanderson

Joseph E Pero

Jian Liu

James J Perkins

Anthony J Roecker

Christopher James Bungard

Hong Liu

Kevin J Rodzinak

Michael A Rossi

Zhe Wu

Ian M Bell

Ashok Arasappan

Shawn J Stachel

Deping Wang

Jason M Cox

Christopher S Burgey

James J Mulhearn

Ting Zhang

Kristen L G Jones

Jun Liang

Dansu Li

Liangqin Guo

Ronald M Kim

Thomas J Greshock

Harry R Chobanian

Walter Won

Jiabing Wang

Michael J Breslin

Vadim Y Dudkin

Deodial Guy Guiadeen

Linda M Suen-Lai

Alexander J Reif

Yasuhiro Goto

Philippe G Nantermet

Toshihiro Sakamoto

Yoshio Ogino

Rajan Anand

Kenneth L Arrington

Scott E Wolkenberg

Xuanjia Peng

Lianyun Zhao

Nicholas D P Cosford

Zhijian Zhao

Essa H Hu

Jeffrey Curtis Kern

Hidetomo Furuyama

Nobuhiko Kawanishi

Anthony T Ginnetti

Gang Zhou

Takashi Mita

Kevin F Gilbert

Yiwei Li

Tianying Jian

Michael David VanHeyst

Pablo De Leon

Yu Onozaki

Xiu Wang

Akshay A Shah

Hannah D G F Lehman

Hannah D Fiji

Craig William Lindsley

Nigel J Liverton

Mark E Fraley

Mark T Bilodeau

John A McCauley

Melissa S Egbertson

Christopher D Cox

Younong Yu

Brian Andrew Stearns

Steven D Young

Jeannie M Arruda

Wayne J Thompson

Peter J Manley

Lida R Tehrani

Izzat Tiedje Raheem

Helen Y Chen

Tony Siu

John W Butcher

Brian T Campbell

Charles J McIntyre

Timothy John Hartingh

John E Stelmach

Jacob M Hoffman

Peter M Munson

Mehul F Patel

Hiroshi Hirai

Brian T Phillips

Akira Naya

Hidehito Kotani

Jeffrey W Schubert

Hannah Fiji

Christine Dieckhaus

Willie Whitter

Donna J Armstrong

Michael J Rossi

Jeffrey William Schubert

James T Olsen

Vadim Dudkin

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors

Disclosed are compounds of Formula A, or a salt thereof: Wherein 'A', R, R, R, R, and Rare as defined herein, which compounds have properties for blocking Nav 1.7 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 and neuropathic pain disorders using the same.

Hydroxypyrrolidine-substituted arylsulfonamide compounds with selective activity in voltage-gated sodium channels

2-amino-n-phenyl-nicotinamides as NAV1.8 inhibitors

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

2-amino-N-heteroaryl-nicotinamides as Na1.8 inhibitors

2-oxoimidazolidine-4-carboxamides as NA1.8 inhibitors

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders. 

2-amino-n-heteroaryl-nicotinamides as Na1.8 inhibitors

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 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-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-1 or their salts, and methods of treating pain (e.g. chronic pain), or cough or itch disorders using the same. 

N1-phenylpropane-1,2-diamine compounds with selective activity in voltage-gated sodium channels

Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein 'Het', R, and Rare defined herein, which 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 neuropathic pain disorders using the same. 

Benzoxazolinone compounds with selective activity in voltage-gated sodium channels

Disclosed are compounds of Formula A-a, or a salt thereof: Where 'B' and 'R' through &#x201c;R&#x201d; are as 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-a or their salts, and methods of treating neuropathic pain disorders using the same. 

Bicycloamine-substituted-N-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels

Disclosed are compounds of Formula Aand Formula A: wherein 'Heteroaryl-1', R, R, R, and Rare defined herein, which novel compounds have properties for blocking Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae Aand Aor their salts, and methods of treating neuropathic pain disorders using the same. 

N-substituted indazole sulfonamide compounds with selective activity in voltage-gated sodium channels

The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluRreceptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.

Imidazopyridin-2-one derivatives

Disclosed are compounds of Formula (A) or a salt thereof, wherein 'Het', R, and Rare defined herein, which 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 neuropathic pain disorders using the same. 

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Harleysville, PA, United States of America

Mark E Layton