Merck Sharp + Dohme Corp.

Walter and Eliza Hall Institute of Medical Research

Msd R&d (China) Co., Ltd.

Merck + Co., Inc.

Merch Sharpe & Dohme LLC

Michael J Kelly, Iii

Mark E Layton

Joseph E Pero

Michael A Rossi

Philip E Sanderson

Anthony J Roecker

James J Mulhearn

Ting Zhang

Bin Hu

John A McCauley

Dansu Li

David Brian Olsen

Jian Liu

James J Perkins

Deping Wang

Jason M Cox

Liangqin Guo

Hong Liu

Thomas J Greshock

Ronald M Kim

Zhuyan Guo

Scott E Wolkenberg

Lianyun Zhao

Christopher James Bungard

Walter Won

Kevin F Gilbert

Pablo De Leon

Zhiyu Lei

Brad Sleebs

Dongmei Zhan

Hannah D Fiji

Hannah D G F Lehman

Ian M Bell

Ashok Arasappan

Jun Liang

Younong Yu

Philippe G Nantermet

Christopher S Burgey

Helen Y Chen

Rajan Anand

Jiabing Wang

Zhijian Zhao

Essa H Hu

Jeffrey Curtis Kern

Timothy John Hartingh

Gang Zhou

Mehul F Patel

Yiwei Li

Tianying Jian

Kevin J Rodzinak

Zhe Wu

Michael David VanHeyst

Alexander J Reif

Alan F Cowman

Akshay A Shah

Jennifer K Thompson

Tony Triglia

Cailing Zhang

Paola Favuzza

Michael J Rossi

Donna J Armstrong

Swati I P Mercer

Methods of treating malaria comprising administration of compounds of Formula (I') or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating ainfection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

Antimalarial agents

The present invention provides methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating ainfection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

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

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-oxoimidazolidine-4-carboxamides as NA1.8 inhibitors

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. 

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

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 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. 

The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, 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.

Positive allosteric modulators of mGluR2

The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, 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.

Substituted 1,3-benzothiazol-2(3H)-ones and [1,3]thiazolo[5,4-B]pyridin-2(1H)-ones as positive allosteric modulators of mGluR2

The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. Compounds disclosed herein have the following chemical structure: 

Substituted naphthyridine compounds as inhibitors of Akt activity

The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Inhibitors of akt activtiy

Inhibitors of Akt activity

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Wayne, PA, United States of America

Michael J Kelly, Iii