Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Canada Inc.

James J Perkins

Robert S Meissner

Mark E Duggan

Christopher James Bungard

George D Hartman

Barbara Hanney

John Howard Hutchinson

Jian Liu

Mark E Layton

Michael J Breslin

Ben C Askew

Ashok Arasappan

Jason M Cox

Hong Liu

Peter J Manley

Helen J Mitchell

Jiabing Wang

Zhe Wu

Ian M Bell

William F Hoffman

Michael A Patane

Yuntae Kim

Shawn J Stachel

Michael T Rudd

Christopher S Burgey

Harry R Chobanian

Timothy John Hartingh

Nathan C Ihle

Thomas G Steele

Antonella Converso

Jesse J Manikowski

Kristen L G Jones

Linda M Suen-Lai

Jeffrey Musselman

Michael R Krout

Paul J Coleman

Wasyl Halczenko

Michael J Kelly, Iii

Zhaoyang Meng

Anthony T Ginnetti

Deodial Guy Guiadeen

Adel M Naylor-Olsen

Youheng Shu

Pablo De Leon

Amy E Krause

David A Claremon

Yongxin Han

Melissa S Egbertson

John S Wai

Younong Yu

Robert R Wilkening

Deping Wang

Iyassu Sebhat

Liangqin Guo

Ronald M Kim

Helen Y Chen

Lushi Tan

Scott B Hoyt

Jessica Frie

Kenneth J Leavitt

Thorsten E Fisher

Aaron S Cote

Walter Won

Ting Zhang

Mehul F Patel

David B Whitman

William P Dankulich

Wenjie Li

Iyassu K Sebhat

Laura M Vassallo

Jeffrey W Schubert

Cecilia A Hunt

Yuan-Hon Kiang

Michael David VanHeyst

Aiwen Li

Karen M Brashear

Joyce Stellabott

John J Hutchinson

Benny C Askew

Akshay A Shah

Michael D Vanheyst

Jesse Josef Manikowski

Michael J Iii Kelly

Jeffrey D Musselman

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-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

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R, L, X, X, and X, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders. 

Tetrahydronaphthyridine derivatives as mGluR2-negative allosteric modulators, compositions, and their use

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The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) 

Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R, -L-, R, n, R, and Rare as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases. 

The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. 

2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [&#x192;]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

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Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Fluorinated 4-azasteroid derivatives as androgen receptor modulators

Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporesis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators

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Churchville, PA, United States of America

James J Perkins