Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Min K Park

Brenda L Palucki

Tesfaye Biftu

Xianhai Huang

Yusheng Xiong

Clare London

Scott B Hoyt

Emma Louise Carswell

Paul David Ratcliffe

D Jonathan Bennett

Ravi P Nargund

William H Parsons

Prasun K Chakravarty

Zhixiong Ye

Bheemashankar A Kulkarni

Andrew John Cooke

Jaiqiang Cai

Bishan Zhou

David James Witter

Stephane L Bogen

David L Sloman

Haifeng Tang

Raman Kumar Bakshi

Purakkattle J Biju

Wanying Sun

Weiguo Liu

Weidong Pan

John K MacLean

Yi Zang

Chunhui Huang

Swapan Kumar Samanta

Iyassu K Sebhat

Khaled J Barakat

Qingmei Hong

Yingjie Lai

Louis L Zuegner, Iii, Legal Representative

John MacLean

Arthur A Patchett

Amjad Ali

Alexander Pasternak

Hongjun Zhang

Feroze Ujjainwalla

Jinlong Jiang

Zhicai Wu

Fa-Xiang Ding

Michelle R Machacek

Liangqin Guo

Joshua Close

Ryan D Otte

Helen Y Chen

Nunzio Sciammetta

Bing Li

Anthony K Ogawa

Yan Guo

Michael Hale Reutershan

Hyun O Ok

Craig R Gibeau

Catherine M White

Christian Fischer

Matthew Lloyd Childers

Lei Chen

Christopher W Plummer

Linda Brockunier

John W Lampe

Peter H Fuller

Brent Whitehead

Pengcheng Patrick Shao

Dann LeRoy Parker, Jr

Francesc Xavier Fradera Llinas

Jiaqiang Cai

Jerry Andrew Taylor

Kake Zhao

Andrew Cooke

Yang Yu

Alexander J Kim

Hongwu Wang

Rudrajit Mal

J Michael Ellis

Rosemary Sisco

Rohit Saxena

Sara Esposite

Daniel R McMasters

Patrick G Pollard

Edward Gonzalez

Louis L Zuegner Iii, Legal Representative

Archana Gupta

Michael Lo

Valdimir Simov

John Maclean

D Jonathan Bennet

Brent White-Head

Michael H Fisher

Brenda Palucki

The present invention relates to monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic. 

Chromane monobactam compounds for the treatment of bacterial infections

The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, Q, A, M, W, Rand Rare as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers. 

Tricyclic compounds as inhibitors of mutant IDH enzymes

The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers. 

This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

This invention relates to imidazopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Imidazopyridyl compounds as aldosterone synthase inhibitors

The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure. 

Aldosterone synthase inhibitors

Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Biaryl substituted triazoles as sodium channel blockers

Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Substituted triazoles as sodium channel blockers

Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

Piperazine urea derivatives as melanocortin-4 receptor agonists

Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Substituted piperidines as melanocortin receptor agonists

Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

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Whippany, NJ, United States of America

Min K Park