Merck Sharp + Dohme Corp.

Kallyope, Inc.

Albany Molecular Research, Inc.

Metabasis Therapeutics, Inc.

Nicox S.a.

Merck Canada Inc.

Merck Shapr & Dohme Corp.

Metabasas Therapeutics, Inc.

Iyassu Sebhat

Robert R Wilkening

Ahmet Kekec

Kenneth J Leavitt

Tesfaye Biftu

Ravi P Nargund

Ashok Arasappan

Zhicai Wu

Danqing D Feng

Bing Li

XiaoXia Qian

Ping Chen

Jacqueline D Hicks

Lan Wei

James M Apgar

Shuwen He

Christopher L Franklin

Amjad Ali

Qun Dang

Peter Guzzo

Jianming Bao

F Anthony Romero

Jinlong Jiang

Michael Man-Chu Lo

Nicoletta Almirante

Linus S Lin

Dariusz Wodka

Ping Lan

Hongjian Jiang

Tony Gibson

Huagang Lu

De Michael Chung

Gergely M Makara

Jian Liu

Scott B Hoyt

Stefano Biondi

Silvia Stefanini

David Chen

Dong-Ming Shen

Ennio Ongini

Duane E DeMong

Rajan Anand

Brett C Bookser

Daniel Cashion

Erin Guidry

Andy Kassick

David Wilson

Chris Franklin

Yongxin Han

Kathleen M Rupprecht

Robert S Meissner

James J Perkins

Thomas H Graham

Lin Yan

Robert K Baker

Zhi-Cai Shi

Peter J Manley

Lin Chu

James Francis Dropinski

Takao Suzuki

Christopher James Bungard

John J Acton, Iii

Laura Storoni

Pei Huo

Jessica Frie

Guizhen Dong

Bruce Sargent

Vincent Colandrea

Alan John Henderson

Mark Hadden

Tianying Jian

Troy McCracken

Alexander J Kim

Christopher R Moyes

Wensheng Liu

Allan James Goodman

Andrew Kassick

Zhifa Pu

Cheng Guo

Larry Yet

Peter H Dobbelaar

Massimiliano Ferrario

Alessia Nicotra

Michael M-c Lo

Michael M C Lo

Megan Ruenz

Michael M -c Lo

Xiaoxia Qian

Lisa Krug

Ann Weber

Brett Lauring

Nancy Thornberry

Paul Richards

Vincent J Colandrea

Tony S Gibson

John J Iii Acton

Troy Mccracken

This disclosure is directed, at least in part, to GPR40 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR40 agonists are gut-restricted compounds. In some embodiments, the GPR40 agonists are full agonists or partial agonists. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

GPR40 agonists

This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.

AMPK activators

This disclosure is directed, at least in part, to GPR119 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR119 agonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

GPR119 agonists

This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists, super agonists, full agonists, or partial agonists.

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I):  and ring B, n, R, R, R, R, and Rare as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild 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.

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2&#x2014;negative allosteric modulators, compositions, and their use

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

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Azabenzimidazole tetrahydrofuran derivatives

Indole derivatives useful as anti-diabetic agents

The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Benzimidazole hexahydrofuro[3,2-b]furan derivatives

Benzimidazole tetrahydrofuran derivatives

Novel compounds described herein are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Benzimidazole tetrahydropyran derivatives

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Azabenzimidazole tetrahydropyran derivatives

Azabenzimidazole hexahydrofuro[3,2-b]furan derivatives

Growing community of inventors

Jersey City, NJ, United States of America

Iyassu Sebhat