Merck Sharp + Dohme Corp.

Metabasis Therapeutics, Inc.

Sankyo Company, Limited

Merck Canada Inc.

Alectos Therapeutics Inc.

Msd Italia S.r.l.

Metabasas Therapeutics, Inc.

Qun Dang

Mark D Erion

K Raja Reddy

Scott J Hecker

Srinivas Rao Kasibhatla

Robert Huerta Lemus

Zhili Sun

Stephane L Bogen

David Brian Olsen

Vinay M Girijavallabhan

Brett C Bookser

Ravi P Nargund

Ian W Davies

Anandan Palani

Venkat Reddy Mali

Peng Li

Serge H Boyer

Xing Dai

Shuwen He

Iyassu Sebhat

Xuanjia Peng

F George Njoroge

Frank W Bennett

Ashok Arasappan

Casey Cameron McComas

Jianming Bao

F Anthony Romero

Raja K Reddy

Hong Liu

Richard Soll

Angela Dawn Kerekes

Vishal Verma

Dariusz Wodka

Nicolas Zorn

Andrew William Stamford

Joseph P Vacca

Hubert B Josien

Bin Hu

Changyou Zhou

Dong Xiao

Feng Tian

Purakkattle J Biju

Dmitri A Pissarnitski

Takao Suzuki

Nicholas Brian Raffaele

Nigel J Liverton

Lihu Yang

William K Hagmann

Hao Wu

Sheo B Singh

Ying Huang

Jinlong Jiang

Robert R Wilkening

Cheng Zhu

Dongfang Meng

Bing Li

Linus S Lin

Jing Su

Frank Narjes

Uwe Koch

Latha G Nair

Zhengxia Chen

Ahmet Kekec

Weidong Pan

Joerg Habermann

James M Apgar

Harold G Selnick

Tesfaye Biftu

Amjad Ali

Michael D Altman

Barbara A Pio

Ernest John McEachern

John S Wai

Yuanxi Zhou

Steven L Colletti

Alan B Northrup

Maria Emilia Di Francesco

Jason M Cox

Solomon D Kattar

Bowei Wang

John S Debenham

Derun Li

Andrew M Haidle

Harry R Chobanian

Ping Chen

David Jaro Vocadlo

James Patrick Jewell

Rajan Anand

John Michael Ellis

De-Yi Yang

Christian Fischer

Linda Brockunier

Timothy A Blizzard

Christopher W Plummer

Quang T Truong

John J Acton, Iii

Brandon Mitsuo Taoka

Anilkumar G Nair

David Jonathan Bennett

Corey E Bienstock

Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof. Formula I 

Glucagon antagonists

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included. 

Hydroxy isoxazole compounds useful as GPR120 agonists

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof and pharmaceutical compositions comprising the same.

Antagonists of the glucagon receptor

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 

Antidiabetic tricyclic compounds

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof. 

The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Activators of glucokinase

The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections byby administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

Nargenicin compounds and uses thereof as antibacterial agents

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 

Antidiabetic substituted heteroaryl compounds

The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 

Cyclic phosphonate substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Glycosidase inhibitors and uses thereof

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. 

Indole derivatives useful as anti-diabetic agents

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Westfield, NJ, United States of America

Qun Dang