Merck Sharp + Dohme Corp.

Michael John Mayer

Hubert B Josien

Jason Louis Davis

William J Greenlee

John W Clader

Robert Jason Herr

Shuangyi Wan

Kai Deng

Ming Min Hsia

This invention provides for certain bridged and fused compounds of the formulaG-L-A&#x2003;&#x2003;Ior a pharmaceutically acceptable salt, ester of solvate thereofwherein: and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

Bridged and fused antidiabetic compounds

This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N&#x2014;N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. 

Phthalazine-containing antidiabetic compounds

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Altmont, NY, United States of America

Michael John Mayer