Metabasis Therapeutics, Inc.

William Craigo

Serge H Boyer

Zhili Sun

Scott J Hecker

Venkat Reddy Mali

Qun Dang

Robert Huerta Lemus

Haiqing Li

Jorge E Gomez-Galeno

Matthew P Grote

Thanh Huu Nguyen

Paul D Van Poelje

Mingwei Chen

Raja K Reddy

K Raja Reddy

Bheemarao G Ugarkar

Mali Venkat Reddy

Serge Henri Boyer

Paul D Van Polje

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

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.

Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: 

Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs

Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs:  wherein:

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San Diego, CA, United States of America

William Craigo