Compound and compositions as TGR5 agonists: WO2012082947

Abstract

The patent application WO2012082947 claims novel compounds as agonists of a plasma membrane-bound bile acid receptor TGR5. By activating TGR5, the agonists improve glycemic control and enhance energy expenditure. The basic generic claim of the patent covers pyrazole derivatives, different permutations on the core pyrazole ring are covered in the subsidiary claims. The claimed compounds are human TGR5 agonists having potency in the nM range.

Keywords::

• bile acid receptor
• GLP-1
• pyrazole derivatives
• TGR5

Acknowledgement

I thank the management of Zydus for the encouragement and for their suggestions.