title: 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.
authors: Zydus Research Centre, Moraiya, Ahmedabad 382210, India. saurinraval@zyduscadila.com
authors: Saurin
authors: S
authors: Raval
mesh_terms: D000818:Animals; D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000378:metabolism; D004335:Drug and Narcotic Control; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D015394:Molecular Structure; D010330:Patents as Topic; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C473772:GPBAR1 protein, human; D007004:Hypoglycemic Agents; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled