1142224-53-0Relevant articles and documents
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates
Brown, Sean P.,Dransfield, Paul,Vimolratana, Marc,Zhu, Liusheng,Luo, Jian,Zhang, Jane,Jiao, Xianyun,Pattaropong, Vatee,Wong, Simon,Zhuang, Run,Swaminath, Gayathri,Houze, Jonathan B.,Lin, Daniel C.-H.
supporting information, p. 757 - 760 (2018/06/18)
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets and enteroendocrine L-cells, and, when activated, elicits increased insulin secretion only in the presence of elevated glucose levels. We recently reported the discovery of AM-1638 (2), a full agonist of GPR40. Herein, we present further structure-activity relationships progressing from AM-1638 (2) to AM-6226 (14) that possesses a profile acceptable for dosing cynomolgus monkeys. The GPR40 full agonist AM-6226 (14) is the first molecule to display significant glucose lowering in cynomolgus monkeys providing additional evidence that GPR40 full agonists afford access to a powerful mechanism for maintaining glycemic control.
SPIROCYCLIC GPR40 MODULATORS
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Page/Page column 123; 124, (2010/04/30)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I'A or I'B, where the definitions of the variables are provided herein. The present invention also