1142232-49-2Relevant academic research and scientific papers
Improving the pharmacokinetics of GPR40/FFA1 full agonists
Du, Xiaohui,Dransfield, Paul J.,Lin, Daniel C.-H.,Wong, Simon,Wang, Yingcai,Wang, Zhongyu,Kohn, Todd,Yu, Ming,Brown, Sean P.,Vimolratana, Marc,Zhu, Liusheng,Li, An-Rong,Su, Yongli,Jiao, Xianyun,Liu, Jiwen,Swaminath, Gayathri,Tran, Thanhvien,Luo, Jian,Zhuang, Run,Zhang, Jane,Guo, Qi,Li, Frank,Connors, Richard,Medina, Julio C.,Houze, Jonathan B.
, p. 384 - 389 (2014/05/06)
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (1). Herein, we describe our efforts in improving the drug-like properties of the full agonists through the systematic introduction of polar groups in the C-, D-, and A-rings. This led to the discovery of new GPR40 full agonists with significantly improved pharmacokinetic propeties. Compound 8 and 20 also showed potent in vivo efficacy in oral glucose tolerance tests in mice in addition to the improvement in properties.
SPIROCYCLIC GPR40 MODULATORS
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Page/Page column 137; 138, (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
