916220-01-4Relevant academic research and scientific papers
Discovery of the imidazole-derived GPR40 agonist AM-3189
Ma, Zhihua,Lin, Daniel C.-H.,Sharma, Rajiv,Liu, Jinqian,Zhu, Liusheng,Li, An-Rong,Kohn, Todd,Wang, Yingcai,Liu, Jiwen,Bartberger, Michael D.,Medina, Julio C.,Zhuang, Run,Li, Frank,Zhang, Jane,Luo, Jian,Wong, Simon,Tonn, George R.,Houze, Jonathan B.
, p. 15 - 20 (2015/12/18)
As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.
Optimization of GPR40 agonists for type 2 diabetes
Liu, Jiwen,Wang, Yingcai,Ma, Zhihua,Schmitt, Mike,Zhu, Liusheng,Brown, Sean P.,Dransfield, Paul J.,Sun, Ying,Sharma, Rajiv,Guo, Qi,Zhuang, Run,Zhang, Jane,Luo, Jian,Tonn, George R.,Wong, Simon,Swaminath, Gayathri,Medina, Julio C.,Lin, Daniel C.-H.,Houze, Jonathan B.
, p. 517 - 521 (2014/06/09)
GPR40 (FFA1 and FFAR1) has gained significant interest as a target for the treatment of type 2 diabetes. TAK-875 (1), a GPR40 agonist, lowered hemoglobin A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patient
Conformationally constrained 3-(4-hydroxy-phenyl)-substituted-propanoic acids useful for treating metabolic disorders
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Page/Page column 42, (2008/06/13)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders
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Page/Page column 25, (2008/06/13)
The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I: wherein Q is an optionally substituted phenyl; L is a bond or O; P is a benzene or an optionally substituted thiazole r
