916220-05-8Relevant 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.
supporting information, 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.
supporting information, 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
The 1,3-diaminobenzene-derived aminophosphine palladium pincer complex {C6H3[NHP(piperidinyl)2]2Pd(Cl)} - A highly active Suzuki-Miyaura catalyst with excellent functional group tolerance
Bolliger, Jeanne L.,Frech, Christian M.
experimental part, p. 1075 - 1080 (2010/06/17)
The rapidly prepared 1,3-diaminobenzenederived aminophosphine pincer complex {C6H3 [NHP(piperidinyl)2] 2Pd(Cl)} (1) is an effective Suzuki catalyst with excellent functional group tolerance. Side-product formations, such as homocoupling, debromation or protodeboration have only rarely been detected and if so, were in all cases below the 5% level. The presented reaction protocol is universally applicable. Experimental observations indicate that palladium nanoparticles are the catalytically active form of 1.
Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders
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Page/Page column 26, (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
