865233-34-7Relevant articles and documents
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents
Ye, Zhiwen,Liu, Chunxia,Zou, Feng,Cai, Yan,Chen, Bin,Zou, Yuxing,Mo, Jiaxian,Han, Ting,Huang, Wenlong,Qiu, Qianqian,Qian, Hai
, (2020/06/19)
Free fatty acid receptor 1 (FFA1 or GPR40) has been studied for many years as a target for the treatment of type 2 diabetes mellitus. In order to increase potency and reduce hepatotoxicity, a series of novel compounds containing imidazo[1,2-a]pyridine sca
A class of GPR40 agonist compounds with amide structure, and uses thereof
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, (2019/05/02)
The present invention relates to a class of amide compounds with a novel structure, and a pharmaceutical composition thereof, wherein the structure of the amide compound is represented by a general formula (I). According to the present invention, the amide compound (I) can regulate GPR40 activity, and can be used for GPR40 activity related diseases such as diabetes and metabolic syndrome. The formula I is defined in the specification.
3-PHENYL-4-HEXYNOIC ACID DERIVATIVES AS GPR40 AGONISTS
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, (2019/07/23)
A compound of the formula (I)wherein R represents a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated, or a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated and wherein one or more of hydrogen atoms is replaced with fluorine atom; X represents hydrogen atom or halogen atom,and* denotes chiral center, and salts thereof. The compound is useful for the treatment of diseases mediated by GPR40, in particular type II diabetes. (I)
NOVEL PHENYL PROPIONIC ACID DERIVATIVES AND USES THEREOF
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, (2018/07/05)
The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of meta
AGONISTS OF GPR40
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, (2012/02/05)
The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are there-fore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
AMG 837: A potent, orally bioavailable GPR40 agonist
Houze, Jonathan B.,Zhu, Liusheng,Sun, Ying,Akerman, Michelle,Qiu, Wei,Zhang, Alex J.,Sharma, Rajiv,Schmitt, Michael,Wang, Yingcai,Liu, Jiwen,Liu, Jinqian,Medina, Julio C.,Reagan, Jeff D.,Luo, Jian,Tonn, George,Zhang, Jane,Lu, Jenny Ying-Lin,Chen, Michael,Lopez, Edwin,Nguyen, Kathy,Yang, Li,Tang, Liang,Tian, Hui,Shuttleworth, Steven J.,Lin, Daniel C.-H.
, p. 1267 - 1270 (2012/03/26)
The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in GPR40 agonists as potential antidiabetic agents. Optimization of a series of β-substituted p
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CANCER
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, (2012/08/07)
New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of
Development of a scalable synthesis of a GPR40 receptor agonist
Walker, Shawn D.,Borths, Christopher J.,Divirgilio, Evan,Huang, Liang,Liu, Pingli,Morrison, Henry,Sugi, Kiyoshi,Tanaka, Masahide,Woo, Jacqueline C. S.,Faul, Margaret M.
, p. 570 - 580 (2011/12/04)
Early process development and salt selection for AMG 837, a novel GPR40 receptor agonist, is described. The synthetic route to AMG 837 involved the convergent synthesis and coupling of two key fragments, (S)-3-(4-hydroxyphenyl) hex-4-ynoic acid (1) and 3-
Novel Spiropiperidine Compounds
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, (2011/05/03)
A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
Walsh, Shawn P.,Severino, Alexandra,Zhou, Changyou,He, Jiafang,Liang, Gui-Bai,Tan, Carina P.,Cao, Jin,Eiermann, George J.,Xu, Ling,Salituro, Gino,Howard, Andrew D.,Mills, Sander G.,Yang, Lihu
, p. 3390 - 3394 (2011/06/24)
The design, synthesis, and structure-activity relationship (SAR) for a series of β-substituted 3-(4-aryloxyaryl)propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further profiling of compound 7 is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model.