1000413-85-3Relevant articles and documents
(S) - 2 - (2,3-dihydrobenzo-furan-3-yl) acetic acid derivatives, its preparation process and its use in medicine
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, (2016/10/08)
The invention relates to an (S)-2-(2,3-dihydrobenzofuran-3-radical) acetic acid derivative, a preparation method of the derivative, a medicine composition containing the derivative and the application of the derivative serving as a therapeutic agent, particularly GPR40/FFA1, and particularly provides the (S)-2-(2,3-dihydrobenzofuran-3-radical) acetic acid derivative shown in a general formula (I), and pharmaceutically acceptable salts of the derivative or a prodrug of the derivative. The compound is an agonist of a GPR40/FFA1 receptor and has a good preventive and therapeutic effect on lots of GPR40-mediated diseases, especially diabetes mellitus. The invention also provides a preparation method of the compound.
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
ANTIDIABETIC TRICYCLIC COMPOUNDS
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Page/Page column 95, (2014/02/16)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.