1000413-84-2Relevant articles and documents
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold
Li,Liu, Chunxia,Yang, Jianyong,Zhou,Ye, Zhiwen,Feng,Yue, Na,Tong,Huang, Wenlong,Qian, Hai
, p. 608 - 622 (2019)
Based on an old phenoxyacetic acid scaffold, CPU014 (compound 14) has been identified as a superior agonist by comprehensive exploration of structure-activity relationship. In vitro toxicity study suggested that CPU014 has lower risk of hepatotoxicity than TAK-875. During acute toxicity study (5–500 mg/kg), a favorable therapeutic window of CPU014 was observed by evaluation of plasma profiles and liver slices. Moreover, CPU014 promotes insulin secretion in a glucose-dependent manner, while no GLP-1 secretion has been enhanced. Other than good pharmacokinetic properties, CPU014 significantly improved glucose tolerance both in normal and diabetic models without the risk of hypoglycemia. These subversive findings provided a safer candidate CPU014, which is currently in preclinical study to assess its potential for the treatment of diabetes.
(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.
PRODUCTION METHOD OF OPTICALLY ACTIVE DIHYDROBENZOFURAN DERIVATIVE
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Page/Page column 157-158, (2012/09/10)
Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like.