280752-79-6Relevant articles and documents
Aromatic propionic acid derivative, preparation method and uses thereof
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, (2019/10/01)
The present invention discloses a compound represented by a general formula I or a tautomer, a racemate, an enantiomer, a diastereomer, a mixture and a pharmaceutically acceptable salt thereof, wherein each substituent is defined in the specification and claims. According to the present invention, the compound has obvious agonistic activity and selectivity to a GPR40 receptor in vitro, and the oral administration of the compound can significantly reduce the blood glucose concentration of rats after oral administration of glucose and increase the glucose tolerance capacity of rats in a dose-dependent manner so as to provide the good in vivo glucose lowering effect and achieve excellent pharmacokinetic properties and excellent drug-forming properties, such that the compound of the present invention can be used for the preparation of drugs for treating metabolic diseases such as diabetes and the like.
RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AS WELL AS PREPARATION METHOD AND USE THEREOF
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, (2019/01/11)
The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).
Enantioselective Access to Chiral 2-Substituted 2,3-Dihydrobenzo[1,4]dioxane Derivatives through Rh-Catalyzed Asymmetric Hydrogenation
Yin, Xuguang,Huang, Yi,Chen, Ziyi,Hu, Yang,Tao, Lin,Zhao, Qingyang,Dong, Xiu-Qin,Zhang, Xumu
, p. 4173 - 4177 (2018/07/29)
Rh-catalyzed asymmetric hydrogenation of various benzo[b][1,4]dioxine derivatives was successfully developed to prepare chiral 2-substituted 2,3-dihydrobenzo[1,4]dioxane derivatives using ZhaoPhos and N-methylation of ZhaoPhos ligands with high yields and excellent enantioselectivities (up to 99% yield, >99% enantiomeric excess (ee), turnover number (TON) = 24 000). Moreover, this asymmetric hydrogenation methodology, as the key step with up to 10 000 TON, was successfully applied to develop highly efficient synthetic routes for the construction of some important biologically active molecules, such as MKC-242, WB4101, BSF-190555, and (R)-doxazosin·HCl.