1061314-04-2Relevant articles and documents
A new and improved process for C-aryl glucoside SGLT2 inhibitors
Liu, Yonghai,Fu, Tingming,Chen, Zhidong,Ou, Chunyan
, p. 1715 - 1721 (2015/09/15)
A practical and scalable synthesis of C-glycosides identified as highly potent sodium-dependent glucose transporter 2 (SGLT2) inhibitors is described. Highlights of the synthetic process are a concise, ten-step synthesis of a structurally complex active pharmaceutical ingredient from a known intermediate via a selective and quantitative addition of an aryl species to the Weinreb amide, and the isomers of undesired ortho-products were avoided during the preparation. The chemistry developed has been applied to prepare SGLT2 inhibitors without recourse to chromatography.
Pyrano[3,2-c]benzopyran-6(2h)-one derivatives and uses thereof
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, (2013/04/10)
The present invention relates to new pyrano[3,2-c]benzopyran-6(2H)-one derivatives that act as SGLT2 inhibitors, which makes them promising candidates for the treatment of diabetes and other diseases and conditions mediated by SGLT2. These new drugs also exhibit platelet aggregation inhibitory activity which makes them promising candidates in the treatment and/or prevention of prothrombotic conditions. The invention also relates to the use of such pyrano[3,2-c]benzopyran-6(2H)-one derivatives in the treatment or prevention of the diabetes and other disorders and conditions mediated by SGLT2, as a single active ingredient or in combination with another antidiabetic agent or a drug for the treatment of hypertension, chronic heart failure or atherosclerosis, and pharmaceutical compositions comprising said new pyrano[3,2-c]benzopyran-6(2H)-one derivatives.
Conformationally constrained spiro C-arylglucosides as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
Lv, Binhua,Feng, Yan,Dong, Jiajia,Xu, Min,Xu, Baihua,Zhang, Wenbin,Sheng, Zelin,Welihinda, Ajith,Seed, Brian,Chen, Yuanwei
scheme or table, p. 827 - 831 (2011/02/22)
(Chemical Equation Presented) Sodium glucose co-transporter 2 (SGLT2) is an emerging target for the treatment of type 2 diabetes mellitus (DM2). Here, the synthesis and preliminary biological evaluation of a series of potent, selective SGLT2 inhibitors, derived from a rigid spiro C-arylglucoside scaffold, is described.