862728-59-4Relevant articles and documents
Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes
Li, Yao,Shi, Zongjun,Chen, Lei,Zheng, Suxin,Li, Sheng,Xu, Bo,Liu, Zhenhong,Liu, Jianyu,Deng, Chongyang,Ye, Fei
, p. 4173 - 4184 (2017/06/05)
A new class of potent and highly selective SGLT2 inhibitors is disclosed. Compound 31 (HSK0935) demonstrated excellent hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of 843-fold. It showed robust urinary glucose excretion in Sprague-Dawley (SD) rats and affected more urinary glucose excretion in Rhesus monkeys. Finally, an efficient synthetic route has been developed featuring a ring-closing cascade reaction to incorporate a double ketal 1-methoxy-6,8-dioxabicyclo[3.2.1]octane ring system.
PREPARATION OF HYDROXY-BENZYLBENZENE DERIVATIVES
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, (2015/04/28)
Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.
PREPARATION OF HYDROXY-BENZYLBENZENE DERIVATIVES
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, (2015/08/04)
Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.