1118567-45-5Relevant 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.
C-Aryl glucosides substituted at the 4′-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
Xu, Baihua,Feng, Yan,Cheng, Huawei,Song, Yanli,Lv, Binhua,Wu, Yuelin,Wang, Congna,Li, Shengbin,Xu, Min,Du, Jiyan,Peng, Kun,Dong, Jiajia,Zhang, Wenbin,Zhang, Ting,Zhu, Liangcheng,Ding, Haifeng,Sheng, Zelin,Welihinda, Ajith,Roberge, Jacques Y.,Seed, Brian,Chen, Yuanwei
, p. 4465 - 4470 (2011/09/12)
A series of C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4′-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy.
CRYSTALLINE FORM OF BENZYLBENZENE SGLT2 INHIBITOR
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Page/Page column 30; 32, (2012/01/04)
Crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2 are disclosed. Pharmaceutical compositions, methods for preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition are also disclosed.