946525-40-2Relevant academic research and scientific papers
NOVEL SGLT INHIBITORS
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, (2013/02/28)
The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula (I) and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
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
scheme or table, 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.
