761424-46-8Relevant academic research and scientific papers
Discovery of Ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus
Imamura, Masakazu,Nakanishi, Keita,Suzuki, Takayuki,Ikegai, Kazuhiro,Shiraki, Ryota,Ogiyama, Takashi,Murakami, Takeshi,Kurosaki, Eiji,Noda, Atsushi,Kobayashi, Yoshinori,Yokota, Masayuki,Koide, Tomokazu,Kosakai, Kazuhiro,Ohkura, Yasufumi,Takeuchi, Makoto,Tomiyama, Hiroshi,Ohta, Mitsuaki
, p. 3263 - 3279 (2012/07/14)
A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly potent and selective SGLT2 inhibitor that reduced blood glucose levels in a dose-dependent manner in diabetic models KK-Ay mice and STZ rats.
C-GLYCOSIDE DERIVATIVES AND SALTS THEREOF
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Page/Page column 13-14, (2008/06/13)
The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via -X- and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
