1245215-47-7Relevant articles and documents
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus
Pfefferkorn, Jeffrey A.,Tu, Meihua,Filipski, Kevin J.,Guzman-Perez, Angel,Bian, Jianwei,Aspnes, Gary E.,Sammons, Matthew F.,Song, Wei,Li, Jian-Cheng,Jones, Christopher S.,Patel, Leena,Rasmusson, Tim,Zeng, Dongxiang,Karki, Kapil,Hamilton, Michael,Hank, Richard,Atkinson, Karen,Litchfield, John,Aiello, Robert,Baker, Levenia,Barucci, Nicole,Bourassa, Patricia,Bourbounais, Francis,D'Aquila, Theresa,Derksen, David R.,MacDougall, Margit,Robertson, Alan
, p. 7100 - 7105 (2013/01/15)
Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyridin-3- yloxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide (42) as a potent activator with favorable preclinical pharmacokinetic properties and in vivo efficacy.
