- The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus
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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.
- 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
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p. 7100 - 7105
(2013/01/15)
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- SUBSTITUTED INDAZOLE AMIDES AND THEIR USE AS GLUCOKINASE ACTIVATORS
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The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
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Page/Page column 29-30
(2010/10/03)
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