852520-52-6Relevant articles and documents
Small-molecule allosteric activation of human glucokinase in the absence of glucose
Bowler, Joseph M.,Hervert, Katherine L.,Kearley, Mark L.,Miller, Brian G.
, p. 580 - 584 (2013/07/26)
Synthetic allosteric activators of human glucokinase are receiving considerable attention as potential diabetes therapeutic agents. Although their mechanism of action is not fully understood, structural studies suggest that activator association requires
NOVEL ACTIVATORS OF GLUCOKINASE
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Page/Page column 121-123, (2009/04/25)
The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistence and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
Discovery, synthesis and biological evaluation of novel glucokinase activators
McKerrecher, Darren,Allen, Joanne V.,Bowker, Suzanne S.,Boyd, Scott,Caulkett, Peter W. R.,Currie, Gordon S.,Davies, Christopher D.,Fenwick, Mark L.,Gaskin, Harold,Grange, Emma,Hargreaves, Rod B.,Hayter, Barry R.,James, Roger,Johnson, Keith M.,Johnstone, Craig,Jones, Clifford D.,Lackie, Sarah,Rayner, John W.,Walker, Rolf P.
, p. 2103 - 2106 (2007/10/03)
The identification, synthesis and SAR of a novel series of glucokinase activators is described. The interplay between lipophilicity, potency and physical properties is discussed, and compound 22 highlighted as having a suitable balance. In vivo pharmacoki