300355-27-5Relevant articles and documents
Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675)
Haynes, Nancy-Ellen,Corbett, Wendy L.,Bizzarro, Fred T.,Guertin, Kevin R.,Hilliard, Darryl W.,Holland, George W.,Kester, Robert F.,Mahaney, Paige E.,Qi, Lida,Spence, Cheryl L.,Tengi, John,Dvorozniak, Mark T.,Railkar, Aruna,Matschinsky, Franz M.,Grippo, Joseph F.,Grimsby, Joseph,Sarabu, Ramakanth
supporting information; experimental part, p. 3618 - 3625 (2010/07/05)
Glucokinase (GK) is a glucose sensor that couples glucose metabolism to insulin release. The important role of GK in maintaining glucose homeostasis is illustrated in patients with GK mutations. In this publication, identification of the hit molecule 1 and its SAR development, which led to the discovery of potent allosteric GK activators 9a and 21a, is described. Compound 21a (RO0281675) was used to validate the clinical relevance of targeting GK to treat type 2 diabetes.
SULFONAMIDE DERIVATIVES AS GLYCOKINASE ACTIVATORS USEFUL IN THE TREATMENT OF TYPE 2 DIABETES
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Page/Page column 42, (2008/06/13)
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SULFONAMIDE-THIAZOLPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS USEFUL THE TREATMENT OF TYPE 2 DIABETES
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Page/Page column 66, (2010/02/14)
The present invention provides compounds of the formula (I), which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, Type 2 diabetes and obesity.
