300355-27-5Relevant academic research and scientific papers
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.
Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes
Bebernitz, Gregory R.,Beaulieu, Valerie,Dale, Bethany A.,Deacon, Richard,Duttaroy, Alokesh,Gao, Jiaping,Grondine, Melissa S.,Gupta, Ramesh C.,Kakmak, Mesut,Kavana, Michael,Kirman, Louise C.,Liang, Jinsheng,Maniara, Wieslawa M.,Munshi, Siralee,Nadkarni, Sunil S.,Schuster, Herbert F.,Stams, Travis,St. Denny, Irene,Taslimi, Paul M.,Vash, Brian,Caplan, Shari L.
experimental part, p. 6142 - 6152 (2010/02/28)
Type 2 diabetes is a polygenic disease which afflicts nearly 200 million people worldwide and is expected to increase to near epidemic levels over the next 10-15 years. Glucokinase (GK) activators are currently under investigation by a number of pharmaceu
ORGANIC COMPOUNDS
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Page/Page column 48-49, (2008/06/13)
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.
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.
Para-aryl or heterocyclic substituted phenyl glucokinase activators
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, (2008/06/13)
Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
Heteroaromatic glucokinase activators
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, (2008/06/13)
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
Para-amine substituted phenylamide glucokinase activators
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, (2008/06/13)
Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
