210530-71-5Relevant articles and documents
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Paragraph 0347-0349, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
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.
HETEROAROMATIC GLUCOKINASE ACTIVATORS
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, (2008/06/13)
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