515160-72-2Relevant articles and documents
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Paragraph 0131; 0134-0135, (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.
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists
Silverman, Lisa S.,Caldwell, John P.,Greenlee, William J.,Kiselgof, Eugenia,Matasi, Julius J.,Tulshian, Deen B.,Arik, Leyla,Foster, Carolyn,Bertorelli, Rosalia,Monopoli, Angela,Ongini, Ennio
, p. 1659 - 1662 (2007/10/03)
A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochemical properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound 27 displayed both superior in vitro and highly promising in vivo profiles.
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1
Matasi, Julius J.,Caldwell, John P.,Zhang, Hongtao,Fawzi, Ahmad,Cohen-Williams, Mary E.,Varty, Geoffrey B.,Tulshian, Deen B.
, p. 3670 - 3674 (2007/10/03)
The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.