- N-[6-Amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy
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In the present article, we report on a strategy to improve the physical properties of a series of small molecule human adenosine 2A (hA2A) antagonists. One of the aromatic rings typical of this series of antagonists is replaced with a series of
- Lanier, Marion C.,Moorjani, Manisha,Luo, Zhiyong,Chen, Yongsheng,Lin, Emily,Tellew, John E.,Zhang, Xiaohu,Williams, John P.,Gross, Raymond S.,Lechner, Sandra M.,Markison, Stacy,Joswig, Tanya,Kargo, William,Piercey, Jaime,Santos, Mark,Malany, Siobhan,Zhao, Marilyn,Petroski, Robert,Crespo, María I.,Díaz, José-Luis,Saunders, John,Wen, Jenny,O'Brien, Zhihong,Jalali, Kayvon,Madan, Ajay,Slee, Deborah H.
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experimental part
p. 709 - 717
(2009/12/05)
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- SUBSTITUTED PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS
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Compounds of formula (I) including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
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Page/Page column 32
(2008/12/06)
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