856173-22-3Relevant academic research and scientific papers
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy
Slee, Deborah H.,Zhang, Xiaohu,Moorjani, Manisha,Lin, Emily,Lanier, Marion C.,Chen, Yongsheng,Rueter, Jaimie K.,Lechner, Sandra M.,Markison, Stacy,Malany, Siobhan,Joswig, Tanya,Santos, Mark,Gross, Raymond S.,Williams, John P.,Castro-Palomino, Julio C.,Crespo, María I.,Prat, Maria,Gual, Silvia,Díaz, José-Luis,Wen, Jenny,O'Brien, Zhihong,Saunders, John
, p. 400 - 406 (2008/12/20)
Potent adenosine hA2A receptor antagonists are often accompanied by poor aqueous solubility, which presents issues for drug development. Herein we describe the early exploration of the structure-activity relationships of a lead pyrimidin-4-yl a
SUBSTITUTED PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 45-46, (2008/12/06)
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.
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents
Slee, Deborah H.,Chen, Yongsheng,Zhang, Xiaohu,Moorjani, Manisha,Lanier, Marion C.,Lin, Emily,Rueter, Jaimie K.,Williams, John P.,Lechner, Sandra M.,Markison, Stacy,Malany, Siobhan,Santos, Mark,Gross, Raymond S.,Jalali, Kayvon,Sai, Yang,Zuo, Zhiyang,Yang, Chun,Castro-Palomino, Julio C.,Crespo, María I.,Prat, Maria,Gual, Silvia,Díaz, José-Luis,Saunders, John
, p. 1719 - 1729 (2008/09/21)
Previously we have described a novel series of potent and selective A 2A receptor antagonists (e.g., 1) with excellent aqueous solubility.1 While these compounds are efficacious A2A antagonists in vivo, the presence of an
2, 6 BISHETEROARYL-4-AMINOPYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 47, (2010/02/12)
4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
