851371-58-9Relevant articles and documents
Discovery and characterization of 4′-(2-furyl)-N-pyridin-3-yl-4, 5′-bipyrimidin-2′-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist
Vidal, Bernat,Nueda, Arsenio,Esteve, Cristina,Domenech, Teresa,Benito, Sonia,Reinoso, Raquel F.,Pont, Mercè,Calbet, Marta,López, Rosa,Cadavid, Marìa Isabel,Loza, María Isabel,Cárdenas, álvaro,Godessart, Núria,Beleta, Jorge,Warrellow, Graham,Ryder, Hamish
, p. 2732 - 2736 (2007)
A novel series of N-heteroaryl 4′-(2-furyl)-4,5′-bipyrimidin- 2′-amines has been identified as potent and selective A2B adenosine receptor antagonists. In particular, compound 5 showed high affinity for the A2B receptor (Ki = 17 nM), good selectivity (IC50: A1 > 1000 nM, A2A > 2500 nM, A3 > 1000 nM), displayed a favorable pharmacokinetic profile in preclinical species, and showed efficacy in functional in vitro models.
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists
Eastwood, Paul,Gonzalez, Jacob,Paredes, Sergio,Nueda, Arsenio,Domenech, Teresa,Alberti, Joan,Vidal, Bernat
scheme or table, p. 1697 - 1700 (2010/08/06)
The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A2B adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.
PYRIMIDIN-2-AMINE DERIVATES AND THEIR USE AS A2B ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 19, (2008/06/13)
This invention is directed to new potent and selective antagonists of the A2B adenosine receptor having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.