851371-60-3Relevant academic research and scientific papers
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.
PYRAZINE DERIVATIVES USEFUL AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 65, (2008/06/13)
The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group ; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the -NH- group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.
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 (2008/02/05)
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.
CONDENSED PYRIDINE DERIVATIVES USEFUL AS A28 ADENOSINE RECEPTOR ANTGONISTS
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Page/Page column 25-26, (2008/06/13)
The present invention relates to new antagonists of the A2B adenosine receptor represented by formula (I). Those compounds are useful for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor such as asthma, bronchoconstriction, allergic diseases, hypertension, atherosclerosis, reperfusion injury, myocardial ischemia, retinopathy, inflammation, gastrointestinal tract disorders, cell proliferation disorders, diabetes mellitus, and/or autoimmune diseases.
PYRIMIDIN-2-AMINE DERIVATES AND THEIR USE AS A2B ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 20, (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.
