124499-21-4Relevant articles and documents
An Fc–Small Molecule Conjugate for Targeted Inhibition of the Adenosine 2A Receptor
Hsiao, Po-Yuan,Kalin, Jay H.,Sun, Im-Hong,Amin, Mohammed N.,Lo, Ying-Chun,Chiang, Meng-Jung,Giddens, John,Sysa-Shah, Polina,Gabrielson, Kathleen,Wang, Lai-Xi,Powell, Jonathan D.,Cole, Philip A.
, p. 1951 - 1960 (2016/10/24)
The adenosine A2A receptor (A2AR) is expressed in immune cells, as well as brain and heart tissue, and has been intensively studied as a therapeutic target for multiple disease indications. Inhibitors of the A2AR have the
Diagnostic uses of 2-substituted adenosine carboxamides
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, (2008/06/13)
The present invention discloses a method for measuring myocardial function in a mammal in need of such measurement by: a) administering 2-substituted adenosine carboxamide derivatives at a dosage rate of less than 1 μg/kg/min, preferably between about 0.01 and 1 μg/kg/min; and then: b) performing a technique on the mammal to detect myocardial function. The method can be used to diagnose myocardial dysfunction by electrophysiologic analysis or by imaging the vasculature of the heart, especially under conditions that simulate stress.
2-(SUBSTITUTED AMINO) ADENOSINES AS ANTIHYPERTENSIVES
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, (2008/06/13)
Disclosed are 2-substituted adenosine derivatives of the formula STR1 in which R represents a substituted amino grouping of the formula STR2 as defined herein; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable prodrug ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for their preparation; and their use in mammals as therapeutically effective adenosine-2 (A-2) agonists.
2-(Arylalkylamino)adenosin-5'-uronamides: A New Class of Highly Selective Adenosine A2 Receptor Ligands
Hutchison, Alan J.,Williams, Michael,Jesus, Reynalda, de,Yokoyama, Rina,Oei, Howard H.,et al.
, p. 1919 - 1924 (2007/10/02)
The synthesis and receptor-binding profiles at adenosine receptor subtypes for a series of 2-(arylalkylamino)adenosin-5'-uronamides is described.Halogenated 2-phenethylamino analogues such as 3e show greater than 200-fold selectivity for the A2 receptor s
2-substituted adenosine 5'-carboxamides as antihypertensive agents
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, (2008/06/13)
The compounds of the formula I STR1 wherein R represents hydrogen or lower alkyl; R 1 represents C 3 -C 6 -cycloalkyl optionally substituted by lower alkyl, C 3 -C 6 -cycloalkyl-lower alkyl optionally substituted by lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, aryl, aryl-lower alkyl, aryl-C 3 -C 6 -cycloalkyl, 9-fluorenyl, diaryl-lower alkyl, 9-fluorenyl-lower alkyl, cycloalkenyl-lower alkyl, bicycloalkenyl-lower alkyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl or adamantyl-lower alkyl; or R 1 represents a bicyclic benzo-fused 5- or 6-membered saturated carbocyclic radical or a benzo-fused 5- or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur which is directly attached to the fused benzene ring, any said bicyclic radical being unsubstituted or substituted on the benzo portion by lower alkyl, lower alkoxy, hydroxy, halogen or trifluoromethyl, or by a substituent -W-Z in which W represents a direct bond, lower alkylene, lower alkenylene, thio-lower alkylene or oxy-lower alkylene and Z represents cyano, carboxy or carboxy derivatized in the form of a pharmaceutically acceptable ester or amide, or R 1 represents any said bicyclic radical substituted-lower alkyl; or R 1 represents aryl-hydroxy-lower alkyl; R 2 represents hydrogen, lower alkyl or aryl-lower alkyl; R 3 represents hydrogen or hydroxy; R 4 represents hydrogen, lower alkyl, aryl-lower alkyl, C 3 -C 6 -cycloalkyl or hydroxy-lower alkyl; aryl represents an optionally substituted carbocyclic aromatic radical, being preferably 1- or 2-naphthyl, phenyl, or naphthyl or phenyl substituted by one to three of lower alkyl, lower alkoxy, hydroxy, halogen or trifluoromethyl, or naphthyl or phenyl substituted by a substitutent -W-Z in which W represents a direct bond, lower alkylene, lower alkenylene, thio-lower alkylene or oxy-lower alkylene and Z represents cyano, carboxy or carboxy derivatized in the form of a pharmaceutically acceptable ester or amide; or aryl represents a heterocyclic aromatic radical, being preferably pyridyl or thienyl, each optionally substituted as described above for phenyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; their preparation; and their use as adenosine-2 receptor agonists are disclosed.