Adenosine A3 receptor modulators
View Patent ↗The compounds of the following formula: wherein R, R 2 , R 3 and A have the meanings given in the specification, are endowed with selective A 3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A 3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A 3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A 3 receptors.
1. A compound of the following formula:
wherein:
A is imidazole, pyrazole, or triazole;
R 2 is hydrogen, alkyl, substituted alkyl, alkenyl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl or aryl;
R 3 is furan; and
R 4 is hydrogen, alkyl, amino, substituted alkyl, alkyl substituted amino, alkyl di-substituted amino, alkenyl, aralkyl, substitute aralkyl, heteroaryl, substituted heteroaryl, heterocycle, aryl, substituted aryl, sulfonyl or substituted sulfonyl; and
pharmaceutically acceptable salts thereof.
2. The compound of claim 1 wherein R 2 is selected from the group consisting of hydrogen, alkyl, alkenyl and aryl.
3. The compound of claim 1 wherein A is a triazolo ring.
4. The compound of claim 1 wherein A is a pyrazolo ring.
5. A compound of the following formula:
wherein:
A is imidazole, pyrazole, or triazole;
R 2 is hydrogen, alkyl, substituted alkyl, alkenyl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl or aryl;
R 3 is furan; and
R 6 is heteroaryl or substituted heteroaryl; and
pharmaceutically acceptable salts thereof.
6. The compound of claim 5 wherein R 2 is selected from the group consisting of hydrogen, alkyl, alkenyl and aryl.
7. The compound of claim 5 wherein A is a triazolo ring.
8. The compound of claim 5 wherein A is a pyrazolo ring.