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Details for Patent: 6,921,825

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Details for Patent: 6,921,825

Title: Adenosine A3 receptor modulators
Abstract:The compounds of the following formula: ##STR1## wherein R, R.sup.2, R.sup.3 and A have the meanings given in the specification, are endowed with selective A.sub.3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A.sub.3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A.sub.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.sub.3 receptors.
Inventor(s): Baraldi; Pier Giovanni (Ferrara, IT), Borea; Pier Andrea (Ferrara, IT)
Assignee: King Pharmaceuticuals Research & Development, Inc. (Cary, NC)
Filing Date:Apr 26, 2002
Application Number:10/134,219
Claims:1. A compound of the following formula: ##STR24## wherein: A is imidazole, pyrazole, or triazole; R.sup.2 is hydrogen, alkyl, substituted alkyl, alkenyl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl or aryl; R.sup.3 is furan; and R.sup.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.sup.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: ##STR25## wherein: A is imidazole, pyrazole, or triazole; R.sup.2 is hydrogen, alkyl, substituted alkyl, alkenyl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl or aryl; R.sup.3 is furan; and R.sup.6 is heteroaryl or substituted heteroaryl; and pharmaceutically acceptable salts thereof.

6. The compound of claim 5 wherein R.sup.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.
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