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Details for Patent: 8,569,260

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Details for Patent: 8,569,260

Title:N-pyrazole A.sub.2A receptor agonists
Abstract: The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A.sub.2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart. ##STR00001##
Inventor(s): Zablocki; Jeff A. (Los Altos, CA), Elzein; Elfatih O. (Fremont, CA), Palle; Venkata P. (Pune, IN), Belardinelli; Luiz (Palo Alto, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Filing Date:Aug 29, 2012
Application Number:13/598,451
Claims:1. A compound of formula; ##STR00021## named (4S,2R,3R,5R)-2-{6-amino-2-[4-(4-methylphenyl)pyrazolyl]purin-9-yl}-5-(hy- droxymethyl)oxolane-3,4-diol.

2. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutically acceptable excipients.

3. The pharmaceutical composition of claim 2, wherein the pharmaceutical composition is in the form of a solution.

4. A method for stimulating coronary vasodilation in a human in need thereof by administering to the human the compound of claim 1.

5. The method of claim 4, wherein the method comprises administering the compound intravenously by bolus.

6. The method of claim 4, wherein the method comprises administering an amount of the compound of claim 1 ranging from 0.01 to 100 mg/kg weight of the human.

7. A method of treating coronary artery disease mediated by A.sub.2A receptor in a human in need thereof, wherein the method comprises administering a therapeutically effective amount of the compound of claim 1 to the human.

8. A method of coronary imaging of a human in need thereof, comprising administering a radioactive imaging agent and the compound of claim 1 to the human.

9. A method of dilating the coronary vessels of a human in need thereof, as an adjunct to angioplasty, wherein the method comprises administering a therapeutically effective amount of the compound of claim 1 to the human.

10. A method for inhibition of platelet aggregation in a human in need thereof comprising administering a therapeutically effective amount of the compound of claim 1 to the human.
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