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 2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart.
1. A compound of formula;
named (4S,2R,3R,5R)-2-{6-amino-2-[4-(4-methylphenyl)pyrazolyl]purin-9-yl}-5-(hydroxymethyl)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 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.