Details for Patent: 7,183,264

Title:	N-pyrazole A2A receptor agonists
Abstract:	2-adenosine N-pyrazole compounds having the following formula: ##STR00001## and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.
Inventor(s):	Zablocki; Jeff (Mountain View, CA), Elzein; Elfatih O. (Fremont, CA), Palle; Venkata P. (Gurgaon, IN), Belardinelli; Luiz (Palo Alto, CA)
Assignee:	CV Therapeutics, Inc. (Palo Alto, CA)
Filing Date:	Aug 29, 2003
Application Number:	10/652,378
Claims:	1. A method for stimulating coronary vasodilatation in a mammal by administering to the mammal a therapeutically effective amount of a compound of Formula I ##STR00021## namely (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. 2. The method of claim 1 wherein the mammal is a human. 3. A pharmaceutical composition comprising the compound of Formula I ##STR00022## namely (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, and one or more pharmaceutical excipients. 4. The pharmaceutical composition of claim 3 wherein the pharmaceutical composition is in the form of a solution. 5. A method of producing coronary vasodilation without peripheral vasodilation comprising administering a compound of Formula I ##STR00023## namely (1-{9-[(2R,3R,4S ,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazo- l-4-yl)-N-methylcarboxamide, to a human. 6. The method of claim 5 wherein the compound of Formula I is administered by iv bolus. 7. The method of claim 6 wherein the compound of Formula I is administered in from about 10 to about 30 seconds. 8. A method of myocardial perfusion imaging of a human, comprising administering a radionuclide and a compound of Formula I. ##STR00024## namely (1-{9-[(2R,3R,4S ,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazo- l-4-yl)-N-methylcarboxamide, to the human wherein the myocardium is examined for areas of insufficient blood flow following administration of the radionuclide and the compound of Formula I. 9. The pharmaceutical composition of claim 3 wherein the pharmaceutical composition is formulated for injection. 10. The method of claim 1, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation. 11. The method of claim 1, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal. 12. The method of claim 1 wherein the compound of Formula I is administered by iv bolus. 13. The method of claim 12 wherein the compound of Formula I is administered in from about 10 to about 30 seconds. 14. The method of claim 5, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation. 15. The method of claim 5, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal. 16. The method of claim 5 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal. 17. The method of claim 8, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation. 18. The method of claim 8, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal. 19. The method of claim 8 wherein the compound of Formula I is administered by iv bolus. 20. The method of claim 19 wherein the compound of Formula I is administered in from about 10 to about 30 seconds. 21. The method of claim 8 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal. 22. The method of claim 1 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal.