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Claims for Patent: 7,683,037

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Claims for Patent: 7,683,037

Title:Myocardial perfusion imaging method
Abstract:The present invention relates to methods for myocardial imaging by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof A.sub.2A adenosine receptor agonist to a human undergoing myocardial imaging. The invention also relates to methods of producing coronary vasodilation without significant peripheral vasodilation by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof adenosine A.sub.2A adenosine receptor agonist to a human.
Inventor(s): Belardinelli; Luiz (Menlo Park, CA)
Assignee: Gilead Palo Alto, Inc. (Foster City, CA)
Application Number:10/629,368
Patent Claims: 1. A method of producing coronary vasodilation without significant peripheral vasodilation comprising administering by intravenous (iv) bolus at least 10 .mu.g of the A.sub.2A receptor agonist CVT-3146, named (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula: ##STR00020## to a human in need thereof.

2. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount that does not exceed about 1000 .mu.g.

3. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 10 to about 600 .mu.g.

4. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in a single dose.

5. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 0.05 to about 60 .mu.g/kg.

6. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 0.1 to about 30 .mu.g/kg.

7. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount no greater than about 20 .mu.g/kg to a supine patient.

8. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount no greater than about 10 .mu.g/kg to a standing patient.

9. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 10 to about 600 .mu.g/kg wherein the wherein the A.sub.2A receptor agonist is administered in about 20 seconds.

10. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 10 to about 600 .mu.g/kg wherein the A.sub.2A receptor agonist is administered in less than about 10 seconds.

11. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount greater than about 100 .mu.g.

12. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount no greater than 600 .mu.g.

13. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount no greater than 500 .mu.g.

14. The method of claim 1 wherein the A.sub.2A receptor agonist is administered in an amount ranging from about 100 .mu.g to about 500 .mu.g.

15. A method of myocardial perfusion imaging of a human, comprising administering a radionuclide and the A.sub.2A receptor agonist CVT-3146, named (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-- aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula: ##STR00021## to the human, wherein the administration of the A.sub.2A receptor agonist causes at least a 2.5 fold increase in coronary blood flow that is achieved within about 1 minute from the administration of the A.sub.2A receptor agonist, and wherein the myocardium is examined for areas of insufficient blood flow following administration of the radionuclide and the A.sub.2A receptor agonist.

16. The method of claim 15 wherein the myocardium examination begins within about 1 minute from the time the A.sub.2A receptor agonist is administered.

17. The method of claim 15 wherein the radionuclide and the A.sub.2A receptor agonist are administered separately.

18. The method of claim 15 wherein the radionuclide and the A.sub.2A receptor agonist are administered simultaneously.

19. The method of claim 15 wherein the administration of the A.sub.2A receptor agonist causes at least a 2.5 fold increase in coronary blood flow for less than about 5 minutes.

20. The method of claim 15 wherein the administration of the A.sub.2A receptor agonist causes at least a 2.5 fold increase in coronary blood flow for less than about 3 minutes.

21. The method of claim 15 wherein the A.sub.2A receptor agonist is CVT-3146 which is administered in an amount ranging from about 10 to about 600 .mu.g in a single intravenous (iv) bolus.

22. The method of claim 21 wherein CVT-3146 is administered in an amount ranging from about 100 to about 500 .mu.g in a single intravenous (iv) bolus.

23. The method of claim 15 wherein the a A.sub.2A receptor agonist is CVT-3146 which is administered in a single dose in an amount ranging from 10 to about 600 .mu.g that is independent of the weight of the human being dosed.

24. The method of claim 23 wherein the dose is administered in about 30 seconds or less.

25. The method of claim 23 wherein the dose is administered in about 20 seconds or less.

26. The method of claim 15 wherein the A.sub.2A receptor agonist is administered in a single dose.
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