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Claims for Patent: 8,183,226

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Claims for Patent: 8,183,226

Title:Myocardial perfusion imaging method
Abstract: The present disclosure provides 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 in a variety of applications including myocardial perfusion imaging and coronary vasodilation methods. ##STR00001##
Inventor(s): Belardinelli; Luiz (Menlo Park, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:12/695,096
Patent Claims: 1. A method of producing coronary vasodilation comprising administering by intravenous (iv) bolus at least 400 micrograms of 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: ##STR00022## to a human in need thereof.

2. The method of claim 1, wherein the CVT-3146 is administered in an amount that does not exceed about 1000 .mu.g.

3. The method of claim 1, wherein the CVT-3146 is administered in a single dose.

4. The method of claim 1, wherein the CVT-3146 is administered in an amount no greater than about 20 .mu.g/kg to a supine patient.

5. The method of claim 1 wherein the CVT-3146 is administered in an amount no greater than about 10 .mu.g/kg to a standing patient.

6. The method of claim 1, wherein the CVT-3146 is administered in about 20 seconds.

7. The method of claim 1, wherein the CVT-3146 is administered in about 10 seconds or less.

8. A method of myocardial perfusion imaging of a human, comprising administering at least 400 micrograms by intravenous (iv) bolus of 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: ##STR00023## and a radionuclide to the human, wherein the myocardium is examined for areas of insufficient blood flow following administration of the CVT-3146 and the radionuclide.

9. The method of claim 8, wherein the myocardium examination begins within about 1 minute from the time the CVT-3146 is administered.

10. The method of claim 8, wherein the administration of the CVT-3146 causes at least a 2.5 fold increase in coronary blood flow.

11. The method of claim 8, wherein the administration of the CVT-3146 causes at least a 2.5 fold increase in coronary blood flow that is achieved within about 1 minute from the administration of the CVT-3146.

12. The method of claim 8, wherein the radionuclide and the CVT-3146 are administered separately.

13. The method of claim 8, wherein the radionuclide and the CVT-3146 are administered simultaneously.

14. The method of claim 8, wherein the administration of the CVT-3146 causes at least a 2.5 fold increase in coronary blood flow for less than about 5 minutes.

15. The method of claim 8, wherein the administration of the CVT-3146 causes at least a 2.5 fold increase in coronary blood flow for less than about 3 minutes.

16. The method of claim 8, wherein the CVT-3146 is administered in a single dose in an amount up to about 600 .mu.g that is independent of the weight of the human being dosed.
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