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Last Updated: April 19, 2024

Claims for Patent: 7,582,617


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Summary for Patent: 7,582,617
Title:Myocardial perfusion imaging method
Abstract:The present invention provides a method for using the partial adenosine A.sub.2A receptor agonists having the following structure ##STR00001## in myocardiological perfusion imaging.
Inventor(s): Belardinelli; Luiz (Menlo Park, CA), Blackburn; Brent K. (Los Altos, CA), Gao; Zhenhai (San Jose, CA)
Assignee: CV Therapeutics, Inc. (Palo Alto, CA)
Application Number:11/070,768
Patent Claims: 1. A method of myocardial perfusion imaging of a mammal in need thereof, comprising administering a radionuclide and a dose of a compound that is a selective partial A.sub.2A adenosine receptor agonist with a short duration of action to a mammal in need thereof, and determining areas of insufficient blood flow, wherein the selective partial A.sub.2A adenosine receptor agonist is CVT-3033, also known as (4S,2R,3R,5R)-2-[6-amino-2-(1-pentylpyrazol-4-yl)purin-9-yl]-5-(hydroxyme- thyl) oxolane-3,4-diol, or CVT-3146, also known as (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, and wherein the dose is from 0.0002 to 0.009 mg/kg.

2. The method of claim 1, wherein the dose of CVT-3033 or CVT-3146 is from 0.10 to 5.0 .mu.g/kg.

3. The method of claim 1 wherein the route of administration of the compound that is a selective partial A.sub.2A adenosine receptor agonist is bolus.

4. The method of claim 1 wherein the selective partial A.sub.2A adenosine receptor agonist compound is formulated into a liquid.

5. The method of claim 1 wherein the compound that is a selective partial A.sub.2A adenosine receptor agonist is administered in a single dose.

6. The method of claim 1 wherein the compound that is a selective partial A.sub.2A adenosine receptor agonist is CVT-3033.

7. The method of claim 6 wherein the route of administration of CVT-3033 is bolus.

8. The method of claim 6 wherein the CVT-3033 is formulated into a liquid.

9. The method of claim 6 wherein the CVT-3033 is administered in a single dose.

10. The method of claim 6, wherein the dose of CVT-3033 is from 0.0002 to 0.009 mg/kg.

11. The method of claim 6, wherein the dose of CVT-3033 is from 0.10 to 5.0 .mu.g/kg.

12. A method for iincreasing coronary blood flow in a mammal in need there of comprising administering a pharmaceutically effective amount of a partial A.sub.2A adenosine receptor agonist to a mammal, wherein the selective partial A.sub.2A adenosine receptor agonist is CVT-3033, also known as (4S,2R,3R,5R)-2-[6-amino-2-(1-pentylpyrazol-4-yl)purin-9-yl]-5-(- hydroxymethyl) oxolane-3,4-diol, or CVT-3146, also known as (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxola-2-yl]-6-aminopu- rin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, and wherein the pharmaceutically effective amount is from 0.0002 to 0.009 mg/kg.

13. The method of claim 12, wherein the method of administration is bolus.

14. The method of claim 12, wherein the dose of CVT-3033 is from 0.10 to 5.0 .mu.g/kg.

15. A method of myocardial perfusion imaging of a mannnal in need thereof, comprising administering a radionuclide and a dose of a compound that is a selective partial A.sub.2A adenosine receptor agonist with a short duration of action to a mammal in need thereof, and determining areas of insufficient blood flow, wherein the selective partial A.sub.2A adenosine receptor agonist is CVT-3146, also known as (1-{9-[(4S,2R,3R,5R)-dihydroxy-5-(hydroxymethyl)oxola-2-yl]-6-aminopurin-- 2-yl}pyrazol-4-yl) and wherein the dose is from 0.0002 to 0.009 mg/kg.

16. The method of claim 15, wherein the route of administration of CVT-3146 is bolus.

17. The method of claim 15, wherein the CVT-3146 is formulated into a liquid.

18. The method of claim 15, wherein the CVT-3146 is administered in a single dose.

19. The method of claim 15, wherein the dose of CVT-3146 is from 0.10 to 5.0 .mu.g/kg.

20. A method for increasing coronary blood flow in a mammal in need there of comprising administering a pharmaceutically effective amount of a partial A.sub.2A adenosine receptor agonist to the mammal, wherein the selective partial A.sub.2A adenosine receptor agonist is CVT-3033, also known as (4S,2R,3R,5R)-2-[6-amino-2-(1-pentylpyrazol-4-yl)purin-9-yl]-5-(- hydroxymethyl) oxolane-3,4-diol, or CVT-3146, also known as (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxola-2-yl]-6-aminopu- rin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, wherein the pharmaceutically effective amount is from 0.0002 to 0.009 mg/kg.

21. The method of claim 20 wherein the dose of CVT-3146 is from 0.10 to 5.0 .mu.g/kg.

22. The method of claim 20, wherein the method of administration is bolus.

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