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Details for Patent: 8,071,566

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Details for Patent: 8,071,566

Title:Methods of coronary imaging
Abstract: The present invention provides methods of myocardial perfusion imaging and increasing coronary blood flow of a mammal that are accomplished by administering doses of a compound that is a selective partial A.sub.2A receptor agonist with a short duration of action, in particular regadenoson, useful for, among other indications, myocardial imaging and coronary vasodilation, and determining areas of insufficient blood flow.
Inventor(s): Belardinelli; Luiz (Palo Alto, CA), Blackburn; Brent K. (Los Altos, CA), Gao; Zhenhai (San Jose, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Filing Date:May 04, 2009
Application Number:12/435,176
Claims:1. A method of myocardial perfusion imaging of a mammal in need thereof, comprising administering an imaging agent comprising a radionuclide and a dose of a compound that is 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 to a mammal in need thereof, and determining areas of insufficient blood flow, wherein the dose is from 0.3 to 103.0 .mu.g/kg, and wherein the dose causes an increase in peripheral blood flow that is less than 50% of the increase in coronary blood flow.

2. The method of claim 1, wherein the dose of CVT-3146 is from 0.3 to 10.0 .mu.g/kg.

3. The method of claim 1, wherein the step of administering the dose of CVT-3146 takes place by a bolus injection of a pharmaceutically acceptable composition thereof.

4. The method of claim 1 further comprising dissolution of CVT-3146 in a pharmaceutically acceptable liquid carrier to form a pharmaceutically acceptable liquid composition.

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

6. The method according to claim 1 wherein the dose is administered immediately prior to or concurrently with the imaging agent.

7. The method according to claim 6 wherein the CVT-3146 compound is administered at the same time as the imaging agent.

8. The method according to claim 6 wherein the CVT-3146 compound is administered before the imaging agent is administered.

9. A method for increasing coronary blood flow in a mammal in need thereof comprising administering a pharmaceutically effective amount of a compound that is 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, wherein the pharmaceutically effective amount is from 0.3 to 103.0 .mu.g/kg, and wherein the administration causes an increase in peripheral blood flow that is less than 50% of the increase in coronary blood flow.

10. The method of claim 9, wherein the pharmaceutically effective amount of CVT-3146 is from 0.3 to 10.0 .mu.g/kg.

11. The method of claim 9, wherein step of administering the pharmaceutically effective amount of the CVT-3146 compound takes place by a bolus injection of a pharmaceutically acceptable composition thereof.

12. The method of claim 9 further comprising dissolution of CVT-3146 in a pharmaceutically acceptable liquid carrier to form a pharmaceutically acceptable liquid composition.

13. The method of claim 9 wherein the administration of the CVT-3146 compound takes place in a single dose.
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