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Claims for Patent: 8,470,801

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Claims for Patent: 8,470,801

Title:Myocardial perfusion imaging methods and compositions
Abstract: A myocardial imaging method that is accomplished by administering one or more adenosine A.sub.2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A.sub.2a receptor agonist, at least one liquid carrier, and at least one co-solvent.
Inventor(s): Belardinelli; Luiz (Menlo Park, CA), Rosner; Mitchell (Mountain View, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:13/361,775
Patent Claims: 1. A method for myocardial perfusion imaging comprising administering to a human subject in need thereof a compound 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## followed by a saline flush, and followed by a radionuclide, wherein the myocardium is examined for areas of insufficient blood flow following the administration of the radionuclide.

2. The method of claim 1, wherein the method comprises administering the compound by intravenous (iv) bolus.

3. The method of claim 1, wherein the method comprises administering 400 micrograms of the compound.

4. The method of claim 1, wherein the method comprises administering 500 micrograms of the compound.

5. The method of claim 1, wherein the method comprises administering the compound in a single dose.

6. A method for myocardial perfusion imaging comprising administering a single bolus intravenous injection of a pharmaceutical composition comprising a compound 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: ##STR00021## to a human subject in need thereof, wherein the compound is administered in an amount of 10 .mu.g to about 1000 .mu.g, and the amount is independent of the human subject's weight.

7. The method of claim 6, wherein the compound is administered in an amount of about 400 .mu.g.

8. The method of claim 7, wherein the pharmaceutical composition further comprises at least one liquid carrier.

9. The method of claim 8, wherein the at least one liquid carrier comprises a buffer solution.

10. The method of claim 7, wherein the pharmaceutical composition further comprises at least one liquid carrier chosen from water, distilled water, de-ionized water, saline, buffer solutions, and combinations thereof; at least one sodium phosphate buffer; EDTA; and propylene glycol in an amount of about 5% to about 25% (w:v), wherein the pH of the pharmaceutical composition is about 6 to about 8.

11. The method of claim 10, wherein the propylene glycol is present in an amount of about 15% (w:v).

12. The method of claim 6, wherein the pharmaceutical composition further comprises about 15% (w:v) propylene glycol, about 100 mM phosphate buffer, and about 0.1% EDTA, and wherein the pH of the pharmaceutical composition is about 6 to about 8.
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