IP Library Granted Patent US 8,470,801
Granted Patent B2
US 8,470,801 · App. 13/361,775 · Granted Jun 25, 2013

Myocardial perfusion imaging methods and compositions

Inventors: Luiz Belardinelli (Menlo Park, CA); Mitchell Rosner (Mountain View, CA)
Assignee: Gilead Sciences, Inc.
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Quick Facts
Patent No.
US 8,470,801
App. No.
13/361,775
Granted
Jun 25, 2013
Kind
B2
Abstract

A myocardial imaging method that is accomplished by administering one or more adenosine A 2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A 2a receptor agonist, at least one liquid carrier, and at least one co-solvent.

Claims (19)

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-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula:

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-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula:

to a human subject in need thereof, wherein the compound is administered in an amount of 10 μg to about 1000 μg, 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 μg.

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.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2012
From: BELARDINELLI, LUIZ; ROSNER, MITCHELL
To: CV THERAPEUTICS, INC.
Reel/Frame 029435/0054 →
MERGER Recorded Dec 10, 2012
From: APEX MERGER SUB, INC.; CV THERAPEUTICS, INC.
To: GILEAD PALO ALTO, INC.
Reel/Frame 029435/0205 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2012
From: GILEAD PALO ALTO, INC.
To: GILEAD SCIENCES, INC.
Reel/Frame 029435/0259 →
Continuity (8)
Continuation 12749328 · Mar 29, 2010
Continuation 10766403 · Jan 27, 2004
Continuation In Part 10629368 · Jul 29, 2003
Provisional Application 60459803 · Apr 2, 2003
Provisional Application 60426902 · Nov 15, 2002
Provisional Application 60399177 · Jul 29, 2002
Provisional Application 60399176 · Jul 29, 2002
Related Publication 20120195827A1 · Aug 2, 2012