IP Library Granted Patent US 7,582,617
Granted Patent B2
US 7,582,617 · App. 11/070,768 · Granted Sep 1, 2009

Myocardial perfusion imaging method

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Quick Facts
Patent No.
US 7,582,617
App. No.
11/070,768
Granted
Sep 1, 2009
Kind
B2
Abstract

The present invention provides a method for using the partial adenosine A 2A receptor agonists having the following structure in myocardiological perfusion imaging.

Claims (22)

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 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 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)oxolan-2-yl]-6-aminopurin-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 μg/kg.

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

4. The method of claim 1 wherein the selective partial A 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 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 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 μg/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 2A adenosine receptor agonist to a mammal, wherein the selective partial A 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-aminopurin-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 μg/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 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 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 μg/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 2A adenosine receptor agonist to the mammal, wherein the selective partial A 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-aminopurin-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 μg/kg.

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

Assignments (7)
MERGER Recorded Aug 11, 2011
From: APEX MERGER SUB, INC.; CV THERAPEUTICS, INC.
To: GILEAD PALO ALTO, INC.
Reel/Frame 026735/0488 →
MERGER Recorded Jun 25, 2011
From: APEX MERGER SUB, INC.; CV THERAPEUTICS, INC.
To: GILEAD PALO ALTO, INC.
Reel/Frame 026500/0039 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 10, 2011
From: GILEAD PALO ALTO, INC.
To: GILEAD SCIENCES, INC.
Reel/Frame 026424/0925 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 6, 2010
From: TPG-AXON ROYALTY TRUST
To: TPG-AXON LEX SUB-TRUST
Reel/Frame 023731/0916 →
MERGER Recorded Oct 6, 2009
From: GILEAD PALO ALTO, INC.
To: TPG-AXON ROYALTY TRUST
Reel/Frame 023330/0648 →
SECURITY AGREEMENT Recorded Apr 16, 2008
From: CV THERAPEUTICS, INC.
To: TPG-AXON ROYALTY TRUST
Reel/Frame 020808/0823 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2006
From: BELARDINELLI, LUIZ; BLACKBURN, BRENT K.; GAO, ZHENHAI
To: CV THERAPEUTICS, INC.
Reel/Frame 018151/0484 →