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Claims for Patent: 8,133,879

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Claims for Patent: 8,133,879

Title:Myocardial perfusion imaging methods and compositions
Abstract: The present disclosure provides 2-adenosine N-pyrazole compounds of structural formula shown below that are potent and selective agonists for A.sub.2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds in a variety of applications including myocardial perfusion imaging methods. ##STR00001##
Inventor(s): Belardinelli; Luiz (Palo Alto, CA), Rosner; Mitchell (Mountain View, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:12/749,328
Patent Claims: 1. A pharmaceutical composition comprising a) CVT-3146, 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## b) at least one liquid carrier selected from the group consisting of water, distilled water, de-ionized water, saline, a buffer, and combinations thereof, c) at least one sodium phosphate buffer; d) EDTA; and e) propylene glycol in an amount from about 5% to about 25% (w:v), and wherein the pH of said pharmaceutical composition is from about 6 to about 8.

2. The pharmaceutical composition of claim 1, wherein the propylene glycol is present in an amount from about 8% to about 20% (w:v).

3. The pharmaceutical composition of claim 2, wherein the propylene glycol is present in an amount of 15% (w:v).

4. The pharmaceutical composition of claim 1, wherein the CVT-3146 is present in an amount from 10 .mu.g to 1000 .mu.g.

5. The pharmaceutical composition of claim 1, wherein the at least one liquid carrier is water.

6. The pharmaceutical composition of claim 1, wherein the pH of said pharmaceutical composition is 7.

7. The pharmaceutical composition of claim 1, wherein the at least one sodium phosphate buffer is of a concentration of 100 mM.

8. The pharmaceutical composition of claim 1, wherein the said pharmaceutical composition comprises 400 micrograms of CVT-3146.

9. The pharmaceutical composition of claim 1 comprising 15% (w:v) propylene glycol and 100 mM phosphate buffer at pH 7 with 0.1% EDTA.

10. A pharmaceutical composition comprising: a) CVT-3146, 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: ##STR00022## b) water; c) at least one sodium phosphate buffer; d) 0.1% EDTA; e) propylene glycol in an amount of 15% (w:v), and wherein the pH of said pharmaceutical composition is about 7.

11. The pharmaceutical composition of claim 10, wherein the at least one sodium phosphate buffer is of a concentration of 100 mM.

12. The pharmaceutical composition of claim 10, wherein the said pharmaceutical composition comprises 100 micrograms/mL CVT-3146.

13. A pharmaceutical composition for intravenous administration comprising a) CVT-3146, 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: ##STR00023## b) at least one liquid carrier selected from the group consisting of water, distilled water, de-ionized water, saline, a buffer, and combinations thereof, c) at least one sodium phosphate buffer; d) EDTA; and e) propylene glycol in an amount from about 5% to about 25% (w:v), wherein the pH of said pharmaceutical composition is from about 6 to about 8, and further wherein the composition may be administered intravenously as a single bolus injection.
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