Myocardial perfusion imaging methods and compositions
View Patent ↗The present disclosure provides 2-adenosine N-pyrazole compounds of structural formula shown below that are potent and selective agonists for A 2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds in a variety of applications including myocardial perfusion imaging methods.
1. A pharmaceutical composition comprising
a) CVT-3146, 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:
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 μg to 1000 μg.
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-aminopurin-2-yl)pyrazol-4-yl)-N-methylcarboxamide, which has the formula:
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-aminopurin-2-yl)pyrazol-4-yl)-N-methylcarboxamide, which has the formula:
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.