C-pyrazole A2A receptor agonists
View Patent ↗2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
1. A compound having the formula:
wherein R 1 is —CH 2 OH;
R 2 is independently selected from the group consisting of hydrogen, C 1-10 alkyl and aryl, wherein the alkyl and aryl substituents are optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, OR 20 , aryl, CF 3 , and CN, and wherein each optional aryl substituent is optionally substituted with halo, alkyl, CF 3 and CN;
R 3 and R 4 are each individually selected from the group consisting of hydrogen, methyl, and halo; and
R 20 is selected from H, and C 1-6 alkyl.
2. A method for stimulating coronary vasodilatation in a mammal by administering to the mammal a therapeutically effective amount of a compound of claim 1 that is sufficient to stress the heart and induce a coronary steal situation for the purposes of imaging the heart.
3. The method of claim 2 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal.
4. The method of claim 2 wherein the mammal is a human.
5. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutical excipients.
6. The pharmaceutical composition of claim 5 wherein the pharmaceutical composition is in the form of a solution.
7. The pharmaceutical composition of claim 6 wherein the solution is formulated for injection.
8. The pharmaceutical composition of claim 5 wherein the composition is useful as an anti-inflammatory, in adjunctive therapy with angioplasty, as a platelet aggregation inhibitor, and as an inhibitor of platelet and neutrophil activation.