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US 6,440,948 B1Granted
Thiophene A2A receptor agonists
AssigneeCV Therapeutics, Inc.
InventorsJeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Abstract
2-(3-,4-(substituted)-5-alkylthienyl)adenosines and the 5′-uronic acid amide analogues thereof having the following formula: are disclosed herein. Additionally disclosed are medicinal methods of treatment wherein the adenosine A2A agonist activity of the noted compounds stimulates mammalian coronary vasodilation for therapeutic purposes and for purposes of imaging the heart.
Claims16
A compound having the following formula:
- wherein R1 is —CH2OH or —CONHEt;
- X is S;
- R2 is selected from the group consisting of hydrogen, C1-8 alkyl, aryl, and halo wherein the alkyl and aryl substituents are optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, OR20, aryl, CF3, and CN, and wherein each optional aryl substituent is optionally substituted with a substituent selected from the group consisting of halo, alkyl, CF3 and CN;
- R3 and R4 are each individually selected from the group consisting of hydrogen, methyl, and halo;
- and
- R20 is selected from hydrogen or C1-6 alkyl wherein, when R1 is —CH2OH, then R2 cannot be hydrogen.
3 more elements
A compound selected from the group consisting of 2-(2-(5-methylthienyl))adenosine;
- 2-(2-(5-iodothienyl))adenosine;
- and 2-(2-(5-phenylthienyl))adenosine.
Dependencies are inferred from the claim text.