Patent Number: 8,796,291

Title: A.sub.3 adenosine receptor antagonists and partial agonists

Abstract: Disclosed are A.sub.3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R.sup.1 to R.sup.5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs. ##STR00001##

Inventors: Jacobson; Kenneth A. (Silver Spring, MD), Melman; Artem (Potsdam, NY), Wang; Ben Bih-Ren (Rockville, MD)

Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services

International Classification: A61K 31/522 (20060101); C07D 473/00 (20060101)

Expiration Date: 8/05/12018