METHODS AND PHARMACEUTICAL COMPOSITIONS FOR PREVENTING AND TREATING RENAL IMPAIRMENT

摘要

The present invention relates to methods for treating and preventing renal impairment by administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent. The invention further encompasses pharmaceutical compositions comprising an A1 adenosine receptor antagonist alone or with, at least, one additional therapeutic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing renal impairment.

主权项

1. A method of preventing or treating renal impairment in a subject, the method comprising administering to the subject a therapeutically effective amount of an A1 adenosine receptor antagonist, wherein the A1 adenosine receptor antagonist comprises a compound of formula (I):wherein R1 is selected from the group consisting of C1-C8 alkyl;
R2 is of the formula:wherein n is an integer ranging from 1 to 8; R5 is H or CH3(CH2)p, wherein p is an integer ranging from 1 to 7; and R6 is H; (CH2)mH; or (CH2)mOH, wherein m is an integer ranging from 1 to 8;
R3 is:
—(CH2)qC6H-4—R7 wherein q is an integer ranging from 1 to 8; wherein R7 is selected from the group consisting of H, OH, NH2, R9COOH, wherein R9 is an alkylene or alkenylene group having 1 to 8 carbon atoms, and (CH2)tOH, wherein t is an integer ranging from 1 to 8; -and
R4 is of the formula: wherein R8 is selected from the group consisting of H, NH2, OH, (CH2)fNH2 wherein f is an integer ranging from 1 to 8, (CH2),OH, wherein s is an integer ranging from 1 to 8, and R10COOH, wherein R10 is an alkylene or alkenylene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8, and hydrates, salts, solvates, and prodrugs thereof.