Patent ID: 6559159
Filing Date: 2003-05-06
Classification: A61P,C07D

Abstract:
A method of inducing kappa opioid receptor antagonism in a subject in need thereof, comprising:administering to said subject a composition comprising a kappa opioid receptor antagonist and a physiologically acceptable carrier, wherein the kappa opioid receptor antagonist is a compound of formula (I): wherein R1 is C2-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, C1-8 alkylaryl or one of the following groups: R2 is a member selected from the group consisting of formulae (a)-(pp): X is NR, O or S; Y is OH, OR9, C1-8 alkyl, F, Cl, or CF3; R is hydrogen, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, C1-8 alkylaryl, CO2R9 W is a member selected from the group consisting of: H, OH, OCOR9; amino, â€”NR3SO2R9 and â€”NR3CO2R9; Z is NR3 or O; n is 1, 2 or 3; m is 1, 2, 3 or 4; j is 2, 3 or 4; k is 1 or 2; R3 is hydrogen, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, or C1-8 alkylaryl; R4 is hydrogen, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, or C1-8 alkylaryl; R5 and R6 are each independently, hydrogen, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, or C1-8 alkylaryl; R7 and R8 are each independently, hydrogen, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, or C1-8 alkylaryl; and R9 is C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, or C1-8 alkylaryl.