초록

3-O-Acetylmorphine-6-sulfate analogues are potent, centrally-acting morphine derivatives. The compounds are useful for the treatment of pain.

대표청구항 ▼

1. A method of treating pain comprising administering to a person in need thereof a therapeutically effective amount of a compound selected from the group consisting of the following formulas I and II: [EQU9]wherein X is selected from the group consisting of -OR2, [EQU10] and [EQU11]wherein R1 may b

1. A method of treating pain comprising administering to a person in need thereof a therapeutically effective amount of a compound selected from the group consisting of the following formulas I and II: [EQU9]wherein X is selected from the group consisting of -OR2, [EQU10] and [EQU11]wherein R1 may be a straight or branched chain alkyl group having 1-5 carbon atoms or alkenyl group having 2-5 carbon atoms, wherein R2 is an alkyl having 1-3 carbon atoms, wherein R3 is H, n-alkyl, or branched alkyl with 2-10 carbon atoms, cycloalkyl with 3-10 carbon atoms, aralkyl with 5-10 carbon atoms, phenyl, n-alkenyl or branched alkenyl with 2-10 carbon atoms, and n-alkynyl or branched alkynyl with 2-10 carbon atoms, and wherein R4 is H or n-alkyl or branched alkyl with 1-10 carbon atoms, cycloalkyl with 3-10 carbon atoms, aralkyl with 5-10 carbon atoms, n-alkenyl or branched alkenyl with 2-10 carbon atoms, and n-alkynyl or branched alkynyl with 2-10 carbon atoms, with the proviso that when R3 is a methyl group, R1 is neither a methyl group nor -CH2-CH.dbd.C(CH3)2 group; and [EQU12]wherein X is selected from the group consisting of -OR2, [EQU13] and [EQU14]wherein R1 may be straight or branched chain alkyl group having 1-5 carbon atoms or alkenyl group having 2-5 carbon atoms, wherein R2 is an alkyl having 1-3 carbon atoms, wherein R3' is H, n-alkyl, or branched alkyl with 2-10 carbon atoms, cycloalkyl with 3-10 carbon atoms, aralkyl with 5-10 carbon atoms, n-alkenyl or branched alkenyl with 2-10 carbon atoms, and n-alkynyl or branched alkynyl with 2-10 carbon atoms, and wherein R4 is H or n-alkyl or branched alkyl with 1-10 carbon atoms, cycloalkyl with 3-10 carbon atoms, aralkyl with 5-10 carbon atoms, n-alkenyl or branched alkenyl with 2-10 carbon atoms, and n-alkynyl or branched alkynyl with 2-10 carbon atoms, with the proviso that when R3 is a methyl group, R1 is not a methyl group.