Patent ID: 6583151
Filing Date: 2003-06-24
Classification: A61K,A61P,C07D

Abstract:
A method for treating nicotine dependence, alcohol dependence, stimulant dependence, central nervous system sedative dependence, or hallucinogen dependence, which method comprises administering to a patient an opioid k receptor agonist represented by the following formula (I) or a pharmacologically acceptable acid-addition salt thereof: wherein is a double bond, or a single bond; R1 is an alkyl group having from 1 to 5 carbon atoms, a cycloalkylalkyl group having from 4 to 7 carbon atoms, a cycloalkenylalkyl group having from 5 to 7 carbon atoms, an aryl group having from 6 to 12 carbon atoms, an aralkyl group having from 7 to 13 carbon atoms, an alkenyl group having from 4 to 7 carbon atoms, an allyl group, a furan-2-ylalkyl group having from 1 to 5 carbon atoms, or a thiophen-2-ylalkyl group having from 1 to 5 carbon atoms; R2 is a hydrogen atom, a hydroxy group, a nitro group, an alkanoyloxy group having from 1 to 5 carbon atoms, an alkoxy group having from 1 to 5 carbon atoms, an alkyl group having from 1 to 5 carbon atoms, or âˆ’NR9R10; R9 is a hydrogen atom or an alkyl group having from 1 to 5 carbon atoms; R10 is a hydrogen atom, an alkyl group having from 1 to 5 carbon atoms, or â€”C(&boxH;O)R11 is a hydrogen atom, a phenyl group, or an alkyl group having from 1 to 5 carbon atoms; R3 is a hydrogen atom, a hydroxy group, an alkanoyloxy group having from 1 to 5 carbon atoms, or an alkoxy group having from 1 to 5 carbon atoms; A is â€”XC(&boxH;Y)â€”, â€”XC(&boxH;Y)Zâ€”, â€”Xâ€”, or â€”XSO2, wherein X, Y and Z are, independently of one another, NR4, S, or O; and R4 is a hydrogen atom, a straight-chain or branched-chain alkyl group having from 1 to 5 carbon atoms, or an aryl group having from 6 to 12 carbon atoms; and R4 is optionally identical or different in the formula; B is a valence bond, a straight-chain or branched-chain alkylene group having from 1 to 14 carbon atoms, wherein the alkylene group is optionally substituted by one or more substituents selected from the group consisting of an alkoxy group having from 1 to 5 carbon atoms, an alkanoyloxy group having from 1 to 5 carbon atoms, a hydroxy group, a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, an amino group, a nitro group, a cyano group, a trifluoromethyl group, a trifluoromethoxy group, and a phenoxy group, and wherein one to three methylene groups of the alkylene group is optionally replaced with carbonyl groups, a straight-chain or branched-chain acyclic unsaturated hydrocarbon containing from one to three double bonds and/or triple bonds and having from 2 to 14 carbon atoms, wherein the acyclic unsaturated hydrocarbon is optionally substituted by one or more substituents selected from the group consisting of an alkoxy group having from 1 to 5 carbon atoms, a hydroxy group, a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, an amino group, a nitro group, a cyano group, a trifluoromethyl group, a trifluoromethoxy group, and a phenoxy group, and wherein one to three methylene groups of the acyclic unsaturated hydrocarbon is optionally replaced with carbonyl groups, or a straight-chain or branched-chain saturated or unsaturated hydrocarbon containing from one to five thioether, ether, and/or amino bonds and having from 1 to 14 carbon atoms, wherein no hetero atoms are bonded directly to A, and one to three methylene groups of the hydrocarbon is optionally replaced with carbonyl groups; and R5 is a hydrogen atom or an organic group having a basic skeleton selected from the group consisting of the following formulas: wherein the organic group optionally has at least one substituent selected form the group consisting of an alkyl group having from 1 to 5 carbon atoms, an alkoxy group having from 1 to 5 carbon atoms, an alkanoyloxy group having from 1 to 5 carbon atoms, a hydroxy group, a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, an amino group, a nitro group, a cyano group, an isothiocyanate group, a trifluoromethyl group, a trifluoromethoxy group, and a methylenedioxy group; R6 is a hydrogen atom; R7 is a hydrogen atom, a hydroxy group, an alkoxy group having from 1 to 5 carbon atoms, or R6 and R7 are â€”Oâ€”, â€”CH2â€”, â€”Sâ€” together; R8 is a hydrogen atom, an alkyl group having from 1 to 5 carbon atoms or an alkanoyl group having from 1 to 5 carbon atoms.