Patent ID: 6156769
Filing Date: 2000-12-05
Classification: A61K,A61P

Abstract:
A method for the prevention or treatment of pruritus in a mammal in need of such prevention or treatment comprising administering to said mammal an effective anti-pruritic amount of the composition formula V or a pharmaceutically acceptable salt thereof ##STR15## wherein ----- represents a single or double bond;R.sup.1 represents an alkyl group having 1.5 carbon atoms, a cycloalkylalkyl group having 4-7 carbon atoms, a cycloalkenylalkyl group having 5-7 carbon atoms, an aryl group having 6-12 carbon atoms, an aralkyl group having 7-13 carbon atoms, an alkenyl group having 4-7 carbon atoms, an allyl group, a furan-2-ylalkyl group having 1-5 carbon atoms, or a thiophen-2-ylalkyl group having 1-5 carbon atoms;R.sup.2 represents a hydrogen atom, a hydroxy group, a nitro group, an alkanoyloxy group having 1-5 carbon atoms, an alkoxy group having 1-5 carbon atoms, an alkyl group having 1-5 carbon atoms, or --NR.sup.9 R.sup.10 wherein R.sup.9 represents a hydrogen atom or an alkyl group having 1-5 carbon atoms, and R.sup.10 represents a hydrogen atom; an alkyl group having 1-5 carbon atoms, or --C(.dbd.O)R.sup.11 wherein R.sup.11 represents a hydrogen atom, a phenyl group or an alkyl group having 1-5 carbon atoms;R.sup.3 represents a hydrogen atom, a hydroxy group, an alkanoyloxy group having 1-5 carbon atoms, or an alkoxy group having 1-5 carbon atoms;A represents --XC(.dbd.Y)--, --XC(.dbd.Y)Z--, --X--, --XSO.sub.2 --, or --OC(OR.sup.4)R.sup.4 -- where, X, Y and Z each independently represent NR.sup.4, S or O wherein R.sup.4 represents a hydrogen atom, a straight-chain or branched chain alkyl group having 1-5 carbon atoms or an aryl group having 6-12 carbon atoms, and wherein R.sup.4 may be identical or different;B represents a valence bond, a straight-chain or branched chain alkylene group having 1-14 carbon atoms which may be substituted with at least one substituent selected from the group consisting of an alkoxy group having 1-5 carbon atoms, an alkanoyloxy group having 1-5 carbon atoms, a hydroxy group, fluorine, chlorine, bromine, iodine, an amino group, a nitro group, a cyano group, a trifluoromethyl group and a phenoxy group, and wherein 1 to 3 methylene groups may be replaced with carbonyl groups, an acyclic unsaturated hydrocarbon containing from 1 to 3 double bonds and/or triple bonds and having 2-14 carbon atoms which may be substituted with at least one substituent group selected from the group consisting of an alkoxy group having 1-5 carbon atoms, an alkanoyloxy group having 1-5 carbon atoms, a hydroxy group, fluorine, chlorine, bromine, iodine, an amino group, a nitro group, a cyano group, a trifluoromethyl group and a phenoxy group, and wherein from 1 to 3 methylene groups may be replaced with carbonyl groups, or a straight-chain or branched chain saturated or unsaturated hydrocarbon group containing from 1 to 5 thioether, ether and/or amino bonds and having 1-14 carbon atoms wherein hetero atoms are not bonded directly to A, and 1 to 3 methylene groups may be replaced with carbonyl groups;R.sup.5 represents a hydrogen atom or an organic group which may be substituted with at least one or more substituent groups selected from the group consisting of an alkyl group having 1-5 carbon atoms, an alkoxy group having 1-5 carbon atoms, an alkoyloxy group having 1-5 carbon atoms, a hydroxy group, fluorine, chlorine, bromine, iodine, an amino group, a nitro group, a cyano group, an isothiocyanate group, a trifluoromethyl group and a methylenedioxy group; orR.sub.5 is ##STR16## wherein Q is N, O or S;T is CH, N, S or O;l is 0-5;m and n are >0;m+n<5;R.sup.6 represents a hydrogen atom;R.sup.7 represents a hydrogen atom, a hydroxy group, an alkoxy group having 1-5 carbon atoms, an alkanoyloxy group having 1-5 carbon atoms, or R.sup.6 and R.sup.7 together represent --O--, --CH.sub.2 -- or --S--, andR.sup.8 represents a hydrogen atom, an alkyl group having 1-5 carbon atoms, or an alkanoyl group having 1-5 carbon atoms in a pharmaceutically acceptable carrier.