Patent ID: 6316461
Filing Date: 2001-11-13
Classification: A61K,A61P,C07D

Abstract:
A method for treating pruritus in a mammalian patient comprising administering a therapeutically effective amount of opiate K receptor agonist wherein the opiate K receptor agonist is a morphinan quaternary ammonium salt derivative represented by the general formula (II): ##STR56##wherein {character pullout} is a double bond, or a single bond; R.sup.1 is alkyl having 1 to 5 carbon atoms, cycloalkylalkyl having 4 to 7 carbon atoms, cycloalkenylalkyl having 5 to 7 carbon atoms, aralkyl having 7 to 13 carbon atoms, alkenyl having 4 to 7 carbon atoms, or allyl; R.sup.2 is hydrogen, hydroxy, nitro, alkanoyloxy having 1 to 5 carbon atoms; R.sup.3 is hydrogen, hydroxy, alkanoyloxy having 1 to 5 carbon atoms, or alkoxy having I to 5 carbon atoms; R.sup.4 is hydrogen, a straight or branched alkyl having 1 to 5 carbon atoms, or aryl having 6 to 12 carbon atoms; A is alkylene having 1 to 6 carbon atoms, --CH.dbd.CH--, or --C.ident.C--; and R.sup.5 is an organic group having any one of the following fundamental structures: ##STR57##wherein the organic group may have at least one substituent selected from the group consisting of alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, alkanoyloxy having 1 to 5 carbon atoms, hydroxy, fluorine, chlorine, bromine, iodine, nitro, cyano, isothiocyanato, trifluoromethyl, trifluoromethoxy and methylenedioxy; R.sup.6 is alkyl having 1 to 5 carbon atoms, or allyl; X.sup.- denotes an anion to form a pharmacologically acceptable salt; and the general formula (II) comprises (+), (-), and (.+-.) isomers.