Patent ID: 6057371
Filing Date: 2000-05-02
Classification: A61K,C07C,C07D

Abstract:
A method of treating a human being suffering from a sigma receptor associated central nervous system disorder, drug abuse, gastrointestinal disorder psychosis, angina, hypertension, migraine or depression, which comprises administering to said human a therapeutically effective amount of a compound of the formula: ##STR282## wherein: Ar is aryl, heteroaryl, substituted aryl or substituted heteroaryl, wherein the substituent is selected from the group consisting of chloro, fluoro, bromo, iodo, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 dialkoxymethyl, C.sub.1 -C.sub.6 alkyl, cyano, C.sub.3 -C.sub.15 dialkylaminoalkyl, carboxy, carboxamido, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 haloalkylthio, allyl, aralkyl, C.sub.3 -C.sub.6 cycloalkyl, aroyl, aralkoxy, C.sub.2 -C.sub.6 acyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C.sub.3 -C.sub.6 heterocycloalkyl, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.1 -C.sub.6 haloalkylsulfonyl, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 haloalkylsulfinyl, arylthio, C.sub.1 -C.sub.6 haloalkoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.15 dialkylamino, hydroxy, carbamoyl, C.sub.1 -C.sub.6 N-alkylcarbamoyl, C.sub.2 -C.sub.15 N,N-dialkylcarbamoyl, nitro, C.sub.2 -C.sub.15 dialkylsulfamoyl;R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, fluoro, chloro, bromo and =0; orR and R.sup.1 together form a morpholino, piperazinyl or piperidinyl ring;n is 0-5;W is --(CH.sub.2).sub.p -- or --H H--, wherein p is 1-3;X is --(CH.sub.2).sub.q --, wherein q is 1-6;--(CH.sub.2).sub.r --C.dbd.C--(CH.sub.2).sub.r --;--(CH.sub.2).sub.r --CH.dbd.CH--(CH.sub.2).sub.r --; ##STR283## --(CH.sub.2).sub.r --Y--(CH.sub.2).sub.r --, wherein each r is independently 0-3 and wherein Y is O or S; orC.sub.1 -C.sub.6 alkyl (wherein Z is hydrogen);Z is hydrogen, cycloalkyl, aryl, an aryl-substituted carboxylic acid group, or heteroaryl wherein Z may be substituted by chloro, fluoro, bromo, iodo, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 dialkoxymethyl, C.sub.1 -C.sub.6 alkyl, cyano, C.sub.3 -C.sub.15 dialkylaminoalkyl, carboxy, carboxamido, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 haloalkylthio, allyl, aralkyl, C.sub.3 -C.sub.6 cycloalkyl, aroyl, aralkoxy, C.sub.2 -C.sub.6 carboxylic acyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C.sub.3 -C.sub.6 heterocycloalkyl, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.1 -C.sub.6 haloalkylsulfonyl, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 haloalkylsulfinyl, arylthio, C.sub.1 -C.sub.6 haloalkoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.15 dialkylamino, hydroxy, carbamoyl, C.sub.1 -C.sub.6 N-alkylcarbamoyl, C.sub.2 -C.sub.15 N,N-dialkylcarbamoyl, nitro, C.sub.2 -C.sub.15 dialkylsulfamoyl or an ortho methylene-dioxy group;wherein said compound exhibits high binding activity with respect to the sigma receptor.