Patent ID: 6319919
Filing Date: 2001-11-20
Classification: A61K,C07D

Abstract:
A method of inhibiting acetyl cholinesterase activity in a patient which comprises administering to said patient a therapeutically effective amount of a compound of the formula ##STR48##wherein the broken line represents an optionally present double bond, R.sub.1 and R.sub.2 are each selected independently from the group consisting of hydrogen, hydroxy, amino, alkylamino, cyano, sulfhydryl, alkoxy of 1-6 carbon atoms, aryloxy, aralkoxy, R.sub.5 -substituted aryloxy, monoalkyl, dialkyl or aryl carbamate group, wherein the monoalkyl, dialkyl or aryl moiety may be R.sub.5 -substituted or unsubstituted, (R.sub.5 -substituted aryl)oxymethyl, alkanoyloxy, hydroxy-substituted alkanoyloxy, benzoyloxy, and R.sub.5 -substituted benzoyloxy;R.sub.3 is hydrogen, straight or branched chain alkyl of 1-6 carbon atoms, cycloalkylmethyl, or alkylphenyl or R.sub.3 is a heterocyclic selected from .alpha.- or .beta.-furyl, or .alpha.- or .beta.-thienyl, thenyl, pyridyl, pyrazinyl or pyrimidyl;each R.sub.4 is independently selected from the group consisting of hydrogen, hydroxyl, sulfhydryl, alkyl, aryl, alkoxy, aryloxy, alkaryloxy, nitro, amino, N-alkylamino, N-arylamino, N-alkarylamino, fluoro, chloro, bromo, iodo and trifluoromethyl;R.sub.5 is selected from the group consisting of hydroxyl, sulfhydryl, alkyl, aryl, alkoxy, aryloxy, alkaryloxy, nitro, amino, N-alkylamino, N-arylamino, N-alkarylamino, fluoro, chloro, bromo, iodo and trifluoromethyl;R.sub.6 is selected from the group consisting of hydrogen, halo, trifluoromethyl or alkyl of from 1 to 4 carbon atoms; R.sub.9 is hydrogen or alkyl of 1 to 6 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof with the proviso that R.sub.3 is not methyl when R.sub.1 is methoxy, R.sub.2 is hydroxy and all R.sub.4 's are hydrogen.