PSYCHOTROPIC POLYCYCLIC IMIDES

摘要

Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: in which X is -O-, -S-, -SO-, -SO2-, -CR3R4- where R3 and R4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R3 and R4 form a cycloalkyl group of 3 to 5 carbon atoms; n is one of the integers 2, 3, 4 or 5; R is phenyl, alkylphenyl in which the alkyl group contains 1 to 4 carbon atoms, halophenyl, trifluoromethylphenyl, alkoxyphenyl, in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R1 and R2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R1 and R2 complete a benzene ring, or a group of the formula: where Y is -CH2, -CH2-CH2-, -O- or -S- and the dotted line represents optional unsaturation; or a pharmaceutically acceptable salt thereof. In addition, the intermediate b3-dicarboxylic and the corresponding anhydrides - 2,3,3a,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopena[a]pentalene-1,3 -dicarboxylic acid and octahydro-1, 5-methano-6,8,9-metheno-pentaleno[1,2,-d]oxepin-2,4(1H, 5H)-dione represent especially significant aspects of the invention.