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AssigneeSchering Corporation
InventorsRalph Schmiechen, Reinhard Horowski, Dieter Palenschat, Gert Paschelke, Helmut Wachtel, Wolfgang Kehr
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4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl, carboxamido or amino or collectively are alkylene of 1-3 carbon atoms, R.sub.3 is H or OCH.sub.3, R.sub.4 is H, alkyl, aryl or acyl and X is O or S possess neuropsychotropic activity. The compounds wherein X is O are produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-aminobutyric acid or alkyl ester thereof. The pyrrolidones are converted to corresponding thiopyrrolidones in a conventional manner, e.g., by reaction with phosphorous pentasulfide in the presence of base.
A pharamaceutical composition for the treatment of neurological and psychic disorders responsive to chlorpromazine therapy and characterized by one or more of the symptoms of anxiety, hostility, agression, withdrawal, hallucination, thought-disturbances, delusion and agitation, comprising, in admixture with a pharmaceutically acceptable carrier, an amount per dosage unit from 0.05-20 mg. effective to reduce the symptoms of such disorders, of a 4-(polyalkoxyphenyl)-2-pyrrolidone of the formula ##STR49## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms or alkyl of 1-5 carbon atoms substituted by one or more halogen atoms or by one hydroxy, carboxy, alkoxy of 1-5 carbon atoms, alkoxycarbonyl of 1-5 carbon atoms in the alkoxy group, carboxamido, alkylcarboxamido, dialkylcarboxamido, carboxycyclicamido, amino, alkylamino, dialkyl or alkyleneimino, wherein alkyl in each instance is of 1-5 carbon atoms and wherein the nitrogen atom of the cyclicamido and alkyleneimino groups is a ring member of alkyleneimino of 4 to 7 members or R.sub.1 or R.sub.2 collectively are alkylene of 1-3 carbon atoms;
Dependencies are inferred from the claim text.