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publicationDate 1983-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-4382940-A
titleOfInvention Ercoline derivatives and therapeutic compositions having CNS affecting activity
abstract Compounds are disclosed of formula (I) <IMAGE> (I) wherein R1 represents a hydrogen atom or a methyl group; R2 represents a hydrogen atom or a methoxy group; X represents an oxygen or sulphur atom or an NH or NCH3 group; R3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms; R4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R3 and R4 together represent a 3- or 4-membered carbon atom chain; Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR5 wherein R5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R5 and R3 together represent a 2- or 3-membered carbon atom chain; R6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; and R7 represents a hydrogen or halogen atom or a methyl or formyl group or a group of the formula SR8 wherein R8 represents a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; and the pharmaceutically acceptable addition salts with organic or inorganic acids thereof. A process for producing these compounds is also disclosed. These compounds are useful antidepressant, anxiolytic and neuroleptic agents. They also display from moderate to good antiprolactinic and antihypertensive activity.
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Total number of triples: 403.