DERIVATIVES OF 4-AMINO BUTYRIC ACID AND THEIR USE AS SEDATIVES

1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Amides of 4-aminobutyric acid corresponding to general formula : see diagramm : EP0046707,P19,F3 in which : R designates a linear or branched alkyl group having from 1 to 7 carbon atoms or a cycloalkyl group ; m represents...

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Hauptverfasser: JEANARLES MOLIMARD, JEAN-PIERRE CHAMBON
Format: Patent
Sprache:eng
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Zusammenfassung:1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Amides of 4-aminobutyric acid corresponding to general formula : see diagramm : EP0046707,P19,F3 in which : R designates a linear or branched alkyl group having from 1 to 7 carbon atoms or a cycloalkyl group ; m represents an integer of from 0 to 3 ; n represents an integer of from 0 to 2, on condition that m + n is equal to or greater than 1 ; X represents hydrogen, a lower alkyl group (1 to 4 carbons), a phenylalkyl group in which the phenyl group is possibility substituted, R1 and R2 considered separately designate hydrogen, a linear or branched alkyl group having from 1 to 18 carbon atoms, an aralkyl group, a cycloalkyl group or a possibly substituted phenyl group, or R1 and R2 considered together with the nitrogen atom to which they are attached represent a heterocycle with 5 or 6 groupings possibly comprising a second heteroatom such as pyrrolidine, morpholine, piperazine or pyridine and its partially or totally hydrogenated derivatives. 1. Claims for the Contracting State : AT Process for preparing amides of 4-aminobutyric acid corresponding to general formula (I) : see diagramm : EP0046707,P20,F3 in which : R designates a linear or branched alkyl group having from 1 to 7 carbon atoms or a cycloalkyl group ; m represents an integer of from 0 to 3 ; n represents an integer from 0 to 2, condition that m + n is equal to or greater than 1 ; X represents hydrogen, a lower alkyl group (1 to 4 carbons), a phenylalkyl group in which the phenyl group is possibly substituted, R1 and R2 considered separately designate hydrogen, a linear or branched alkyl group having from 1 to 18 carbon atoms, an aralkyl group, a cycloalkyl group or a possibly substituted phenyl group, or R1 and R2 considered together with the nitrogen atom to which they are attached represent a theterocycle with 5 or 6 groupings possibly comprising a second heteroatom such as pyrrolidine, morpholine, piperazine or pyridine and its partially or totally hydrogenated derivatives, characterized in that the starting product is constituted by an aminoacid of formula : see diagramm : EP0046707,P20,F4 in which m, n and X are such as defined above and R' is a hydrogen atom or a lower alkyl group (1 to 4 carbon atoms), said product is reacted on an acid chloride of formula R-COCI so as to convert the amine of the starting product into an amide radical and the product obtained is subjected to an amidification with a product of