3-AMINO-1-BENZAZEPIN-2-ONE-1-ALCANOIC ACIDS, PROCESS FOR THEIR PREPARATION, THEIR PHARMACEUTICAL PREPARATION AS WELL AS THEIR THERAPEUTIC USE

1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Compounds of the general formula see diagramm : EP0119955,P34,F1 wherein R**1 represents 4-aminobutyl, R**2 and R**3 represent, independently of each other, hydroxy or lower alkoxy, and S represents the chirality, or salts...

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1. Verfasser: WATTHEY, JEFFREY W.H
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Compounds of the general formula see diagramm : EP0119955,P34,F1 wherein R**1 represents 4-aminobutyl, R**2 and R**3 represent, independently of each other, hydroxy or lower alkoxy, and S represents the chirality, or salts thereof. 1. Claims for Contracting State : AT A process for the preparation of a 3-(5-aminopentyl)- amino-1-benzazepin-2-one-1-alkanoic acid of the general formula see diagramm : EP0119955,P38,F1 wherein R**1 represents 4-aminobutyl, R**2 and R**3 represent, independently of each other, hydroxy or lower alkoxy, and S represents the chirality, or a salt thereof, characterised in that a) a compound of the formula see diagramm : EP0119955,P38,F2 as the S-enantiomer or mixture of stereoisomers containing said enantiomer, wherein R**3 has the meanings given above, is alkylated with a compound of the formula see diagramm : EP0119955,P38,F3 as the S-enantiomer or mixture of stereoisomers containing said enantiomer, wherein Z is a reactive esterified hydroxy group and R**1 and R**2 have the meanings given above, or with a compound of the formula R**1 -CO-COR**2 wherein R**1 and R**2 have the meanings given above, in the presence of a reducing agent, with the temporary protection of the amino group and/or of hydroxy groups that may be present in any one of the radicals R**1 , R**2 and R**3 , or b) a compound of the formula see diagramm : EP0119955,P39,F1 or a mixture of stereoisomers containing said compound, wherein S, R**1 and R**2 have the meanings given above, is alkylated with a compound of the formula Z-CH2 COR**3 wherein Z is a reactive esterified hydroxy group and R**3 has the meanings given above, preferably with the temporary protection of the amino group and/or of hydroxy groups that may be present in any one of the reactants, or c) a compound of the formula see diagramm : EP0119955,P39,F2 wherein Y is oxo, a reactive esterified or etherified hydroxy group Z together with hydrogen or two reactive esterified or etherified hydroxy groups Z, and R**3 has the meanings given above, is condensed with an amine of the formula see diagramm : EP0119955,P39,F3 as the S-enantiomer or mixture of stereoisomers containing said enantiomer, wherein R**1 and R**2 have the meanings given above, with the proviso that when Y is oxo or two esterified or etherified hydroxy groups, the condensation is carried out in the presence of a reducing agent, or d) in a compound of the formul