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    • 95. 发明专利
      ES546807A0  未知
    • ES546807A0
    • 1987-05-01
    • ES546807
    • 1985-09-09
    • DUPHAR INT RES
    • C07D211/46 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/455 , C07D211/32 , C07D211/58 , C07D211/62 , C07D295/18 , C07D295/194 , C07C87/20 , A61K31/13
    • The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1)wherein the symbols have the following meanings:Ⓐ is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and or sulphur and or nitrogen;R 1 and R 2 may be equal or different and are hydrogen, alkyl having 1-3 carbon atoms, hydroxyalkyl or mercaptoalkyl having 1-3 carbon atoms wich may be etherified or esterified, alkoxy having 1-3 carbon atoms, the group S(O) m -R 9 , wherein Rg is an alkyl group having 1-3 carbon atoms, and m has the value 0, 1 or 2, a group - NR 10 R 11 , wherein R io and R 11 represent alkyl having 1-3 carbon atoms, or together may form a saturated, 5 or 6 membered ring which may contain a sulphur, oxygen or nitrogen atom as second hetero atom, R, and R 2 represent an optionally derivated hydroxy group, mercapto group or amino group, or a halogen atom, or R 1 and R 2 together may form a 5- or 6-membered ring optionally containing 1 or 2 oxygen, and/or nitrogen and/or sulphur atoms, which ring is condensed with Ⓐ, is fully or partly unsaturated and may be substituted by one or more alkyl groups having 1-3 carbon atoms, optionally etherified or esterified hydroxyalkyl having 1-3 carbon atoms or an oxygen atom;R 3 is a hydrogen atom or, together with R 4 , may form a ring consisting of 6 or 7 carbon atoms;R 4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R 5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R 6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR 12 , wherein R 12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or S0 2 group.R 7 and R 8 , together with the nitrogen atom to which they are bound, constitute a fully or partly saturated heterocyclic ring consisting of 5-8 ring atoms and which may comprise in addition an 0, N or S-atom as the second hetero atom, and may be substituted by 1 or 2 alkyl groups having 1-3 carbon atoms, an alkylene bridge of 2 or 3 carbon atoms across the ring. or an oxygen atom which, in case of a keto function may optionally have the form of a ketal or oxim, or the ring formed by R 7 and R 8 may be substituted directly or via an alkylene chain of 1-3 carbon atoms, with 1 or 2 of the following substituents: phenyl or phenyl substituted with halogen, alkyl or alkoxy having 1-3 carbon atoms, hydroxy, amino, mono- or dialkylamino having 1-3 carbon atoms in the alkyl group(s), alkanoyl or thioalkanoyl having 1-3 carbon atoms, hydroxy alkanoyl having 1-3 carbon atoms, benzoyl, optionally esterified or etherified hydroxy or mercapto, optionally mono- or dialkyl and/or -acyl substituted amino, carbalkoxy having 1-3 carbon atoms in the alkoxy group, a carbamoyl, thiocarbamoyl, sulfamoyl or carbamoyloxy group of which the nitrogen atom may be substituted by 1 or 2 alaoxy groups having 1-3 carbon atoms and/or alkyl groups having 1-5 carbon atoms, which, optionally via a nitrogen, oxygen or sulphur atom, may form a substituted or non- sabstituted saturated heterocyclic grohup consisting of 5 or 6 ring atoms
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