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    Phenoxypropanolamine
    1.
    发明授权
    Phenoxypropanolamine 失效
    酚羟丙基胺

    公开(公告)号：EP0140243B1

    公开(公告)日：1988-11-09

    申请号：EP84112213.8

    申请日：1984-10-11

    申请人： F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft

    发明人： Alig, Leo, Dr. ,  Müller, Marcel, Dr.

    IPC分类号： C07C101/42 ,  C07C101/34 ,  C07C101/28 ,  C07C97/10 ,  C07C103/28 ,  C07C103/76 ,  C07C93/06 ,  C07C93/14 ,  C07C93/187 ,  C07C143/80 ,  C07D333/06

    CPC分类号： C07D295/088 ,  C07C229/38 ,  C07D333/20 ,  C07D333/24 ,  C07D333/38

    摘要： 1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE) Phenoxypropanolamines of the formula see diagramm : EP0140243,P23,F1 wherein n is the number 1 or 2, R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl, X**1 is phenoxymethyl optionally monofluorinated or mono-chlorinated in the ortho-position, X**2 is lower-alkyl, phenoxymethyl optionally monofluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy, Y is hydrogen or methyl, Z is a group of the formula see diagramm : EP0140243,P24,F1 or see diagramm : EP0140243,P24,F2 R**1 is optionally N-mono-lower-alkylated or N-di-lower-alkylated aminomethyl or a residue -(C(O)R**2 , -C(R**3 ) = CH-(CH2 )m -C(O)R**2 , -C(H,R**3 )-(CH2 )m+1 -C(O)R**2 , -C(H,R**3 )-(CH2 )p -OH or -C(R**3 ) = CH-C(CH3 ) = CH-COOCH3 , R**11 is hydroxy, lower-alkanoyloxy, sulphamoyl, benzyloxy or phenoxy optionally ring-substituted by fluorine, chlorine, trifluoromethyl, lower-alkyl or lower-alkoxy, or a group R**1 , -O-(CH2 )q -OH, -O-(CH2 )q -O-(CH2 )t -R**5 or see diagramm : EP0140243,P24,F3 R**2 is hydroxy, lower-alkyl, lower-alkoxy, dimethylaminoethoxy, lower-alkoxycarbonylethyl or optionally mono-lower alkylated or di-lower alkylated amino, R**3 is hydrogen or methyl, R**5 is hydrogen, lower-alkyl or phenyl, R**6 is lower-alkyl or phenyl optionally para-substituted by fluorine, chlorine, lower-alkyl or lower-alkoxy, m and p are whole numbers of 0 to 6, v is a whole number of 2 to 4, q and t are whole numbers of 1 to 6, and physiologically compatible salts thereof. 1. Claims (for the Contracting State AT) A process for the manufacture of phenoxypropanolamines of the formula see diagramm : EP0140243,P25,F1 wherein n is the number 1 or 2, R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl, X**1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position, X**2 is lower-alkyl, phenoxymethyl optionally monofluorinated or mono-chlorinated in the orthoposition or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy, Y is hydrogen or methyl, Z is a group of the formula see diagramm : EP0140243,P25,F2 or see diagramm : EP0140243,P25,F3 R**1 is optionally N-mono-lower-alkylated or N-di-lower-alkylated aminomethyl or a residue -C(O)R**2 , -C(R**3 ) = CH-(CH2 )m -C(O)R**2 , -C(H,R**3 )-(CH2 )m+1 -C(O)R**2 , -C(H,R**3 )-(CH2 )p -OH or -C(R**3 ) = CH-C(CH3 ) = CH-COOCH3 , R**11 is hydroxy, lower-alkanoyloxy, sulphamoyl, benzyloxy or phenoxy optionally ring-substituted by fluorine, chlorine, trifluoromethyl, lower-alkyl or lower-alkoxy, or a group R**1 , -O-(CH2 )q -OH, -O-(CH2 )q -O-(CH2 )t -R**5 or see diagramm : EP0140243,P26,F1 R**2 is hydroxy, lower-alkyl, lower-alkoxy, dimethylaminoethoxy, lower-alkoxycarbonylethyl or optionally mono-lower alkylated or di-lower alkylated amino, R**3 is hydrogen or methyl, R**5 is hydrogen, lower-alkyl or phenyl, R**6 is lower-alkyl or phenyl optionally para-substituted by fluorine, chlorine, lower-alkyl or lower-alkoxy, m and p are whole numbers of 0 to 6, v is a whole number of 2 to 4, q and t are whole numbers of 1 to 6, and of physiologically compatible salts thereof, characterized by a) reacting an epoxide of the formula see diagramm : EP0140243,P26,F2 or a beta-keto halide of the formula see diagramm : EP0140243,P26,F3 with a primary amine of the formula see diagramm : EP0140243,P26,F4 or a secondary amine of the formula see diagramm : EP0140243,P26,F5 wherein in formulae II-V n, Y and Z the above significance, Hal is halogen, one of the groups X**3 and X**4 is a group X**1 and the other is a group X**2, whereby further X**3 is a group X**1 when a compound of formula II or III is reacted with a compound of formula IV, and reducing a X**1 -C(O)- or X**2 -C(O)- group in a compound obtained to a X**1 -CHOH- or X**2 -CHOH- group, b) if desired, functionally modifying a reactive substituent present in a group Z of a compound of formula I, c) if desired, alkanoylating or phenalkanoylating the hydroxy groups present in a diol of formula I, and d) if desired, converting a compound of formula I into a salt.

    摘要翻译： 1.索赔（对于缔约国：BE，CH，DE，FR，GB，IT，LI，LU，NL，SE）下式的苯氧基丙醇胺见图示：EP0140243，P23，F1，其中n为数1或2， R是氢，低级烷酰基或苯基 - 低级 - 烷酰基，X ** 1是在邻位任选单氟化或单氯化的苯氧基甲基，X ** 2是低级烷基，任选地单氟或单氯化的苯氧基甲基 邻位或苯基，任选被氟，氯，三氟甲基或低级烷氧基单取代，Y为氢或甲基，Z为下式基团：EP0140243，P24，F1或见图表：EP0140243，P24，F2 R * * 1任选为N-单低级烷基化或N-二 - 低级烷基化氨基甲基或残基 - （C（O）R ** 2，-C（R ** 3）= CH-（CH 2）m - C（O）R ** 2，-C（H，R ** 3） - （CH 2）m + 1 -C（O）R ** 2，-C（H，R ** 3） - （CH 2） p -OH或-C（R ** 3）= CH-C（CH 3）= CH-COOCH 3，R ** 11是羟基，低级烷酰氧基，氨磺酰基，苄氧基或任选被氟取代的苯氧基，氯 或三氟甲基，低级烷基或低级烷氧基，或基团R ** 1，-O-（CH 2）q -OH，-O-（CH 2）q -O-（CH 2）t -R ** 5或 参见图示：EP0140243，P24，F3 R ** 2是羟基，低级烷基，低级烷氧基，二甲基氨基乙氧基，低级烷氧基羰基乙基或任选的单 - 低级烷基化或二 - 低级烷基化氨基，R ** 3是氢或甲基， R ** 5为氢，低级烷基或苯基，R ** 6为低级烷基或任选被氟，氯，低级烷基或低级烷氧基取代的苯基，m和p为0至6的整数 ，v为2〜4的整数，q和t为1〜6的整数，以及其生理相容的盐。 1.索赔（用于缔约国AT）制备下式的苯氧基丙醇胺的方法见图表：EP0140243，P25，F1，其中n为数1或2，R为氢，低级烷酰基或苯基 - 低级烷酰基 X ** 1是在邻位任选单氟化或单氯化的苯氧基甲基，X ** 2是低级烷基，任选地在任意单氟化或单氯化的苯氧基甲基或任选被氟，氯，三氟甲基单取代的苯基 或低级烷氧基，Y为氢或甲基，Z为下式的基团：见图表：EP0140243，P25，F2或见图表：EP0140243，P25，F3 R ** 1任选为N-单低级烷基化或N - 二低级烷基化氨基甲基或残基-C（O）R ** 2，-C（R ** 3）= CH-（CH 2）m -C（O）R ** 2，-C（H， R ** 3） - （CH 2）m + 1 -C（O）R ** 2，-C（H，R ** 3） - （CH 2）p -OH或-C（R ** 3）= CH -C（CH 3）= CH-COOCH 3，R ** 11是羟基，低级烷酰氧基，氨磺酰基，苄氧基或任选被氟，氯，三 氟代甲基，低级烷基或低级烷氧基，或基团R ** 1，-O-（CH 2）q -OH，-O-（CH 2）q -O-（CH 2）t -R ** 5或见图 ：EP0140243，P26，F1 R ** 2是羟基，低级烷基，低级烷氧基，二甲基氨基乙氧基，低级烷氧基羰基乙基或任选的单 - 低级烷基化或二 - 低级烷基化氨基，R ** 3是氢或甲基，R * * 5是氢，低级烷基或苯基，R ** 6是低级烷基或任选被氟，氯，低级烷基或低级烷氧基取代的苯基，m和p是整数0至6，v 是整数2至4，q和t是1至6的整数，以及其生理上相容的盐，其特征在于：a）使下式的环氧化物反应见图示：EP0140243，P26，F2或β-酮 下式的卤化物参见图示：EP0140243，P26，F3与下式的伯胺见图表：EP0140243，P26，F4或下式的仲胺见图表：EP0140243，P26，F5其中式II-V n， Y和Z具有以上意义，Hal为卤素，1 基团X ** 3和X ** 4是基团X ** 1，另一个是基团X ** 2，其中当式II化合物或式II化合物时X ** 3为X ** 1族 III化合物与式IV化合物反应，并将所得化合物中的X ** 1 -C（O） - 或X ** 2 -C（O） - 基团还原成X ** 1 -CHOH-或X ** 2 -CHOH-基团，b）如果需要，功能性地修饰存在于式I化合物的基团Z中的反应性取代基，c）如果需要，烷酰基化或苯烷酰化存在于式I的二醇中的羟基，以及 d）如果需要，将式I化合物转化为盐。

    Orally effective inotropic compounds
    3.
    发明公开
    Orally effective inotropic compounds 失效
    ORALLY有效的无机化合物

    公开(公告)号：EP0146920A3

    公开(公告)日：1985-08-07

    申请号：EP84115837

    申请日：1984-12-19

    申请人： Key Pharmaceuticals, Inc.

    发明人： Tuttle, Ronald R.

    IPC分类号： C07C103/28 ,  A61K31/165

    CPC分类号： C07C255/00

    摘要： A method for increasing cardiac contractility in a warm-blooded animal suffering from acutely depressed cardiac contractility which comprises administering to said animal an effective amount of a compound of the formula
    wherein R is hydrogen or isobutyrate, or a pharmaceutically acceptable acid addition salt thereof.

    Orally effective inotropic compounds
    9.
    发明公开
    Orally effective inotropic compounds 失效
    链接口服性肌力作用。

    公开(公告)号：EP0146920A2

    公开(公告)日：1985-07-03

    申请号：EP84115837.1

    申请日：1984-12-19

    申请人： IVAX LABORATORIES INCORPORATED

    发明人： Tuttle, Ronald R.

    IPC分类号： C07C103/28 ,  A61K31/165

    CPC分类号： C07C255/00

    摘要： A method for increasing cardiac contractility in a warm-blooded animal suffering from acutely depressed cardiac contractility which comprises administering to said animal an effective amount of a compound of the formula
    wherein R is hydrogen or isobutyrate, or a pharmaceutically acceptable acid addition salt thereof.