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    Derivatives of 1-phenoxy-3-amino-propan-2-ol
    3.
    发明授权
    Derivatives of 1-phenoxy-3-amino-propan-2-ol 失效

    公开(公告)号：US4066768A

    公开(公告)日：1978-01-03

    申请号：US669995

    申请日：1976-03-24

    申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    IPC分类号： C07C43/205 ,  C07D213/30 ,  C07D213/50 ,  C07D231/12 ,  C07D237/08 ,  C07D239/36 ,  C07D241/12 ,  C07D277/28 ,  C07D303/24 ,  C07D307/46 ,  C07D333/22 ,  A61K31/44 ,  C07D213/36

    CPC分类号： C07D213/30 ,  C07C43/2055 ,  C07D213/50 ,  C07D231/12 ,  C07D237/08 ,  C07D239/36 ,  C07D241/12 ,  C07D277/28 ,  C07D303/24 ,  C07D307/46 ,  C07D333/22

    摘要： The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##STR1## wherein X denotes ##STR2## A denotes --CH.sub.2 --alkoxy, --O--alkoxyalkyl, --O--hydroxyalkyl or ##STR3## AN AROMATIC OR QUASI-AROMATIC, 5-MEMBERED OR 6-MEMBERED, MONOCYCLIC RING WHICH IS LINKED THROUGH A C atom which has one or 2 nitrogen, oxygen and/or sulphur hetero-atoms and which can be substituted additionally by one or more methyl groups, and R.sub.2 and R.sub.3 denote hydrogen, alkyl, alkenyl or cycloalkyl or, conjointly with the N atom to which they are linked, and optionally with a further oxygen or sulphur hetero-atom, denote a saturated, 5-membered or 6-membered, monocyclic, heterocyclic structure, and alkyl radicals contain 1 to 4 carbon atoms, alkoxy radicals contain 1 to 4 carbon atoms, alkenyl radicals contain 3 to 4 carbon atoms and cycloalkyl radicals contain 5 to 7 carbon atoms; and aldehyde condensation products and acid addition salts thereof and to the production thereof by a method selected from (A) reacting a compound having the formula ##STR4## with a compound of the general formula Y -- X wherein X has the meanings indicated above and Y represents halogen and, if X denotes ##STR5## ALSO REPRESENTS --OH, --OK and --ONa; (B) reacting a compound having the formula ##STR6## with a compound of the formula H.sub.2 N--X wherein X has the meanings indicated above and Z represents ##STR7## AND Hal denotes halogen; (C) reacting a phenol of the formula ##STR8## with a compound of the formula Z--CH.sub.2 NH--X wherein X has the meanings indicated above and Z denotes ##STR9## WHEREIN Hal represents a halogen atom; and that the resulting compound is optionally reacted with an aldehyde of the formula R.sub.4 --CHO, wherein R.sub.4 denotes hydrogen or a lower alkyl radical having up to 4 C atoms, to form an oxyzolidine of the formula ##STR10## or is optionally reacted with an acid to form an acid addition salt.

    Derivatives of 1-phenoxy-3-amino-propan-2-ol and process for their production
    4.
    发明授权
    Derivatives of 1-phenoxy-3-amino-propan-2-ol and process for their production 失效
    1-苯氧基-3-氨基 - 丙-2-醇的衍生物及其制备方法

    公开(公告)号：US3969363A

    公开(公告)日：1976-07-13

    申请号：US531325

    申请日：1974-12-10

    申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    IPC分类号： C07D213/38 ,  C07D213/50 ,  C07D213/85 ,  C07D303/24 ,  C07D413/06 ,  C07D213/72

    CPC分类号： C07D303/24 ,  C07D213/38 ,  C07D213/50 ,  C07D213/85

    摘要： The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU1## and the aldehyde condensation products and acid addition salts thereof wherein X is selected from the group consisting of ##EQU2## wherein the phenyl ring I may have attached to it up to three similar or different substituents selected from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, alkinyloxy, benzyloxy, phenyl, halogen and --NR.sub.1 R.sub.2, wherein R.sub.1 is selected from alkyl and acyl, and R.sub.2 is selected from hydrogen and alkyl and n is 1, 2 or 3; and to the production thereof by a method selected from (A) reacting 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU3## with a compound having the formula Y-X, wherein X has the above defined meaning and Y is selected from halogen, --OH, --OK or --ONa; (B) reacting a compound of the formula ##EQU4## with a compound of the formula H.sub.2 N--X, wherein X has the above-defined meaning and Z is selected from ##EQU5## and ##EQU6## (C) reacting a phenol ##EQU7## with Z--CH.sub.2 --NH--X, wherein X and Z have the meaning defined above.

    摘要翻译： 本发明涉及具有式-O-CH2-CH-CH2-NH-X | OH的1-苯氧基-3-氨基 - 丙-2-醇的新药理学上有价值的衍生物及其醛缩合产物及其酸加成盐 其中X选自-C = CH-C和| PARALLEL CH3O -CH-CH2-CH || CH3OH，其中苯环I可以连接至最多三个相似或不同的取代基，所述取代基选自 烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，链烯氧基，苄氧基，苯基，卤素和-NR1R2，其中R1选自烷基和酰基，R2选自氢和烷基，n为1,2或 3; 并通过选自（A）使具有式-O-CH 2 -CH-CH 2 -NH 2 | OH的1-苯氧基-3-氨基 - 丙-2-醇与具有式YX的化合物反应的方法制备， 其中X具有上述含义，Y选自卤素，-OH，-OK或-ONa; （B）使式-O-CH2-Z的化合物与式H2N-X的化合物反应，其中X具有上述定义，Z选自-CH-CH 2 ANGLE O和-CH 2 -CH 2 - 卤素; | OH（C）使苯酚-OH与Z-CH2-NH-X反应，其中X和Z具有上述定义。

    Derivatives of 1-phenoxy-3-amino-propan-2-ol
    5.
    发明授权
    Derivatives of 1-phenoxy-3-amino-propan-2-ol 失效
    1-苯氧基-3-氨基 - 丙-2-醇的衍生物

    公开(公告)号：US4020071A

    公开(公告)日：1977-04-26

    申请号：US531324

    申请日：1974-12-10

    申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

    IPC分类号： C07D239/26 ,  C07D303/22 ,  C07D303/24 ,  C07D239/06

    CPC分类号： C07D303/22 ,  C07D239/26 ,  C07D303/24 ,  Y10S514/821

    摘要： The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##STR1## and the aldehyde condensation products and acid addition salts thereof wherein X is selected from the group consisting of ##STR2## wherein the phenyl ring I may have attached to it up to three similar or different substituents selected from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, alkinyloxy, benzyloxy, phenyl, halogen and --NR.sub.1 R.sub.2, wherein R.sub.1 is selected from alkyl and acyl, and R.sub.2 is selected from hydrogen and alkyl; and to the production thereof by a method selected from (A) reacting 1-phenoxy-3-amino-propan-2-ol having the formula ##STR3## with a compound having the formula Y-X, wherein X has the above-defined meaning and Y is selected from halogen, --OH, --OK or --ONa; (B) reacting a compound of the formula ##STR4## with a compound of the formula H.sub.2 N--X, wherein X has the above-defined meaning and Z is selected from ##STR5## and ##STR6## (C) reacting a phenol ##STR7## wherein X and Z have the meaning defined above.

    摘要翻译： 本发明涉及具有下式的1-苯氧基-3-氨基 - 丙-2-醇的新药理学上有价值的衍生物及其醛缩合产物及其酸加成盐，其中X选自和，其中苯环I可以连接至多至三个相似或不同的选自烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，烷氧基，苄氧基，苯基，卤素和 -NR1R2，其中R1选自烷基和酰基，R2选自氢和烷基; 并且通过选自（A）使具有式“IMAGE”的1-苯氧基-3-氨基 - 丙-2-醇与具有式YX的化合物反应的方法制备，其中X具有上述含义， Y选自卤素，-OH，-OK或-ONa; （B）使式“IMAGE”的化合物与式H2N-X的化合物反应，其中X具有上述含义并且Z选自和（C）使苯酚其中X和Z具有上述定义。

    Derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production
    7.
    发明授权
    Derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production 失效
    1-苯氧基-3-氨基丙烷-2-醇的衍生物及其制备方法

    公开(公告)号：US3940406A

    公开(公告)日：1976-02-24

    申请号：US362567

    申请日：1973-05-21

    申请人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

    发明人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

    IPC分类号： C07D213/30 ,  A61K31/4406 ,  C07D213/38 ,  C07D213/50 ,  C07D303/24 ,  C07D413/06 ,  C07D213/36 ,  C07D213/40

    CPC分类号： C07D303/24 ,  C07D213/38 ,  C07D213/50

    摘要： The present invention relates to pharmacologically valuable new derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production. The new derivatives of 1-phenoxy-3-amino-propane-2-ol are suitable for the treatment and prophylaxis of diseases of the heart. Some possess pronounced .beta.-adrenalytic or anti-arythmic properties. These new derivatives have the structural formula ##SPC1##Wherein X signifies ##SPC2##And the phenyl nucleus I may be mono-, di- or trisubstituted by alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, phenyl, halogen or the radical --NR.sub.1 R.sub.2, in which R.sub.1 stands for alkyl or acyl and R.sub.2 for hydrogen or alkyl, together with their aldehyde condensation products and their acid addition salts.

    摘要翻译： 本发明涉及1-苯氧基-3-氨基丙烷-2-醇的药理学有价值的新衍生物及其生产方法。 1-苯氧基-3-氨基 - 丙烷-2-醇的新衍生物适用于治疗和预防心脏疾病。 一些具有显着的β-去肾上腺素或抗-Arcional性质。 这些新衍生物具有结构式X表示，而苯基核I可以被烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，苯基，卤素或基团-NR1R2单，二或三取代，其中 R1代表烷基或酰基，R2代表氢或烷基，以及它们的醛缩合产物及其酸加成盐。

    Derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production
    8.
    发明授权
    Derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production 失效
    1-苯氧基-3-氨基丙烷-2-醇的衍生物及其制备方法

    公开(公告)号：US4018778A

    公开(公告)日：1977-04-19

    申请号：US488194

    申请日：1974-07-12

    申请人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

    发明人： Thomas Raabe ,  Josef Scholtholt ,  Rolf-Eberhard Nitz

    IPC分类号： C07D213/50 ,  C07D213/28

    CPC分类号： C07D213/50

    摘要： The present invention relates to pharmacologically valuable new derivatives of 1-phenoxy-3-amino-propane-2-ol and process for their production. The new derivatives of 1-phenoxy-3-amino-propane-2-ol are suitable for the treatment and prophylaxis of diseases of the heart. Some possess pronounced .beta.-adrenalytic or anti-arythmic properties. These new derivatives have the structural formula ##STR1## wherein X signifies ##STR2## and the phenyl nucleus I may be mono-, di- or trisubstituted by alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, phenyl, halogen or the radical --NR.sub.1 R.sub.2, in which R.sub.1 stands for alkyl or acyl and R.sub.2 for hydrogen or alkyl, together with their aldehyde condensation products and their acid addition salts.

    摘要翻译： 本发明涉及1-苯氧基-3-氨基丙烷-2-醇的药理学有价值的新衍生物及其生产方法。 1-苯氧基-3-氨基 - 丙烷-2-醇的新衍生物适用于治疗和预防心脏疾病。 一些具有显着的β-去肾上腺素或抗-Arcional性质。 这些新衍生物具有结构式：其中X表示“IMAGE”，苯基核I可以被烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，苯基，卤素或 基团-NR1R2，其中R1代表烷基或酰基，R2代表氢或烷基，以及它们的醛缩合产物及其酸加成盐。

    N-Aryloxypropyl-N'-dioxopyrimidyl-.alpha.,.omega.-alkylenediamines
    9.
    发明授权
    N-Aryloxypropyl-N'-dioxopyrimidyl-.alpha.,.omega.-alkylenediamines 失效
    N-芳氧基丙基-N'-二氧嘧啶基-α，ω-亚烷基二胺

    公开(公告)号：US4216314A

    公开(公告)日：1980-08-05

    申请号：US902000

    申请日：1978-05-02

    申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Eckhard Schraven

    发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Eckhard Schraven

    IPC分类号： C07D239/54 ,  A61K31/505 ,  A61K31/513 ,  A61P9/06 ,  A61P9/12 ,  A61P25/02 ,  C07D233/40 ,  C07D233/44 ,  C07D239/545 ,  C07D413/12

    CPC分类号： C07D239/545 ,  Y10S514/821

    摘要： Physiologically-acceptable substituted 1,2-ethylenediamines and 1,3-propylenediamines, in free-base and in acid-addition-salt form, have highly pronounced and cardioselective .beta.-adrenolytic action, antiarrhythmic action and hypotensive action on administration to humans. The diamines are, more specifically, N-[3-aryloxy-2-hydroxypropyl]-N'-[1,3-(di-R.sup.3)-2,4-dioxypyrimid-6-yl] (ethylene or propylene)diamines wherein R.sup.3 is --H or lower alkyl and the aryl nucleus is either further unsubstituted, further monosubstituted or further disubstituted.The compounds are prepared, e.g, by reacting a corresponding N-[3-phenoxy-2-hydroxypropyl] (ethylene or propylene)diamine with a corresponding 6-chloropyrimidine-2,4-dione in a suitable medium containing an acid-binding agent.Such compounds are administered orally or parenterally in effective, but substantially non-toxic, doses either in substantially pure form, in virtually any standard dosage form or in combination with one or more other pharmacologically- and chemically-compatible drugs.

    摘要翻译： 以游离碱和酸加成盐形式的生理学上可接受的取代的1,2-乙二胺和1,3-丙二胺具有非常显着的和心脏选择性的β-肾上腺素能作用，抗心律失常作用和对人的施用的降血压作用。 二胺更具体地是N- [3-芳氧基-2-羟丙基] -N' - [1,3-（二-R 3）-2,4-二氧嘧啶-6-基]（乙烯或丙烯）二胺，其中 R3是-H或低级烷基，芳基核可以是未被取代的，进一步单取代的或进一步二取代的。 制备化合物，例如通过使相应的N- [3-苯氧基-2-羟丙基]（乙烯或丙烯）二胺与相应的6-氯嘧啶-2,4-二酮在合适的含有酸结合剂的介质中反应 。 这些化合物以实质上任何标准剂型形式或与一种或多种其它药学上和化学上相容的药物组合的有效但基本上无毒的剂量以基本上纯的形式口服或肠胃外给药。