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63 条记录 (耗时 0.031 秒)

    Process for the preparation of monocyclic, bicyclic and tricyclic aminoacids
    21.
    发明授权
    Process for the preparation of monocyclic, bicyclic and tricyclic aminoacids 失效
    制备单环，双环和三环氨基酸的方法

    公开(公告)号：US4691022A

    公开(公告)日：1987-09-01

    申请号：US623200

    申请日：1984-06-21

    申请人： Rainer Henning ,  Hansjorg Urbach

    发明人： Rainer Henning ,  Hansjorg Urbach

    IPC分类号： C07D207/16 ,  C07D207/20 ,  C07D209/08 ,  C07D209/42 ,  C07D209/52 ,  C07D209/54 ,  C07D209/72 ,  C07D209/96 ,  C07C103/52

    CPC分类号： C07D209/54 ,  C07D207/16 ,  C07D207/20 ,  C07D209/08 ,  C07D209/42 ,  C07D209/52

    摘要： The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which R represents hydrogen, alkyl or aralkyl, and R.sup.1 to R.sup.6 denote identical or different radicals hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aralkyl or aryl, both being monosubstituted, disubstituted or trisubstituted in the aryl moiety by alkyl, alkoxy, hydroxyl, halogen, nitro, methylenedioxy and/or cyano, or in which two of the radicals R.sup.1 to R.sup.6, together with the carbon atom(s) bearing them form a monocyclic or bicyclic ring system, and the remaining radicals are hydrogen, which process comprises converting, with an oxidizing agent in the presence of a silver salt, a pyrrolidine derivative of the formula II into a .DELTA..sup.1 -pyrroline derivative of the formula III, reacting the latter with hydrogen cyanide or a metal cyanide to form a nitrile of the formula IV, and subjecting the latter to solvolysis with a compound of the formula ROH.

    摘要翻译： 本发明涉及一种制备式I化合物的方法，其中R代表氢，烷基或芳烷基，R1至R6表示相同或不同的基团氢，烷基，环烷基，环烷基烷基，环烯基烷基，芳烷基或芳基 两者在芳基部分中被烷基，烷氧基，羟基，卤素，硝基，亚甲二氧基和/或氰基单取代，二取代或三取代，或其中两个基团R1至R6与带有它们的碳原子一起 形成单环或双环系统，其余基团是氢，该方法包括用银盐存在下的氧化剂将式II的吡咯烷衍生物转化为式III的DELTA 1-吡咯啉衍生物 使后者与氰化氢或金属氰化物反应以形成式IV的腈，并使其后者与式ROH的化合物溶剂解。

    N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use thereof
    22.
    发明授权
    N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use thereof 失效
    N-酰基六氢吲哚-2-羧酸及其抗高血压用途

    公开(公告)号：US4562202A

    公开(公告)日：1985-12-31

    申请号：US477333

    申请日：1983-03-21

    申请人： Hansjorg Urbach ,  Rainer Henning ,  Volker Teetz ,  Hans Wissmann ,  Reinhard Becker

    发明人： Hansjorg Urbach ,  Rainer Henning ,  Volker Teetz ,  Hans Wissmann ,  Reinhard Becker

    IPC分类号： A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  C07D209/42 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  A61K31/40

    CPC分类号： C07K5/0222 ,  C07D209/42 ,  A61K38/00

    摘要： The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1,R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl,and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes for their preparation.

    摘要翻译： 本发明涉及式I的化合物，其中n表示0或1，R表示氢，烷基或芳烷基，R1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰基氨基取代， ，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可以被烷基，烷氧基或卤素，芳基烷基或芳酰基烷基取代，二者可以在如上所定义的芳基中被取代，单环或双环硫 或氧和/或氮杂环基或天然存在的氨基酸的侧链，R 2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢或Y，Z一起表示氧，X表示烷基， 烯基，环烷基，芳基，其被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基或3-吲哚基单取代或三取代，及其生理学 表盐，其制备方法，含有这些物质的药剂及其作为药物的用途以及双环氨基酸作为其中间体及其制备方法。

    Derivatives of tricyclic aminoacids, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation
    23.
    发明授权
    Derivatives of tricyclic aminoacids, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation 失效
    三环氨基酸的衍生物，其制备方法，含有这些化合物的药剂及其用途，以及新的双环氨基酸作为其中间体及其制备方法

    公开(公告)号：US4558065A

    公开(公告)日：1985-12-10

    申请号：US550531

    申请日：1983-11-10

    申请人： Hansjorg Urbach ,  Rainer Henning ,  Reinhard Becker

    发明人： Hansjorg Urbach ,  Rainer Henning ,  Reinhard Becker

    IPC分类号： C07D209/70 ,  A61K31/40 ,  A61K31/403 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/58 ,  C07D221/22 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  A61K37/00

    CPC分类号： C07D209/58 ,  C07D221/22 ,  C07K5/0222 ,  A61K38/00

    摘要： The invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR1## in which n denotes 0 or 1, A denotes --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S-, O- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation.

    摘要翻译： 本发明涉及式I（I）的三环氨基酸的新衍生物，其中n表示0或1，A表示-CH = CH-或-CH 2 -CH 2 - ，R表示氢，烷基或芳烷基， R 1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰基氨基取代，或链烯基，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可被烷基，烷氧基或卤素取代，或芳烷基或 芳基烷基，二者可以如上所定义，或可被保护的单环或双环S-，O-和/或N-杂环烯基或天然存在的氨基酸的侧链，R 2表示氢，烷基 ，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基，环烷基，芳基，可以被烷基，烷氧基单，二或三取代 ，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和/或亚甲二氧基，或 3-吲哚基及其生理学上可接受的盐，其制备方法，含有这些化合物的试剂及其用途，以及新的双环氨基酸作为其中间体及其制备方法。

    Derivatives of 2-azabicyclo[3.1.0]hexane-3-carboxylic acid, and hypotensive use thereof
    28.
    发明授权
    Derivatives of 2-azabicyclo[3.1.0]hexane-3-carboxylic acid, and hypotensive use thereof 失效
    2-氮杂双环[3.1.0]己烷-3-羧酸的衍生物及其降血压用途

    公开(公告)号：US4591598A

    公开(公告)日：1986-05-27

    申请号：US627639

    申请日：1984-07-03

    申请人： Hansjorg Urbach ,  Rainer Henning ,  Reinhard Becker

    发明人： Hansjorg Urbach ,  Rainer Henning ,  Reinhard Becker

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/52 ,  C07D221/04 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K14/81 ,  C07D209/02

    CPC分类号： C07D221/04 ,  C07D209/52 ,  C07K5/0222 ,  A61K38/00

    摘要： The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1, R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, aralkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined previously, a monocyclic or bicyclic S- or O- and/or N-heterocyclic radical or a side chain of an aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, acylamino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and to a process for their preparation, agents containing them and and their use, and to 2-azabicyclo[3.1.0]hexane derivatives as intermediates, and a process for their preparation.

    摘要翻译： 本发明涉及式I的化合物，其中n表示0或1，R表示氢，烷基，链烯基或芳烷基，R1表示氢或烷基，其可任选被氨基，酰氨基或苯甲酰氨基 ，烯基，环烷基，环烯基，环烷基烷基，芳基或部分氢化的芳基，其各自可以被烷基，烷氧基或卤素取代，芳烷基或芳酰基烷基，它们都可以在如前定义的芳基中被取代，单环或双环 S-或O-和/或N-杂环基或氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z一起表示氧，X表示 烷基，烯基，环烷基，芳基，其可以被烷基，烷氧基，羟基，卤素，硝基，氨基，酰氨基，烷基氨基，二烷基氨基和/或亚甲二氧基或3-吲哚基单取代或三取代， 准备，代理 含有它们及其用途，以及作为中间体的2-氮杂双环[3.1.0]己烷衍生物及其制备方法。

    2-Azasfiro[4.(3+N)]-3-carboxylic acid derivatives, a process for their preparation, agents containing these derivatives and their use
    29.
    发明授权
    2-Azasfiro[4.(3+N)]-3-carboxylic acid derivatives, a process for their preparation, agents containing these derivatives and their use 失效
    2-氮杂四环[4.（3 + N）] - 3-羧酸衍生物，其制备方法，含有这些衍生物的试剂及其用途

    公开(公告)号：US4558064A

    公开(公告)日：1985-12-10

    申请号：US478780

    申请日：1983-03-25

    申请人： Volker Teetz ,  Hansjorg Urbach ,  Reinhard Becker

    发明人： Volker Teetz ,  Hansjorg Urbach ,  Reinhard Becker

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K38/00 ,  A61P9/12 ,  C07D209/54 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07D209/96 ,  A61K31/395

    CPC分类号： C07K5/0222 ,  C07D209/54 ,  A61K38/00

    摘要： The invention relates to compounds of the formula I ##STR1## in which n denotes 1, 2, 3 or 4, R is alkyl, alkenyl cycloalkyl, aryl, optionally mono-, di- oder trisubstituted by alkyl, alkoxy, hydroxy, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or indol-3-yl, R.sup.1 denotes an optionally protected radical of a naturally occurring amino acid HOOC--CH(NH.sub.2)--R.sup.1, R.sup.2 denotes hydrogen, alkyl or optionally nitro-substituted aralkyl, R.sup.3 denotes hydrogen, alkyl or cycloalkyl or optionally nitro-substituted aralkyl and X denotes 2 hydrogen atoms or 1 oxygen atom, their physiologically tolerated salts with acids and, if R.sup.2 and/or R.sup.3 denote hydrogen, with bases, a process for their preparation, agents containing these derivatives and their use as medicaments.

    摘要翻译： 本发明涉及式I化合物（Ⅰ），其中n表示1,2,3或4，R是烷基，链烯基环烷基，芳基，任选地被烷基，烷氧基，羟基 ，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基或吲哚-3-基，R 1表示天然存在的氨基酸HOOC-CH（NH 2）-R 1的任意保护的基团，R 2表示氢，烷基或任选的硝基 - 取代的芳烷基，R 3表示氢，烷基或环烷基或任选的硝基取代的芳烷基，X表示2个氢原子或1个氧原子，它们与酸的生理上可耐受的盐，如果R2和/或R3表示氢，则与碱反应， 其制剂，含有这些衍生物的药剂及其作为药物的用途。