利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

86 条记录 (耗时 0.025 秒)

    Process for the preparation of monocyclic, bicyclic and tricyclic aminoacids
    34.
    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。

    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
    35.
    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
    39.
    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。

    Aminodiol derivatives
    40.
    发明授权
    Aminodiol derivatives 失效
    氨基酸衍生物

    公开(公告)号：US5235057A

    公开(公告)日：1993-08-10

    申请号：US723223

    申请日：1991-06-28

    申请人： Heinz-Werner Kleemann ,  Rainer Henning ,  Hansjorg Urbach

    发明人： Heinz-Werner Kleemann ,  Rainer Henning ,  Hansjorg Urbach

    IPC分类号： C07D317/28 ,  C07D405/06

    CPC分类号： C07D405/06 ,  C07D317/28

    摘要： The invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen or aralkyl, R.sup.3 is alkyl, cycloalkyl or cycloalkylalkyl, R.sup.4 and R.sup.5 are identical or different and are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a heterocyclic radical and R.sup.6 and R.sup.7 are identical or different and are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl or arlkyl or R.sup.6 and R.sup.7, together with the carbon atom carrying them, are cycloalkyl. The novel compounds are prepared by a carbonyl olefination according to Wittig. They are intermediates for the preparation of pharmaceuticals, in particular of inhibitors of renin and HIV protease.

    摘要翻译： 本发明涉及下式化合物：其中R 1和R 2相同或不同并且是氢或芳烷基，R 3是烷基，环烷基或环烷基烷基，R 4和R 5是相同或不同的，是氢，烷基，环烷基，环烷基烷基 芳基，芳烷基或杂环基，R 6和R 7相同或不同，为氢，烷基，环烷基，环烷基烷基，芳基或芳烷基或R6和R7与携带它们的碳原子一起为环烷基。 根据Wittig，通过羰基烯化制备新化合物。 它们是用于制备药物的中间体，特别是肾素和HIV蛋白酶的抑制剂。