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63 条记录 (耗时 0.037 秒)

    Optically active bicyclic imino-alpha-carboxylic esters
    46.
    发明授权
    Optically active bicyclic imino-alpha-carboxylic esters 失效
    光学活性双环亚氨基-α-羧酸酯

    公开(公告)号：US4822894A

    公开(公告)日：1989-04-18

    申请号：US23277

    申请日：1987-03-09

    申请人： Rolf Geiger ,  Volker Teetz ,  Dietrich Langner ,  Hansjorg Urbach ,  Rainer Henning

    发明人： Rolf Geiger ,  Volker Teetz ,  Dietrich Langner ,  Hansjorg Urbach ,  Rainer Henning

    IPC分类号： A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/54 ,  C07K1/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K14/81

    CPC分类号： C07C255/00 ,  C07D209/42 ,  C07D209/52 ,  C07D209/54 ,  C07K5/0222 ,  C07K5/06026 ,  C07K5/06078

    摘要： The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic esters into the components by crystallization of diastereomeric salts, which comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-amino carboxylic acids which contain a phenyl nucleus, recrystallizing them from an organic solvent, decomposing the precipitated, optically homogeneous diastereomeric salts in a manner known per se, and isolating the enantiomers and, where appropriate, converting the latter into the free acids by hydrolysis in a manner known per se. The invention also relates to optically pure compounds of the formula ##STR1## and to diastereomeric salts of these compounds, in which two of the radicals A, B.sup.1, B.sup.2 and C form a carbon chain and the others denote hydrogen, and R is an esterifying group.

    摘要翻译： 本发明涉及一种通过非对映体盐结晶将双环亚氨基-α-羧酸酯的外消旋混合物分解成组分的方法，其包括用光学活性N-酰化的R-或S-氨基羧酸制备外消旋酯的盐 其包含苯基核，从有机溶剂中重结晶它们，以本身已知的方式分解沉淀的，光学上均匀的非对映异构体盐，并分离对映异构体，并且在适当情况下以已知的方式通过水解将其转化为游离酸 本身。 本发明还涉及式“IMAGE”的光学纯化合物和这些化合物的非对映体盐，其中基团A，B 1，B 2和C 2中的两个形成碳链，而其它基团表示氢，R是酯化反应 组。

    Derivatives of cis, endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid, and their use for treating hypertension
    47.
    发明授权
    Derivatives of cis, endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid, and their use for treating hypertension 失效
    顺式，内-2-氮杂双环[5.3.0]癸烷-3-羧酸的衍生物及其用于治疗高血压的用途

    公开(公告)号：US4714708A

    公开(公告)日：1987-12-22

    申请号：US561230

    申请日：1983-12-14

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

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

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K38/00 ,  A61P9/12 ,  A61P43/00 ,  C07D209/52 ,  C07K1/113 ,  C07K5/02 ,  C07K14/81 ,  C07D209/02

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

    摘要： The invention relates to derivatives of cis,endo-2-azabicyclo[5.3.0]decane-3-carboxylic acid of the formula I ##STR1## in which R denotes hydrogen, alkyl, alkenyl or aralkyl, R.sup.1 denotes hydrogen, allyl, vinyl or a side chain of an optionally protected naturally occurring .alpha.-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 substituted once, twice or three times by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, and their physiologically acceptable salts, a process for their preparation, agents containing them and their use.

    摘要翻译： 本发明涉及式I（I）的顺式，内-2-氮杂双环[5.3.0]癸烷-3-羧酸衍生物，其中R表示氢，烷基，烯基或芳烷基，R1表示氢， 烯丙基，乙烯基或任选保护的天然α-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 烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲基二氧基取代一次，两次或三次的芳基，或表示吲哚-3-基，及其生理上可接受的盐， 他们的准备，包含他们的代理和他们的使用。

    Spirocyclic aminoacid derivatives, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and processes for their preparation
    49.
    发明授权
    Spirocyclic aminoacid derivatives, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and processes for their preparation 失效
    螺环氨基酸衍生物，其制备方法，含有它们的药剂及其用途和新的螺环氨基酸作为中间体及其制备方法

    公开(公告)号：US4620012A

    公开(公告)日：1986-10-28

    申请号：US569758

    申请日：1984-01-10

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

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

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/96 ,  C07D317/28 ,  C07D317/30 ,  C07D317/32 ,  C07D317/72 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K14/81 ,  C07C103/52 ,  A61K37/02

    CPC分类号： C07K5/0222 ,  C07D209/96 ,  C07D317/28 ,  C07D317/30 ,  A61K38/00

    摘要： The invention relates to new spirocyclic aminoacid derivatives of the formula I ##STR1## in which m denotes 1 or 2, n denotes 0 or 1, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl which can be optionally 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, arylalkyl or aroylalkyl, both of which can be substituted as defined above in the aryl radical, an S- or O- and/or N-heterocyclic radical or a side chain of an .alpha.-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 and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and a process for their preparation.

    摘要翻译： 本发明涉及式I（I）的新的螺环氨基酸衍生物，其中m表示1或2，n表示0或1，R表示氢，烷基或芳烷基，R1表示氢或可任意取代的烷基 芳基或部分氢化的芳基，其中每一个可以被烷基，烷氧基或卤素取代，芳基烷基或芳酰基烷基，它们都可以如上所述被取代，在芳基 基团，S-或O-和/或N-杂环基团或α-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在一起 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，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， 准备工作 包含它们及其用途和新的螺环氨基酸作为中间体及其制备方法。