The use of 2- phenylmethylene -1- 3'-(amino)-2'-(hydroxy)--propoxy-imino -cyclohexane derivatives
    2.
    发明公开
    The use of 2- phenylmethylene -1- 3'-(amino)-2'-(hydroxy)--propoxy-imino -cyclohexane derivatives 失效
    Die Verwendung von 2-苯基亚甲基-1,3' - (氨基)-2-(羟基) - 丙氧基 - 亚氨基 - 环己烷 - 衍生物。

    公开(公告)号:EP0636368A1

    公开(公告)日:1995-02-01

    申请号:EP94111107.2

    申请日:1994-07-18

    IPC分类号: A61K31/15 A61K31/495

    CPC分类号: A61K31/15 A61K31/495

    摘要: The subject-matter of the invention is the use of 2-[phenylmethylene]-1-[3'-(amino)-2'-(hydroxy)-propoxy-imino]-cyclohexane derviates of formula

    wherein

    R and R₁ independently mean hydrogen or halogen atom(s),
    R o stands for hydrogen or a C₁₋₄ alkoxy group,
    R₂ and R₃ independently represent hydrogen atom(s), straight and/or branched chain C₁₋₈ alkyl group(s), optionally substituted by a dimethylamino group, or C₂₋₆ alkenyl or C₃₋₇ cycloalkyl group(s) or
    R₂ and R₃ together with the nitrogen atom to which they are attached form a 6-membered heterocyclic group containing an additional nitrogen atom, which latter optionally may bear a phenyl group, optionally substituted by a C₁₋₄ alkoxy group,
    and their stereoisomers and optical isomers and mixtures thereof as well as pharmaceutically acceptable acid addition salts and quaternary ammonium derivatives thereof, optionally in admixture with 1 or more carrier(s) commonly used in pharmaceutical compositions, for preparing medicaments having gastroprotective and antimicrobial including antiulcer activity.

    摘要翻译: 本发明的主题是使用式CHEM的2- [苯基亚甲基] -1- [3' - (氨基)-2' - (羟基) - 丙氧基 - 亚氨基] - 环己烷衍生物,其中R和R 1 独立地表示氢或卤素原子,Ro表示氢或C1-4烷氧基,R2和R3独立地表示氢原子,直链和/或支链C1-8烷基,任选取代的 二甲基氨基或C 2-6烯基或C 3-7环烷基或R 2和R 3与它们所连接的氮原子一起形成含有另外的氮原子的6元杂环基,后者任选地可以 承担任选被C 1-4烷氧基取代的苯基及其立体异构体和旋光异构体及其混合物,以及其药学上可接受的酸加成盐和季铵衍生物,任选与1种或多种载体混合 用于药物组合物,用于制备药物 胃肠保护和抗微生物剂,包括抗溃疡活性。

    Oxaindene derivatives and a process for preparing them as well as medicaments containing them and the use of them
    3.
    发明公开
    Oxaindene derivatives and a process for preparing them as well as medicaments containing them and the use of them 失效
    Oxaindene衍生物,制备方法,其用途和含有它们的药物

    公开(公告)号:EP0751137A1

    公开(公告)日:1997-01-02

    申请号:EP96110220.9

    申请日:1996-06-25

    CPC分类号: C07D307/91 C07D307/93

    摘要: A subject-matter of the invention are oxaindene derivatives of general formula
    wherein

    R 1 represents a C 1-4 -alkyl, C 1-4 -alkoxy or C 3-6 -cycloalkyl group,
    R 2 stands for hydrogen or a C 1-4 -alkyl or C 3-6 -cycloalkyl group,
    R 3 represents hydrogen or a C 1-4 -alkyl, C 1-4 -alkoxy or benzyloxy group,
    X means hydrogen, an aliphatic C 1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C 1-4 -alkoxy group(s) or a group of formula
    in which latter
    R 7 stands for a C 1-4 -alkylene group
       and
    R 5 and R 6 each represents a C 1-4 -alkyl group
       or
    R 5 and R 6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group,
    A and B together form an ethylene or a vinylene group
       and
    n is 1, 2 or 3,
    and their stereoisomers and their mixtures as well as acid addition salts of these compounds.
    Moreover there are provided for a process for preparing these compounds, medicaments containing them and the use of these compounds.
    They have a strong 5-lipoxygenase enzyme inhibiting activity.

    摘要翻译: 本发明的主题是通式 worin R1 darstellt一个C 1-4烷基的oxaindene衍生物,C 1-4烷氧基或C 3-6环烷基,R2代表氢或C 1-4烷基 或C 3-6 - 环烷基,R 3 darstellt氢或C 1-4 - 烷基,C 1-4 - 烷氧基或苄氧基,X表示氢在脂肪族C 1-4酰基或苯甲酰基或萘基,任选被1或取代 多个硝基或C 1-4烷氧基(一个或多个)或下式基团的在后一种R7代表一个C 1-4的亚烷基基团和R 5和R 6各自darstellt C 1-4烷基或R5和R6 一起与氮原子到它们所连接形成哌啶基或吗啉基,A和B一起形成亚乙基或亚乙烯基的和n是1,2或3,和其立体异构体和它们的混合物以及将酸加成盐 合成化合物。 更上方设置有用于制备合成的化合物,药物含有它们和使用合成的化合物的方法。 他们有强烈的5-脂氧合酶抑制活性。

    1-(Phenyl)-3-[omega-(amino)-alkoxyimino]-alk-1-ene derivatives, a process for preparing them as well as medicaments containing them and the use of them
    6.
    发明公开
    1-(Phenyl)-3-[omega-(amino)-alkoxyimino]-alk-1-ene derivatives, a process for preparing them as well as medicaments containing them and the use of them 失效
    1-(苯基)-3-Ω - (氨基)-alkoxyimino-ALK -1-烯衍生物,它们的制备方法和含有它们和它们的药物使用。

    公开(公告)号:EP0619299A2

    公开(公告)日:1994-10-12

    申请号:EP94105517.0

    申请日:1994-04-11

    摘要: A subject-matter of the invention are 1-(Phenyl)-3-[ω-(amino)-alkoxyimino]-alk-1-ene derivatives of general formula

    wherein

    R₁ and R₂ independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group or together represent a 3,4-methylenedioxy group,
    R stands for C₁₋₈ alkyl,
    R₃ represents hydrogen, C₁₋₄ alkyl or hydroxy,
    R₄ and R₅ independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl or C₃₋₆ cycloalkyl group,
    óóóor
    R₄ and R₅ together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent
    óóóand
    A represents a valency bond or a -CH₂-group,
    as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof.
    Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting and anxiolytic effects.

    摘要翻译: 本发明的主题是1-(苯基)-3- [Ω - (氨基)烷氧基亚氨基]通式 worin R1和R2的链-1-烯衍生物unabhängig各自表示氢,卤素或 C1-4烷氧基或一起代表3,4-亚甲二氧基,R代表C1-8烷基,R3 darstellt氢,C 1-4烷基或羟基,R4和R5各自独立地darstellt氢,C 1-12烷基 ,任选被羟基substituiertem,或C 2-12烯基或C 3-6环烷基,或R4和R5一起与氮原子到它们所连接形成4-至7-元杂环,其任选地包含氧,硫的 或氮原子。此外,后一种可任选地携带一个苯基,苄基或C 1-4烷基取代基,A表示一个价键或-CH 2基团,以及立体声和旋光异构体和它们的混合物,酸加成盐 它们的和季铵衍生物。 进一步,本发明涉及有用于制备合成化合物以及含有它们的药物和用于制备药物的用途其中,特别是具有ulcus和胃酸分泌抑制作用和抗焦虑作用的方法。

    The use of( a) bicycloheptane derivative(s)
    8.
    发明公开
    The use of( a) bicycloheptane derivative(s) 失效
    Verwendung vom einem Bicycloheptan-Derivat

    公开(公告)号:EP0694299A1

    公开(公告)日:1996-01-31

    申请号:EP95110311.8

    申请日:1995-07-03

    IPC分类号: A61K31/135

    CPC分类号: A61K31/135

    摘要: The subject matter of the invention is the use of [a] bicycloheptane derivative(s) of formula

    wherein

    R represents a phenyl or a benzyl group,
    R₁ and R₂ , which may be the same or different stand for straight or branched chained alkyl groups or one of R₁ and R₂ is hydrogen and the other is a straight or branched chained alkyl group,
    A denotes a straight or branched chained alkylene group and
    ∼ represents a valence bond,
    and [an] N-oxide(s) as well as [an] optical isomer(s) thereof and mixtures of the optical isomers and [an] acid addition salt(s) and quaternary ammonium derivative(s) of the bicycloheptane derivatives of formula I as well as [an] optical isomer(s) thereof and mixtures of the optical isomers for preparing medicaments for the treatment of diseases and disorders which are connected with the influence on the peripheral cholecystokinin (CCK) system.

    摘要翻译: 本发明的主题是使用式CHEM的二环庚烷衍生物,其中R表示苯基或苄基,R 1和R 2可以相同或不同,代表直链或支链链烷基 或者R 1和R 2中的一个是氢,另一个是直链或支链链烷基,A表示直链或支链链亚烷基,而SIMALAR表示价键,并且ÄnN-氧化物以及Äan光学异构体 和与式I的双环庚烷衍生物的光学异构体和Äanü酸加成盐和季铵衍生物的混合物以及其旋光异构体和用于制备的光学异构体的混合物 用于治疗与周围胆囊收缩素(CCK)系统的影响相关的疾病和病症的药物。