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    Diorthosubstituted benzene derivatives, especially for use in a method of therapy, processes for their preparation, and pharmaceutical compositions containing them
    1.
    发明公开
    Diorthosubstituted benzene derivatives, especially for use in a method of therapy, processes for their preparation, and pharmaceutical compositions containing them 失效
    二邻取代的苯衍生物，特别是用于治疗性治疗，以及含有它们的药物组合物的方法中使用。

    公开(公告)号：EP0000826A1

    公开(公告)日：1979-02-21

    申请号：EP78300227.2

    申请日：1978-08-01

    申请人： Kabi AB

    发明人： Joensson, Aake Nils ,  Merenyi, Ferenc ,  Moses, Pinchas ,  Karlsson, Lennart Olof ,  Hanshoff, Gunnar

    IPC分类号： C07C143/74 ,  C07C143/78 ,  C07C143/80 ,  C07C149/453 ,  A61K31/18 ,  A61K31/63

    CPC分类号： C07D209/48 ,  C07C309/00

    摘要： New compounds of the general formula I
    wherein R' and R 2 each independently represent an alkyl group containing 1 to 4 carbon atoms, or an alkoxy group containing 1 to 3 carbon atoms, or halogen, R' represents hydrogen, halogen, an alkyl group containing 1 to 4 carbon atoms, an alkoxv group containing 1 to 3 carbon atoms, an amino group or a nitro group, A represents
    which is bonded to the benzene ring by its sulphu r or nitrogen atom and in which R' is hydrogen or an alkyl group containing to 4 carbon atoms; together with salts thereof with I physiologically acceptable acids and, when R' is hydrogen, with physiologically acceptable bases are described. The compounds are of use in inhibiting thrombosis formation, in treating thrombosis and in fibronolytic therapy. Various methods of producing the new compound are described involving the building up of the -A-CH 2 -CH 2 -S-CH 2 CH 2 -NH 2 side chain from aromatic precursors having an imcomplete side chain or by introducing at least one of R 1 , R or R'substituents into a precursor lacking that substituent or from an amino-protected precursor.

    Geminally disubstituted indene derivatives, processes for their preparation and pharmaceutical compositions containing them
    3.
    发明公开
    Geminally disubstituted indene derivatives, processes for their preparation and pharmaceutical compositions containing them 失效
    偕二取代的茚衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0000825A1

    公开(公告)日：1979-02-21

    申请号：EP78300226.4

    申请日：1978-08-01

    申请人： Kabi AB

    发明人： Joensson, Aake Nils ,  Kempe, Tomas Goeran ,  Mikiver, Lembit ,  Sparf, Bengt Aake

    IPC分类号： C07C91/23 ,  C07C93/14 ,  C07C135/02 ,  A61K31/135 ,  C07D295/08

    CPC分类号： C07D295/084 ,  C07C17/10 ,  C07C47/453 ,  C07C215/38 ,  C07C215/40 ,  C07C217/74 ,  C07C291/02 ,  C07C2602/08 ,  C07C2603/94 ,  C07C23/34

    摘要： New geminally disubstituted indenet are of general formula I
    wherein each of R 1 and R 2 is hydrogen or R 1 and R 2 together form a direct bond or an alkylene group -(CH 2 )n-, in which n is an integer from 1 to 4,R 3 is hydrogen, C1-3-alkoxy or halogen, and each of R 4 and R 5 is hydrogen or C1-4-loweralkyl, or R 4 and R 5 togetherform an alkylene group-(CH 2 )m-, in which m is an integer from 3 to 6; and the corresponding amine oxides, quaternary ammonium compounds and salts with physiotog- ically acceptable acids.
    The indenes find use in treating incontinence, as a mucous membrane decongestant, as a blood pressure reducing agent, as a vasoconstrictor or as an antireserpine agent.
    The indenes may be prepared by process known per se.

    摘要翻译： 新偕二取代的茚为通式I （I）worin每个R1和R2是氢或R 1和R 2一起形成直接键或在亚烷基基团 - （CH 2）N，其中n是从整数 为1〜4，R 3是氢，C 1-3烷氧基或卤素，以及每个R 4和R 5的是氢或C1-4的低级烷基，或R4和R5在亚烷基基团一起形成 - （CH 2）米，其中 m为3至6的整数; 和胺氧化物CORRESPONDING，季铵化合物及其盐与生理上可接受的酸。 的茚可用于治疗失禁使用，作为粘膜减充血剂，作为降血压剂，或vasocostrictor以抗利血平剂。 的茚可通过借助于在侧链不完整或式I化合物的前体茚本身已知的方法中涉及的（a）synthesing侧链CH（OH）CH2NR4R5本身已知的方法来制备（b）中 引入双键引入在其中双键不存在或（c）释放的末端氨基在其中末端氨基是受保护的式I化合物的前体的式I化合物的茚满基前体。