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    Benzothiazole derivatives, processes for their preparation and pharmaceutical compositions containing these compounds
    2.
    发明授权
    Benzothiazole derivatives, processes for their preparation and pharmaceutical compositions containing these compounds 失效
    苯并噻唑衍生物，其制备方法和含有这些化合物的药物组合物

    公开(公告)号：US4732986A

    公开(公告)日：1988-03-22

    申请号：US51214

    申请日：1987-05-12

    申请人： Kay Brune ,  Heidrun Engler ,  Istvan Szelenyi ,  Peter Morsdorf ,  Helmut Schickaneder ,  Kurt H. Ahrens

    发明人： Kay Brune ,  Heidrun Engler ,  Istvan Szelenyi ,  Peter Morsdorf ,  Helmut Schickaneder ,  Kurt H. Ahrens

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D277/82 ,  C12N9/99

    CPC分类号： C07D277/82

    摘要： Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.

    摘要翻译： 对应于通式I（I）的苯并噻唑衍生物，其中R 1，R 2，R 3和R 4彼此独立地表示氢原子，卤素原子，直链C 1 -C 3 - 烷基或直链C 1 -C 3 - C 3 - 烷氧基，R 5表示氢原子或直链C 1 -C 3 - 烷基，R 6表示氢原子，R 7表示甲酰基，式◎的烷氧基，其中，R 8表示直链或支链 或者它表示下式的酰基，其中R 9表示直链C 1 -C 3 - 烷基，或者R 6和R 7一起表示基团，其中R 10和R 11独立地表示 另一方面，氢原子或直链C 1 -C 6 - 烷基或R 6和R 7表示基团，其中R 12和R 13彼此独立地表示直链C 1 -C 3 - 烷基或直链C 1 -C 3 - 烷氧基或R6和R7表示基团，其中R14表示直链C1-C3-烷基，以及生理记录 描述了其可接受的盐，制备这些化合物的方法和含有它们的药物制剂。

    Indolyl-3-glyoxylic acid derivatives having antitumor action
    3.
    发明授权
    Indolyl-3-glyoxylic acid derivatives having antitumor action 失效
    具有抗肿瘤作用的吲哚基-3-乙醛酸衍生物

    公开(公告)号：US07579365B2

    公开(公告)日：2009-08-25

    申请号：US10309204

    申请日：2002-12-04

    申请人： Bernd Nickel ,  Istvan Szelenyi ,  Jürgen Schmidt ,  Peter Emig ,  Dietmar Reichert ,  Eckhard Günther ,  Kay Brune ,  Guillaume Le Baut

    发明人： Bernd Nickel ,  Istvan Szelenyi ,  Jürgen Schmidt ,  Peter Emig ,  Dietmar Reichert ,  Eckhard Günther ,  Kay Brune ,  Guillaume Le Baut

    IPC分类号： A61K31/44 ,  C07D401/00

    CPC分类号： A61K31/496 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  C07D209/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

    摘要翻译： 本发明涉及通式I的N-取代的吲哚-3-乙醛酰胺作为抗肿瘤剂和具有抗肿瘤作用的药物组合物的用途，其特征在于其含有至少一种通式1的化合物，如果 也适用于生理上可耐受的酸加成盐或N-氧化物的形式。 此外，本发明还包括抗肿瘤剂，其包含根据通式1的一种或多种N-取代的吲哚-3-乙醛酰胺作为活性化合物，以及如果合适的话，其生理上可耐受的酸加成盐，以及如果可能的话，N-氧化物和 片剂，包衣片剂，胶囊，输注溶液或安瓿，栓剂，贴剂，可通过吸入，悬浮液，霜剂和软膏使用的粉末制剂的药学上可用的载体和/或稀释剂或辅助物质。

    Indolyl-3-glyoxylic acid derivatives having antitumor action
    9.
    发明授权
    Indolyl-3-glyoxylic acid derivatives having antitumor action 有权
    具有抗肿瘤作用的吲哚基-3-乙醛酸衍生物

    公开(公告)号：US06232327B1

    公开(公告)日：2001-05-15

    申请号：US09285058

    申请日：1999-04-02

    申请人： Bernd Nickel ,  Istvan Szelenyi ,  Jürgen Schmidt ,  Peter Emig ,  Dietmar Reichert ,  Eckhard Günther ,  Kay Brune

    发明人： Bernd Nickel ,  Istvan Szelenyi ,  Jürgen Schmidt ,  Peter Emig ,  Dietmar Reichert ,  Eckhard Günther ,  Kay Brune

    IPC分类号： A61K31435

    CPC分类号： A61K31/496 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  C07D209/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

    摘要翻译： 本发明涉及通式I的N-取代吲哚-3-乙醛酰胺作为抗肿瘤剂，并且具有抗肿瘤作用的药物组合物的用途，其特征在于，如果适用，其含有至少一种通式1的化合物 还以生理上可耐受的酸加成盐或N-氧化物的形式。 此外，本发明还包括抗肿瘤剂，其包含根据通式1的一种或多种N-取代的吲哚-3-乙醛酰胺作为活性化合物，以及如果合适的话，其生理上可耐受的酸加成盐，以及如果可能的话，N-氧化物和 片剂，包衣片剂，胶囊，输注溶液或安瓿，栓剂，贴剂，可通过吸入，悬浮液，霜剂和软膏使用的粉末制剂的药学上可用的载体和/或稀释剂或辅助物质。