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51 条记录 (耗时 0.025 秒)

    Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides
    2.
    发明授权
    Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides 失效
    取代的3-（正 - 杂环）-2,6-二氨基吡啶和 - 氧化物

    公开(公告)号：US4923858A

    公开(公告)日：1990-05-08

    申请号：US352287

    申请日：1989-05-16

    申请人： Jurgen Engel ,  Peter Emig ,  Bernd Nickel ,  Istvan Szelenyi

    发明人： Jurgen Engel ,  Peter Emig ,  Bernd Nickel ,  Istvan Szelenyi

    IPC分类号： A61K31/44 ,  A61K31/535 ,  A61P25/04 ,  A61P25/08 ,  A61P29/00 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D401/04 ,  C07D413/04 ,  C07D417/04

    摘要： Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.6 -alkylphenyl or trifluoromethylphenyl, their pyridine-N-oxides and physiologically acceptable salts thereof, processes for their preparation and medicines containing such compounds as active ingredients.

    摘要翻译： 通式为：其中基团R 1和R 2相同或不同并且表示氢或C 1 -C 6烷基的通式为：其中R 3和R 4相同或不同，表示氢，C 1 -C 6 - 烷基 ，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，卤素或C 2 -C 6 - 烷酰基，X是氧，硫或基团-NR 5和R 5是氢，C 1 -C 6烷基，C 2 -C 6 - 烷酰基或 苯甲酰基，m和n各自可以表示整数1,2或3，苯基A未取代或被卤素，硝基，C 1 -C 6 - 烷基，三氟甲基，C 3 -C 7 - 环烷基，羟基，C 1 -C 6 - C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6 - 烷基氨基，C 2 -C 6 - 烷酰基氨基，CN，羧基，C 1 -C 6 - 烷氧基羰基，苯基，C 1 -C 6烷基苯基或 三氟甲基苯基，它们的吡啶-N-氧化物及其生理学上可接受的盐，其制备方法和含有活性成分的化合物的药物。

    Indolyl-3-glyoxylic acid derivatives having antitumor action
    5.
    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
    7.
    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。

    Nitrogen-containing cyclo-aliphatic compounds having an amino radical and a pyridine radical
    8.
    发明授权
    Nitrogen-containing cyclo-aliphatic compounds having an amino radical and a pyridine radical 失效
    含氨基和吡啶基的含氮环脂族化合物

    公开(公告)号：US4946836A

    公开(公告)日：1990-08-07

    申请号：US399439

    申请日：1989-08-28

    申请人： Jurgen Engel ,  Axel Kleemann ,  Bernd Nickel ,  Istvan Szelenyi

    发明人： Jurgen Engel ,  Axel Kleemann ,  Bernd Nickel ,  Istvan Szelenyi

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P25/04 ,  C07D401/12 ,  C07D401/14

    CPC分类号： C07D401/12

    摘要： Compounds of formula ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen, halogen atoms, a trifluoromethyl group, a cyano, a nitro group, an amino group, a mono-C.sub.1 -C.sub.6 -alkylamino group, a di-C.sub.1 -C.sub.6 -alkylamino group, an amino group that is substituted by a phenyl C.sub.1 -C.sub.4 -alkyl radical, a C.sub.2 -C.sub.6 -alkanoyl-amino group, a C.sub.1 -C.sub.6 -alkoxycarbonyl amino group, a C.sub.1 -C.sub.6 -alkyl group optionally substituted by a phenyl radical, a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group, a phenoxy group or represent a carbamoyl group optionally substituted by one or two C.sub.1 -C.sub.6 -alkyl groups and the radical A is an acyl group which is derived from an amino acid as well as processes for their preparation.

    摘要翻译： 其中基团R 1和R 2相同或不同并表示氢，卤原子，三氟甲基，氰基，硝基，氨基，单C 1 -C 6 - 烷基氨基， 二C1-C6烷基氨基，被苯基C1-C4-烷基取代的氨基，C2-C6-烷酰基 - 氨基，C1-C6-烷氧基羰基氨基，C1-C6-烷基 任选被苯基，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，苯氧基取代的基团，或表示任选被一个或两个C 1 -C 6 - 烷基取代的氨基甲酰基， 基团A是衍生自氨基酸的酰基以及它们的制备方法。