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286 条记录 (耗时 0.015 秒)

    Aminoguanidines
    41.
    发明公开
    Aminoguanidines 失效
    氨基胍。

    公开(公告)号：EP0505322A1

    公开(公告)日：1992-09-23

    申请号：EP92810191.4

    申请日：1992-03-17

    申请人： SANDOZ LTD. ,  SANDOZ-PATENT-GMBH ,  SANDOZ ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.

    发明人： Giger, Rudolf Karl Andreas ,  Mattes, Henri

    IPC分类号： C07D209/14 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

    CPC分类号： C07D403/12 ,  C07D209/14 ,  C07D333/58 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07F7/0814 ,  C07F9/5728

    摘要： Compounds of formula

            A-X--Y-NH-B


    wherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alcoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X---Y is -CR₈=N- or CH(R₈)-NH- wherein R₈ is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue

    wherein R₁₀ is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X₂ is alkylthio or NR₃R₁₀ wherein R₃ is H or alkyl or R₃ and R₁₀ together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.

    摘要翻译： 式AX-Y-NH-B的化合物，其中A衍生自任选取代的苯并噻吩，吲哚，4-氮杂 - 和7-氮杂 - 苯并噻吩或 - 吲哚，A在5位氢，卤素，任选取代的烷基，羟基 硝基，氨基，烷基氨基，酰氨基，烷氧基羰基，氨磺酰基，氰基，三甲基甲硅烷基，羧基，氨基甲酰基，磷酸酯，氧基氨基甲酰基，杂环基或醚或酯基，X --- Y是-CR8 = N-或CH（R8） - NH-，其中R8是-H或烷基并且连接在A的3位，B是杂环基团或残基，其中R10是H，任选取代的烷基，环烷基，芳基，金刚烷基，酰基或氨基甲酰基，X 2是 烷硫基或NR 3 R 10，其中R 3为H或烷基或R 3和R 10与它们所连接的氮原子一起形成游离形式或盐形式的杂环基，具有药理活性，例如 用于治疗胃肠道疾病。

    Benzo[b]thiophene-containing lipoxygenase-inhibiting compounds
    45.
    发明公开
    Benzo[b]thiophene-containing lipoxygenase-inhibiting compounds 失效
    吲哚，苯并呋喃和含苯并二氢ING ING SE SE SE TING TING TING TING

    公开(公告)号：EP0416609A3

    公开(公告)日：1992-01-02

    申请号：EP90117171.0

    申请日：1990-09-06

    申请人： ABBOTT LABORATORIES

    发明人： Brooks, Dee W. ,  Summers, James B.

    IPC分类号： C07D333/58 ,  A61K31/38

    CPC分类号： C07D307/81 ,  C07D209/14 ,  C07D333/58

    摘要： Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula
    in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R¹ is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R¹ must bear a metabolically cleavable leaving group.

    Benzo[b]thiophene-containing lipoxygenase-inhibiting compounds
    46.
    发明公开
    Benzo[b]thiophene-containing lipoxygenase-inhibiting compounds 失效
    Indol，Benzofuran und Benzothiophen enthaltende lipoxygenaseinhibierende Verbindungen。

    公开(公告)号：EP0416609A2

    公开(公告)日：1991-03-13

    申请号：EP90117171.0

    申请日：1990-09-06

    申请人： ABBOTT LABORATORIES

    发明人： Brooks, Dee W. ,  Summers, James B.

    IPC分类号： C07D333/58 ,  A61K31/38

    CPC分类号： C07D307/81 ,  C07D209/14 ,  C07D333/58

    摘要： Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula
    in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R¹ is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R¹ must bear a metabolically cleavable leaving group.

    摘要翻译： 有效的5-脂氧合酶抑制化合物的前药包括其中A为亚烷基或亚烯基的式CHEM的化合物，X为氧，硫，亚砜基或取代的氮，Y为包括取代或未取代的基团 碳环或取代或未取代的杂环芳基。 R 1是烷基，烯基，氨基，烷基氨基，二烷基氨基或羟基氨基或具有代谢可切割离去基团的胺基。 M是氢，药学上可接受的阳离子或代谢可切割的离去基团，条件是M或R 1必须具有代谢可切割的离去基团。