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    Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them
    1.
    发明授权
    Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them 失效
    取代的降冰片基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物

    公开(公告)号：US06825231B2

    公开(公告)日：2004-11-30

    申请号：US09734008

    申请日：2000-12-12

    申请人： Uwe Heinelt ,  Hans-Jochen Lang ,  Heinz-Werner Kleemann ,  Jan-Robert Schwark ,  Klaus Wirth ,  Hans-Willi Jansen

    发明人： Uwe Heinelt ,  Hans-Jochen Lang ,  Heinz-Werner Kleemann ,  Jan-Robert Schwark ,  Klaus Wirth ,  Hans-Willi Jansen

    IPC分类号： A61K31335

    CPC分类号： C07C317/32 ,  C07B2200/07 ,  C07C211/38 ,  C07C211/49 ,  C07C215/30 ,  C07C217/58 ,  C07C217/60 ,  C07C217/62 ,  C07C229/38 ,  C07C237/30 ,  C07C255/58 ,  C07C257/18 ,  C07C311/37 ,  C07C323/32 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/68

    摘要： The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endothelial dysfunction, and organ hypertrophies and hyperplasias. They are inhibitors of the cellular sodium/proton antiporter. They have an influence on serum lipoproteins and can therefore be used for the prophylaxis and regression of atherosclerotic changes.

    摘要翻译： 本申请公开了取代的降冰片烷基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物具有外部构型的氮的取代的降冰片烷基氨基衍生物和式I的内部稠合的五元环，或具有外部配置的氮 和R 1，R 2，R 3，R 4，R 5，A，B，S 1和S 2如权利要求中所定义的式I ain的外部稠合的五元环非常适合用作抗高血压剂，用于 减少或预防缺血性损伤，用作外科手术治疗神经系统缺血，中风和脑水肿，休克，呼吸驱动受损，用于治疗打鼾的药物，作为泻药，作为药物 外寄生虫，用于预防胆汁结石的形成，作为抗动脉粥样硬化，作为晚期糖尿病并发症的药剂，癌性疾病，纤维化疾病，en 上皮功能障碍，器官肥厚和增生。它们是细胞钠/质子逆转录酶的抑制剂。 它们对血清脂蛋白有影响，因此可用于预防和消除动脉粥样硬化变化。

    Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them
    4.
    发明授权
    Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them 失效
    取代的杂环降冰片基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物

    公开(公告)号：US06737423B2

    公开(公告)日：2004-05-18

    申请号：US10020241

    申请日：2001-12-18

    申请人： Uwe Heinelt ,  Hans-Jochen Lang ,  Klaus Wirth ,  Hans-Willi Jansen

    发明人： Uwe Heinelt ,  Hans-Jochen Lang ,  Klaus Wirth ,  Hans-Willi Jansen

    IPC分类号： C07D21338

    CPC分类号： C07D207/335 ,  C07D213/38 ,  C07D231/12 ,  C07D231/16 ,  C07D233/56 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D261/18 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D333/44

    摘要： Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia. The compounds of the invention are inhibitors of the cellular sodium-proton antiporter. Additonally, the compounds of the invention influence the serum lipoproteins and can therefore be used for the prophylaxis and the regression of atherosclerotic changes.

    摘要翻译： 取代的杂环降冰片基氨基衍生物具有：a）外配构型氮和式（I）的内联稠合五元环或六元环，或b）外配构氮和外稠合五元环 或式（Ⅰa）的六元环，其中Rn，Het，A，B和T具有权利要求中给出的含义。 这些化合物具有多种用途。 它们可用作抗高血压药物，用于减少或预防化学诱导的损伤，作为手术干预的药物，用于治疗神经系统缺血，包括中风和脑水肿，用于治疗由于休克和受干扰的局部缺血 呼吸驱动，用作治疗打鼾，作为泻药，作为对外寄生虫的药物，用于预防胆结石形成，作为抗动脉粥样硬化，作为抗糖尿病晚期并发症，癌症，纤维化病症，内皮功能障碍，器官肥大的药剂，以及 器官增生。本发明的化合物是细胞钠 - 质子逆转录酶的抑制剂。 此外，本发明的化合物影响血清脂蛋白，因此可用于预防和消除动脉粥样硬化变化。