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    Substituted 2-amino-4-phenyldihydroquinolines, processes for their preparation, pharmaceutical compositions and methods for their use
    31.
    发明授权
    Substituted 2-amino-4-phenyldihydroquinolines, processes for their preparation, pharmaceutical compositions and methods for their use 有权
    取代的2-氨基-4-苯基二氢喹啉，其制备方法，药物组合物及其使用方法

    公开(公告)号：US08106204B2

    公开(公告)日：2012-01-31

    申请号：US12212294

    申请日：2008-09-17

    申请人： Hans-Jochen Lang ,  John Weston ,  Uwe Heinelt

    发明人： Hans-Jochen Lang ,  John Weston ,  Uwe Heinelt

    IPC分类号： C07D215/04

    CPC分类号： C07D215/38

    摘要： The invention relates to NHE-3 inhibitor compounds of formula I: In which R1-R11 are more specifically defined herein. These substituted 2-amino-4-phenyl-dihydroquinolines are useful the treatment of various renal and respiratory disorders such as acute or chronic renal failure, for impairments of biliary function and respiratory impairments such as snoring, sleep apneas or stroke. Formulations comprising them and methods for their use are also described herein.

    摘要翻译： 本发明涉及式I的NHE-3抑制剂化合物：其中R1-R11在本文中更具体地定义。 这些取代的2-氨基-4-苯基 - 二氢喹啉可用于治疗各种肾脏和呼吸系统疾病如急性或慢性肾衰竭，胆汁功能障碍和呼吸障碍如打鼾，睡眠呼吸暂停或中风。 本文还描述了包含它们的制剂及其使用方法。

    Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them
    38.
    发明授权
    Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them 有权
    取代的4-苯基四氢异喹啉鎓，其制备方法，它们作为药物的用途，以及含有它们的药物

    公开(公告)号：US06911453B2

    公开(公告)日：2005-06-28

    申请号：US10309352

    申请日：2002-12-04

    申请人： Armin Hofmeister ,  Uwe Heinelt ,  Hans-Jochen Lang ,  Markus Bleich ,  Klaus Wirth ,  Michael Gekle

    发明人： Armin Hofmeister ,  Uwe Heinelt ,  Hans-Jochen Lang ,  Markus Bleich ,  Klaus Wirth ,  Michael Gekle

    IPC分类号： C07D217/18 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D217/00 ,  A61K31/47

    CPC分类号： C07D401/12 ,  C07D217/18 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： The invention relates to compounds of the formula I in which R1 to R9 are as defined herein. In one embodiment, these compounds may be used as antihypertensives, for reducing or preventing ischemia-induced damage, as medicaments for surgical intervention for the treatment of ischemias of the nervous system, of stroke and of cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxative, as agent against ectoparasites, to prevent the formation of gallstones, as antiatherosclerotics, agents against late complications of diabetes, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophies and hyperplasias. In one embodiment, the compounds may be inhibitors of the cellular sodium-proton antiporter and influence serum lipoproteins and thus be used for the prophylaxis and for the regression of atherosclerotic lesions.

    摘要翻译： 本发明涉及其中R 1至R 9如本文所定义的式I化合物。 在一个实施方案中，这些化合物可以用作抗高血压药物，用于减少或预防缺血诱发的损伤，作为用于治疗神经系统缺血性卒中和脑水肿的外科手术的药物，休克，受损的呼吸驱动 用于治疗打鼾，作为缓泻剂，作为对外寄生虫剂的药剂，以防止胆结石的形成，作为抗动脉粥样硬化剂，用于治疗糖尿病晚期并发症的药物，癌症，纤维化病症，内皮功能障碍，器官肥厚和增生。 在一个实施方案中，化合物可以是细胞钠 - 质子逆转录酶的抑制剂并影响血清脂蛋白，因此用于预防动脉粥样硬化病变的消退。

    Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them
    40.
    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。