Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them
    44.
    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

    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 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use
    50.
    发明授权
    Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use 有权
    取代的4-苯基四氢异喹啉,其药物组合物,其制备方法和治疗用途

    公开(公告)号:US07790742B2

    公开(公告)日:2010-09-07

    申请号:US11680668

    申请日:2007-03-01

    IPC分类号: C07D217/00 A61K31/47

    摘要: The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines, derivatives thereof and compositions containing them formulated in combination with other compounds which also regulate the intracellular pH environment such as inhibitors of carbonic anhydrase and inhibitors of the transport systems that carry bicarbonate ions, such as of the sodium-bicarbonate co-transporter (NBC) or the sodium-dependent chloride-bicarbonate exchanger.

    摘要翻译: 本发明涉及式I结构的取代的4-苯基四氢异喹啉化合物和包含它们的药物组合物,其中本文定义了R基团。 这些是钠 - 氢交换器(NHE),特别是亚型3(NHE3)的钠 - 氢交换器的优异抑制剂。 因此,这些化合物可用于治疗肾脏和呼吸系统的各种疾病,例如急性或慢性肾衰竭,肺并发症,胆汁功能障碍,呼吸系统疾病如打鼾或睡眠呼吸暂停和心血管/中枢神经系统疾病,例如 行程。 更具体地,本发明涉及取代的4-苯基 - 四氢异喹啉,其衍生物和含有它们的组合物,其与调节细胞内pH环境的其它化合物配制,例如碳酸酐酶抑制剂和携带碳酸氢根离子的运输系统的抑制剂 ,例如碳酸氢钠共转运体(NBC)或钠依赖性氯化碳 - 碳酸氢盐交换剂。