SUBSTITUTED 1-AMINO-4-PHENYL-DIHYDROISOQUINOLINES, METHODS FOR THE PRODUCTION THEREOF, USE THEREOF AS A MEDICAMENT, AND MEDICAMENTS CONTAINING THEM
    4.
    发明申请
    SUBSTITUTED 1-AMINO-4-PHENYL-DIHYDROISOQUINOLINES, METHODS FOR THE PRODUCTION THEREOF, USE THEREOF AS A MEDICAMENT, AND MEDICAMENTS CONTAINING THEM 有权
    取代的1-氨基-4-苯基 - 二氢喹啉,其生产方法,作为药物使用,以及含有它们的药物

    公开(公告)号:US20090118327A1

    公开(公告)日:2009-05-07

    申请号:US12212301

    申请日:2008-09-17

    CPC分类号: C07D217/22 C07D401/10

    摘要: The present invention relates to compounds useful in the prevention or treatment of various disorders such as acute or chronic renal failure, for impairments of biliary function, for respiratory impairments such as snoring or sleep apneas or for stroke, and pharmaceutical compositions comprising them. More specifically, the compounds of the present invention comprises substituted 1-amino-4-phenyl-dihydroisoquinolines and their derivatives of formula I: Wherein the substituents R1-R11 are more specifically defined hereinbelow. The claimed compounds of the present invention also include their pharmaceutically acceptable salts and trifluoroacetates thereof as well as methods for their preparation and pharmaceutical delivery systems thereof.

    摘要翻译: 本发明涉及可用于预防或治疗诸如急性或慢性肾衰竭,胆汁功能障碍,呼吸障碍如打鼾或睡眠呼吸暂停或中风的各种疾病的化合物和包含它们的药物组合物。 更具体地,本发明的化合物包括取代的1-氨基-4-苯基 - 二氢异喹啉及其式I的衍生物:其中取代基R 1 -R 11在下文更具体地定义。 所要求保护的本发明化合物还包括其药学上可接受的盐和三氟乙酸盐以及其制备方法和药物递送系统。

    Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use
    8.
    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。