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    Substituted 4-phenyltetrahydroisoquinolines, process for their preparation, pharmaceutical compositions and therapeutic use
    1.
    发明授权
    Substituted 4-phenyltetrahydroisoquinolines, process for their preparation, pharmaceutical compositions and therapeutic use 有权
    取代的4-苯基四氢异喹啉，其制备方法，药物组合物和治疗用途

    公开(公告)号：US08455515B2

    公开(公告)日：2013-06-04

    申请号：US12046928

    申请日：2008-03-12

    申请人： Hans-Jochen Lang

    发明人： Hans-Jochen Lang

    IPC分类号： C07D217/04 ,  A61K31/472

    CPC分类号： C07D217/14

    摘要： The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds and pharmaceutical compositions comprising them which are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE-3). 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 defined by the formula I in which R1-R8 are defined herein.

    摘要翻译： 本发明涉及取代的4-苯基四氢异喹啉化合物和包含它们的药物组合物，它们是钠 - 氢交换器（NHE），特别是亚型3（NHE-3）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，本发明涉及由式I定义的取代的4-苯基 - 四氢异喹啉，其中R 1 -R 8在本文中定义。

    2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
    10.
    发明申请
    2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开
    2-PHENYL-INDOLES作为PROSTAGLANDIN D2受体拮抗剂

    公开(公告)号：US20070265278A1

    公开(公告)日：2007-11-15

    申请号：US11782890

    申请日：2007-07-25

    申请人： Keith HARRIS ,  Hans-Jochen Lang ,  Rose Mathew ,  Stephen Shimshock ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Zhaoxia Yang ,  Kenneth Bordeau

    发明人： Keith HARRIS ,  Hans-Jochen Lang ,  Rose Mathew ,  Stephen Shimshock ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Zhaoxia Yang ,  Kenneth Bordeau

    IPC分类号： A61K31/404 ,  A61K31/4245 ,  A61K31/435 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/495 ,  A61P1/04 ,  A61P37/08 ,  A61P9/00 ,  C07D209/04 ,  C07D271/113 ,  C07D401/12

    CPC分类号： C07D209/12 ,  C07D209/18 ,  C07D209/22 ,  C07D209/24 ,  C07D405/12 ,  C07D413/06

    摘要： The present invention is directed to a compound of Formula (XVI): (please replace Formula (I) with Formula (XVI) as shown below) wherein R, R2, R3, R4, R5, R6, R7 and n are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (XVI) in admixture with a pharmaceutically acceptable carrier, a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (XVI).

    摘要翻译： 本发明涉及式（ⅩⅥ）化合物：（如下所示，用式（ⅩⅥ）表示的式（I）表示）其中R，R 2，R 3， R 4，R 4，R 5，R 6，R 7和n如本文所定义，或 其药学上可接受的盐，水合物或溶剂化物，其药学上可接受的前药，或药学上可接受的盐，水合物或溶剂化物，药物组合物，其包含药学上有效量的根据式（XVI）的一种或多种化合物 与药学上可接受的载体混合，治疗患有PGD2介导的病症的患者的方法，包括但不限于过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身肥大细胞增多症 ，伴有系统性肥大细胞活化，过敏性休克，支气管收缩，支气管炎，荨麻疹， 湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），伴随瘙痒的行为（如刮伤和殴打）而产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍） ，炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向所述患者施用药学有效量的根据式（XVI）的化合物。