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    SUBSTITUTED 4-PHENYLTETRAHYRDOISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS THEREOF, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USE
    16.
    发明申请
    SUBSTITUTED 4-PHENYLTETRAHYRDOISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS THEREOF, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USE 有权
    取代的4-苯基乙酰氧基喹啉，其药物组合物，其制备和治疗用途的方法

    公开(公告)号：US20070225323A1

    公开(公告)日：2007-09-27

    申请号：US11680668

    申请日：2007-03-01

    申请人： Hans-Jochen LANG ,  Uwe HEINELT ,  Klaus WIRTH ,  Thomas LICHER ,  Armin HOFMEISTER

    发明人： Hans-Jochen LANG ,  Uwe HEINELT ,  Klaus WIRTH ,  Thomas LICHER ,  Armin HOFMEISTER

    IPC分类号： A61K31/47

    CPC分类号： C07D405/12 ,  C07D217/14 ,  C07D401/12

    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

    THIENO-IMINO ACID DERIVATIVES FOR USE AS MATRIX METALLOPROTEINASE INHIBITORS
    17.
    发明申请
    THIENO-IMINO ACID DERIVATIVES FOR USE AS MATRIX METALLOPROTEINASE INHIBITORS 有权
    用作基质金属蛋白酶抑制剂的噻二唑酸衍生物

    公开(公告)号：US20070093482A1

    公开(公告)日：2007-04-26

    申请号：US11461189

    申请日：2006-07-31

    申请人： Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER ,  Maxime LAMPILAS

    发明人： Manfred SCHUDOK ,  Hans MATTER ,  Armin HOFMEISTER ,  Maxime LAMPILAS

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4743 ,  C07D498/02

    CPC分类号： C07D495/04

    摘要： The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier. The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof. Furthermore the invention is directed to a method for preparing a compound of formula I.

    摘要翻译： 本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。 本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。 本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病 诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄 ，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量 的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。 此外，本发明涉及制备式I化合物的方法。