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44 条记录 (耗时 0.06 秒)

    Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use
    13.
    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

    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： C07D217/00 ,  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。

    Factor VIIa inhibitors
    17.
    发明授权
    Factor VIIa inhibitors 有权
    因子VIIa抑制剂

    公开(公告)号：US06500803B1

    公开(公告)日：2002-12-31

    申请号：US09588651

    申请日：2000-06-07

    申请人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    发明人： Otmar Klingler ,  Manfred Schudok ,  Gerhard Zoller ,  Uwe Heinelt ,  Elisabeth Defossa ,  Hans Matter ,  Pavel Safar

    IPC分类号： A61K3805

    CPC分类号： C07K5/06086 ,  A61K38/00

    摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。 式I化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。 本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    Indole derivatives as inhibitors or factor Xa
    18.
    发明授权
    Indole derivatives as inhibitors or factor Xa 有权
    吲哚衍生物作为抑制剂或因子Xa

    公开(公告)号：US06337344B1

    公开(公告)日：2002-01-08

    申请号：US09582344

    申请日：2000-08-14

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    IPC分类号： A61K3144

    CPC分类号： C07D401/06 ,  C07D209/42 ,  C07D401/12 ,  C07D403/10 ,  C07D471/04

    摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.

    摘要翻译： 本发明涉及抑制血液凝固蛋白质，更具体地说，涉及式（I）的吲哚衍生物，其中R1a，R1b，R1c R1d，R2，R3，R4和A如权利要求中所示定义。 式（I）的化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式（I）化合物治疗和预防可以 通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防，以及式（I）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及包含与惰性载体混合或以其它方式结合的式（I）化合物的组合物，特别是含有式（I）化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。

    Substituted 1-amino-4-phenyl-dihydroisoquinolines, methods for the production thereof, use thereof as a medicament, and medicaments containing them
    20.
    发明授权
    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 - 二氢异喹啉，其制备方法，作为药物的用途，以及含有它们的药物

    公开(公告)号：US08124621B2

    公开(公告)日：2012-02-28

    申请号：US12212301

    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： C07D217/22 ,  A61K31/47

    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。