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1. 发明申请

US20070225323A1 SUBSTITUTED 4-PHENYLTETRAHYRDOISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS THEREOF, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USE 有权
标题翻译：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

2. 发明申请

US20080058328A1 SUBSTITUTED 4-PHENYLTETRAHYDROISOQUINOLINES, PHARMACEUITCAL COMPOSITIONS COMPRISING THEM AND THERAPEUTIC METHODS FOR THEIR USE 有权
标题翻译：取代的4-苯基恶唑啉酮，包含它们的药物组合物及其使用的治疗方法
公开(公告)号：US20080058328A1
公开(公告)日：2008-03-06
申请号：US11776041
申请日：2007-07-11
申请人： Uwe HEINELT , Hans-Jochen LANG , Klaus WIRTH , Thomas LICHER , Armin HOFMEISTER
发明人： Uwe HEINELT , Hans-Jochen LANG , Klaus WIRTH , Thomas LICHER , Armin HOFMEISTER
IPC分类号： C07D217/12 , A61K31/47 , A61K31/5377 , A61P13/00 , C07D413/10 , A61P25/00 , A61P33/00 , A61P9/00
CPC分类号： C07D401/10 , C07D217/18
摘要： The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.
摘要翻译：本发明涉及式I的取代的4-苯基四氢异喹啉，其中R1-R8，N，W，X和Z如本文所定义。这些化合物和包含它们的药物组合物可用于治疗呼吸障碍，睡眠呼吸暂停，肾脏疾病，高血压，高血压，中枢神经系统疾病等。

3. 发明申请

US20140106366A1 METHODS FOR DETERMINING SODIUM-PROTON-EXCHANGER LIGAND EFFICIENCY 审中-公开
标题翻译：用于确定钠 - 交换器配体效率的方法
公开(公告)号：US20140106366A1
公开(公告)日：2014-04-17
申请号：US14017854
申请日：2013-09-04
申请人： Thomas LICHER , Hans-Willi JANSEN , Ursula SCHINDLER , Stefan SCHAEFER
发明人： Thomas LICHER , Hans-Willi JANSEN , Ursula SCHINDLER , Stefan SCHAEFER
IPC分类号： G01N33/68
CPC分类号： G01N33/6872 , G01N33/5008
摘要： The present invention relates to methods for determining the efficiency of an ion channel ligand comprising (a) contacting a cell expressing the ion channel with (i) plasma of an animal and (ii) the ion channel ligand and (b) determining the effect of the ion channel ligand on the cell.
摘要翻译：本发明涉及用于确定离子通道配体的效率的方法，其包括（a）使表达离子通道的细胞与（i）动物血浆和（ii）离子通道配体）和（b）确定细胞上的离子通道配体。

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