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公开(公告)号：US20090192150A1
公开(公告)日：2009-07-30
申请号：US12364124
申请日：2009-02-02
申请人： Uwe HEINELT , Armin HOFMEISTER , Joerg CZECH
发明人： Uwe HEINELT , Armin HOFMEISTER , Joerg CZECH
IPC分类号： A61K31/538 , C07D471/04 , A61K31/4439 , A61K31/5377 , A61P9/00 , A61P19/02 , C07D213/36 , C07C323/07
CPC分类号： C07D471/04
摘要： The invention relates to compounds of the formula I having antithrombotic activity, which in particular inhibit the protease-activated receptor 1 (PAR1), processes for their preparation and use thereof as medicaments.
摘要翻译： 本发明涉及具有抗血栓形成活性的式I化合物，其特别是抑制蛋白酶活化受体1（PAR1），其制备方法和用途作为药物。
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2.发明申请SUBSTITUTED THIOPHENES: COMPOSITIONS, PROCESSES OF MAKING, AND USES IN DISEASE TREATMENT AND DIAGNOSIS 有权替代THIOPHENES：组合物，制备方法和用于疾病治疗和诊断的用途公开(公告)号：US20080070947A1
公开(公告)日：2008-03-20
申请号：US11863608
申请日：2007-09-28
申请人： Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Klaus WIRTH , Michael GEKLE , Markus BLEICH
发明人： Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Klaus WIRTH , Michael GEKLE , Markus BLEICH
IPC分类号： A61K31/4184 , A61K31/454 , A61P1/00 , A61P25/00 , A61P3/00 , A61P35/00 , A61P9/00
CPC分类号： C07D409/12 , A61K31/4184 , A61K31/454
摘要： Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.
摘要翻译： 取代的噻吩，其制备方法，其用作药物或诊断剂。 取代的噻吩衍生物具有以下骨架结构：包含这种类型的化合物的药物可用于预防或治疗各种疾病，例如呼吸障碍和打鼾，急性和慢性疾病，由缺血和/或再灌注事件诱导的疾病，以及由 增生或纤维化事件，中枢神经系统疾病和脂质代谢，糖尿病，凝血和寄生虫感染。
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3.发明申请N-Substituted (Benzoimidazol-2-yl)phenylamines, Processes for Their Preparation, Their Use as a Medicament or Diagnostic Aid, and a Medicament Comprising Them 失效N-取代的（苯并咪唑-2-基）苯胺，其制备方法，用作药物或诊断辅助剂，以及包括它们的药物公开(公告)号：US20100168196A1
公开(公告)日：2010-07-01
申请号：US12722634
申请日：2010-03-12
申请人： Uwe HEINELT , Hans-Jochen LANG , Armin HOFMEISTER , Klaus WIRTH , Martin HUG
发明人： Uwe HEINELT , Hans-Jochen LANG , Armin HOFMEISTER , Klaus WIRTH , Martin HUG
IPC分类号： A61K31/4184 , C07D235/30 , A61P11/00 , A61P13/12 , A61P1/00 , A61P9/12 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/18 , A61P9/10 , A61P7/02 , A61P1/16 , A61P33/00 , A61P33/02 , A61P33/06
CPC分类号： C07D235/30
摘要： This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.
摘要翻译： 本发明涉及式（I）化合物，含有抑制亚型3（NHE3）的钠 - 质子交换剂的所述化合物的组合物，其可用于预防或治疗患有疾病状态的患者中的各种疾病， 例如包括急性或慢性肾衰竭，胆汁功能障碍和呼吸系统疾病如打鼾或睡眠呼吸暂停或中风的肾脏疾病。
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4.发明申请N-Substituted (Benzoimidazol-2-yl)phenylamines, Processes for Their Preparation, Their Use as a Medicament or Diagnostic Aid, and a Medicament Comprising Them 审中-公开N-取代的（苯并咪唑-2-基）苯胺，其制备方法，用作药物或诊断辅助剂，以及包括它们的药物公开(公告)号：US20080167359A1
公开(公告)日：2008-07-10
申请号：US12027033
申请日：2008-02-06
申请人： Uwe HEINELT , Hans-Jochen LANG , Armin HOFMEISTER , Klaus WIRTH , Martin HUG
发明人： Uwe HEINELT , Hans-Jochen LANG , Armin HOFMEISTER , Klaus WIRTH , Martin HUG
IPC分类号： A61K31/4184 , C07D235/04 , A61P11/00 , A61P13/12 , A61P9/00 , A61P25/00 , A61P3/00 , A61P33/00
CPC分类号： C07D235/30
摘要： This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.
摘要翻译： 本发明涉及式（I）化合物，含有抑制亚型3（NHE3）的钠 - 质子交换剂的所述化合物的组合物，其可用于预防或治疗患有疾病状态的患者中的各种疾病， 例如包括急性或慢性肾衰竭，胆汁功能障碍和呼吸系统疾病如打鼾或睡眠呼吸暂停或中风的肾脏疾病。
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5.发明申请SUBSTITUTED THIOPHENES: COMPOSITIONS, PROCESSES OF MAKING, AND USES IN DISEASE TREATMENT AND DIAGNOSIS 有权替代THIOPHENES：组合物，制备方法和用于疾病治疗和诊断的用途公开(公告)号：US20090137630A1
公开(公告)日：2009-05-28
申请号：US12363030
申请日：2009-01-30
申请人： Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Klaus WIRTH , Michael GEKLE , Markus BLEICH
发明人： Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Klaus WIRTH , Michael GEKLE , Markus BLEICH
IPC分类号： A61K31/454 , A61K31/4184 , A61P13/12
CPC分类号： C07D409/12 , A61K31/4184 , A61K31/454
摘要： The present invention comprises compounds and compositions comprising substituted thiophene derivatives with the following backbone structure: The compounds of this type are of useful in the treatment of various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.
摘要翻译： 本发明包括具有以下骨架结构的取代噻吩衍生物的化合物和组合物：这种类型的化合物可用于治疗各种疾病，例如呼吸系统疾病和打鼾，急性和慢性疾病，由缺血性和 /或再灌注事件以及增殖或纤维化事件，中枢神经系统疾病和脂质代谢，糖尿病，凝血和寄生虫感染。
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6.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
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7.发明申请NOVEL SUBSTITUTED 2-AMINOIMIDAZOLES, PROCESS FOR THEIR PREPARATION, THEIR USE AS MEDICAMENT OR DIAGNOSTIC AID 审中-公开新型取代的2-氨基嘧啶，其制备方法，用作药物或诊断辅助剂公开(公告)号：US20080275098A1
公开(公告)日：2008-11-06
申请号：US12172380
申请日：2008-07-14
IPC分类号： C07D233/50 , A61K31/4168 , C07D235/30 , C07D317/72 , A61P9/10 , A61P3/00 , A61P3/10 , C07D317/10 , A61K31/4184
CPC分类号： C07D233/50
摘要： The present invention comprises novel substituted 2-aminoimidazoles of formula I, processes for their preparation, pharmaceutical compositions thereof, and methods for their use in the treatment of disorders of the central nervous system, cardiovascular disorders, stroke and pulmonary disorders, urinary disorders such as acute or chronic renal failure, disorders of biliary function, respiratory disorders such as snoring or sleep apnea. wherein the substitutents R1-R8 are further defined herein.
摘要翻译： 本发明包括式I的新型取代的2-氨基咪唑，其制备方法，其药物组合物及其用于治疗中枢神经系统疾病，心血管疾病，中风和肺部疾病的方法，尿障碍如 急性或慢性肾衰竭，胆汁功能障碍，呼吸系统疾病如打鼾或睡眠呼吸暂停。 其中取代基R1-R8在本文中进一步定义。
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8.发明申请METHODS FOR THE IMPROVEMENT OF MEMORY AND NEUROLOGICAL FUNCTION COMPRISING THE ADMINISTRATION OF COMPOSITIONS THAT ACT AS INHIBITORS OF THE SODIUM PROTON (NA+ /H+ ) EXCHANGER, SUBTYPE 5 (NHE-5) 审中-公开改进存储器和神经功能的方法，包括作为钠原子（NA + / H +）交换剂，第5类（NHE-5）交换剂的抑制剂的组合物的管理，公开(公告)号：US20080234317A1
公开(公告)日：2008-09-25
申请号：US12046920
申请日：2008-03-12
申请人： Heinz-Werner KLEEMANN , Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Holger GAUL , Ulrich Hendrich SCHROEDER , Klaus REYMANN
发明人： Heinz-Werner KLEEMANN , Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Holger GAUL , Ulrich Hendrich SCHROEDER , Klaus REYMANN
CPC分类号： A61K31/47
摘要： The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na+/H+ exchanger, subtype 5 (NHE-5) as inhibitors of cellular NHE-5 enhance long term potentiation (LTP) and are therefore effective in the treatment of memory impairments, dementing disorders, and for improving memory. Particularly suitable for the treatment of neurodegenerative disorders, memory impairments and dementing disorders, and for improving memory, are the following NHE-5 inhibitors of the formula I Wherein the R1-R8 substituents are further defined herein:
摘要翻译： 本发明包括使用有效抑制作为细胞NHE抑制剂的第5型（NHE-5）型的Na + / H + -5增强长期增强（LTP），因此有效治疗记忆障碍，痴呆症和改善记忆。 特别适用于治疗神经变性疾病，记忆障碍和痴呆病症以及改善记忆力，是下列式I的NHE-5抑制剂，其中R1-R8取代基在本文中进一步定义：
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9.发明申请SUBSTITUTED 4-PHENYLTETRAHYDROISOQUINOLINES, PHARMACEUITCAL COMPOSITIONS COMPRISING THEM AND THERAPEUTIC METHODS FOR THEIR USE 有权取代的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。
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10.发明申请TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权三唑盐作为PAR1抑制剂，其生产和用作药物公开(公告)号：US20120208805A1
公开(公告)日：2012-08-16
申请号：US13452146
申请日：2012-04-20
IPC分类号： A61K31/5025 , A61K31/5377 , A61K31/538 , A61P7/02 , A61P29/00 , A61P9/10 , A61P25/00 , A61P9/00 , A61P37/00 , A61P3/10 , A61P3/00 , A61P35/00 , A61P35/04 , A61P11/00 , A61P27/02 , A61P17/02 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to novel compounds of formula I where X, A−, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
摘要翻译： 本发明涉及式I的新化合物，其中X，A，Q 1，Q 2，Q 3，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9各自定义如下。 式I的化合物具有抗血栓形成活性并特别抑制蛋白酶活化的受体1（PAR1）。 本发明还涉及制备式I化合物及其作为药物的用途的方法。
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