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1.发明授权Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments 有权三唑并嘧啶作为PAR1抑制剂，其生产和用作药物公开(公告)号：US09079906B2
公开(公告)日：2015-07-14
申请号：US13243118
申请日：2011-09-23
申请人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen , Bodo Scheiper
发明人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen , Bodo Scheiper
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D487/04 , A61K31/5025
CPC分类号： C07D487/04 , A61K31/5025
摘要： The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 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： 本发明涉及新的式I化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，Q1，Q2和Q3各自如下所定义。 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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2.发明授权SF5 derivatives as PAR1 inhibitors, production thereof, and use as medicaments 有权SF5衍生物作为PAR1抑制剂，其生产和用作药物公开(公告)号：US08466169B2
公开(公告)日：2013-06-18
申请号：US12851229
申请日：2010-08-05
IPC分类号： A61K31/4035 , C07D209/44 , C07D471/04
CPC分类号： C07D209/44 , C07D403/10
摘要： The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the 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 the formula I and to the use thereof as a medicament.
摘要翻译： 本发明涉及新的式I化合物，其中R1，R2，R3，R4，R5，R9，Ar，Q1，Q2和Q3各自如下所定义。 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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3.发明授权Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments 有权三唑并嘧啶作为PAR1抑制剂，其生产和用作药物公开(公告)号：US08076336B2
公开(公告)日：2011-12-13
申请号：US12851189
申请日：2010-08-05
申请人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen , Bodo Scheiper
发明人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen , Bodo Scheiper
IPC分类号： C07D487/04 , A61K31/5025 , A61P7/02 , A61P9/10 , A61P29/00 , A61P11/05 , A61P3/114
CPC分类号： C07D487/04 , A61K31/5025
摘要： The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 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： 本发明涉及新的式I化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，Q1，Q2和Q3各自如下所定义。 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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4.发明授权Imidazopyridazines as PAR1 inhibitors, production thereof, and use as medicaments 有权咪唑并哒嗪作为PAR1抑制剂，其制备及用作药物公开(公告)号：US08598177B2
公开(公告)日：2013-12-03
申请号：US12851198
申请日：2010-08-05
IPC分类号： A61K31/501 , A61K31/50 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 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： 本发明涉及新的式I化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，Q1，Q2和Q3各自如下所定义。 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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5.发明授权Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments 有权作为PAR1抑制剂的三唑鎓盐，其制备和用作药物公开(公告)号：US08853206B2
公开(公告)日：2014-10-07
申请号：US13452146
申请日：2012-04-20
IPC分类号： C07D249/00 , C07D413/06 , C07D487/04 , C07D471/04 , A61P7/00
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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6.发明授权Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments 有权作为PAR1抑制剂的三唑鎓盐，其制备和用作药物公开(公告)号：US08198272B2
公开(公告)日：2012-06-12
申请号：US12851219
申请日：2010-08-05
IPC分类号： C07D487/04 , C07D413/10 , A61K31/5025 , A61K31/5355 , A61P7/00 , A61P9/10 , A61P29/00 , A61P37/08 , A61P3/14
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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7.发明授权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，它们作为药物或诊断助剂的用途，以及包含它们的药物公开(公告)号：US08067614B2
公开(公告)日：2011-11-29
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
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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8.发明申请SUBSTITUTED AMINOINDANES AND ANALOGS THEREOF, AND THE PHARMACEUTICAL USE THEREOF 有权取代氨基酸及其类似物及其药物用途公开(公告)号：US20110201590A1
公开(公告)日：2011-08-18
申请号：US13061805
申请日：2009-08-25
申请人： Nils Rackelmann , Laurent Bialy , Heinrich Englert , Klaus Wirth , Petra Arndt , John Weston , Uwe Heinelt , Markus Follmann
发明人： Nils Rackelmann , Laurent Bialy , Heinrich Englert , Klaus Wirth , Petra Arndt , John Weston , Uwe Heinelt , Markus Follmann
IPC分类号： A61K31/454 , A61K31/4025 , A61K31/5377 , A61K31/4995 , A61K31/496 , A61K31/4439 , A61K31/4178 , A61K31/407 , C07D243/08 , C07D413/12 , C07D403/12 , C07D401/12 , C07D487/04 , A61P25/00 , A61P11/00 , A61P13/12 , A61P1/00 , A61P9/12 , A61P9/00 , A61P3/06 , A61P3/10 , A61P3/00
CPC分类号： C07D487/10 , C07D205/04 , C07D207/08 , C07D211/56 , C07D243/08 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D411/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D487/08
摘要： The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
摘要翻译： 本发明涉及式（I）的取代氨基茚子及其类似物及其药物用途。 包含这种类型化合物的药物适用于预防或治疗多种疾病，例如呼吸系统疾病，囊性纤维化疾病，急性或慢性肾脏疾病或排便障碍。
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9.发明申请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 - 二氢喹啉，其生产方法，作为药物使用，以及含有它们的药物公开(公告)号：US20090118327A1
公开(公告)日：2009-05-07
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： A61K31/472 , C07D217/22 , A61P1/10 , A61P11/16 , A61P25/20
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。
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10.发明授权Substituted 2-aminoimidazoles, process for their preparation, their use as medicament or diagnostic aid 失效取代的2-氨基咪唑，其制备方法，用作药物或诊断辅助剂公开(公告)号：US07442717B2
公开(公告)日：2008-10-28
申请号：US10771185
申请日：2004-02-03
IPC分类号： A61K31/4168 , C07D233/88
CPC分类号： C07D233/50
摘要： Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed inter alia for renal disorders such as acute or chronic renal failure, for disorders of biliary function, for respiratory disorders such as snoring or sleep apneas or for stroke
摘要翻译： 式I的新型取代的2-氨基咪唑，其制备方法，它们作为药物或诊断助剂的用途以及含有它们的药物。 这种类型的化合物可用于预防或治疗各种疾病，并且可以特别用于肾脏疾病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
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