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1.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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2.发明申请SF5 DERIVATIVES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权作为PAR1抑制剂的SF5衍生物，其生产和用作药物公开(公告)号：US20110034461A1
公开(公告)日：2011-02-10
申请号：US12851229
申请日：2010-08-05
IPC分类号： A61K31/5377 , C07D209/44 , A61K31/4035 , C07D413/10 , C07D403/10 , C07C381/00 , C07C303/40 , C07D207/404 , C07D295/112 , C07D207/06 , A61P7/02 , A61P29/00 , A61P9/06 , A61P9/10 , A61P3/04 , A61P35/00
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.发明申请IMIDAZOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权咪达唑啶作为PAR1抑制剂，其生产和用作药物公开(公告)号：US20110034456A1
公开(公告)日：2011-02-10
申请号：US12851198
申请日：2010-08-05
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/5025 , A61P9/10 , A61P9/00 , A61P7/02 , A61P29/00 , A61P3/10 , A61P35/00 , A61P35/04 , A61P19/02 , A61P11/00 , A61P3/00 , A61P9/06
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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4.发明申请TRIAZOLOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权作为PAR1抑制剂的三唑并吡嗪，其生产和用作药物公开(公告)号：US20120010203A1
公开(公告)日：2012-01-12
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： A61K31/5025 , C07D413/14 , A61K31/5377 , A61K31/538 , A61P7/02 , A61P29/00 , A61P9/10 , A61P25/00 , A61P9/06 , A61P3/10 , A61P3/00 , A61P35/00 , A61P35/04 , A61P11/00 , A61P27/02 , A61P17/02 , C07D487/04
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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5.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：US20110034452A1
公开(公告)日：2011-02-10
申请号：US12851219
申请日：2010-08-05
IPC分类号： A61K31/536 , C07D487/04 , C07D471/04 , A61K31/5025 , A61K31/5377 , A61K31/437 , A61P7/02 , A61P29/00 , A61P9/10 , A61P9/00 , A61P11/00 , A61P9/06 , A61P3/10 , A61P35/00 , A61P35/04
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： 本发明涉及新的式I化合物，其中X，A-，Q1，Q2 Q3，R2，R3，R4，R5，R6，R7，R8和R9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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6.发明申请TRIAZOLOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权作为PAR1抑制剂的三唑并吡嗪，其生产和用作药物公开(公告)号：US20110034451A1
公开(公告)日：2011-02-10
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： A61K31/538 , C07D487/04 , A61K31/5025 , A61K31/5377 , A61P7/02 , A61P9/10 , A61P9/00 , A61P11/00 , A61P9/06 , A61P29/00 , A61P3/10 , A61P35/00 , A61P35/04
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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公开(公告)号：US20100249101A1
公开(公告)日：2010-09-30
申请号：US12683736
申请日：2010-01-07
申请人： Henning STEINHAGEN , Hauke SZILLAT , Markus FOLLMANN , Reinhard KIRSCH , Volkmar WEHNER , Hans MATTER , Martin LORENZ , Kent W. Neuenschwander , Anthony C. SCOTESE
发明人： Henning STEINHAGEN , Hauke SZILLAT , Markus FOLLMANN , Reinhard KIRSCH , Volkmar WEHNER , Hans MATTER , Martin LORENZ , Kent W. Neuenschwander , Anthony C. SCOTESE
IPC分类号： A61K31/553 , C07D213/90 , A61K31/455 , C07C237/20 , A61K31/167 , A61K31/4409 , C07D265/30 , A61K31/5375 , C07D309/08 , A61K31/351 , C07D211/66 , A61K31/4465 , C07D211/42 , C07D409/12 , A61K31/381 , C07D207/12 , A61K31/4015 , C07D277/24 , A61K31/426 , C07D241/04 , A61K31/4965 , C07D241/18 , C07D267/10 , A61P9/00 , A61P11/00 , A61P31/12 , A61P35/00 , A61P29/00
CPC分类号： C07D213/80 , C07C257/18 , C07C311/08 , C07C311/46 , C07C317/22 , C07C317/32 , C07C2601/14 , C07D211/42 , C07D213/30 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially 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 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。式I化合物是有价值的药理学活性化合物。 它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶，特别是因子VIIa的抑制剂，并且通常可用于其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件。 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。
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8.发明申请CHLOROTHIOPHENE-ISOXAZOLES AS INHIBITORS OF COAGULATION FACTORS XA AND THROMBIN 有权作为凝血因子XA和THROMBIN的抑制剂的氯噻酮 - 异丙嗪公开(公告)号：US20110112074A1
公开(公告)日：2011-05-12
申请号：US12858981
申请日：2010-08-18
申请人： Markus FOLLMANN , Volkmar WEHNER , Jean-Michel ALTENBURGER , Gilbert LASSALLE , Jean-Pascal HERAULT
发明人： Markus FOLLMANN , Volkmar WEHNER , Jean-Michel ALTENBURGER , Gilbert LASSALLE , Jean-Pascal HERAULT
IPC分类号： A61K31/55 , C07D413/14 , A61P9/10 , A61P7/02 , A61K31/454 , A61K31/496 , A61K31/5377
CPC分类号： C07D413/14 , C07D413/04
摘要： The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the 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; R3; R4; R5，R16，X和M具有权利要求中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和凝血酶的可逆抑制剂，并且通常可用于存在因子Xa和/或凝血酶的不期望活性或用于治疗或预防因子Xa和凝血酶的抑制的病症 是打算的 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。
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公开(公告)号：US20080262028A1
公开(公告)日：2008-10-23
申请号：US12102105
申请日：2008-04-14
IPC分类号： A61K31/4365 , C07D213/02 , C07D221/02 , A61P3/00 , A61P11/00 , A61P35/00 , A61P9/00 , A61K31/4439
CPC分类号： C07D413/14 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound of formula I: or any stereoisomeric form of the compound of the formula I or a mixture of these forms in any ratio or a physiologically acceptable salt of the compound of the formula I which inhibit the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor), and to a process for their preparation and to their use to treat described diseases where the substituents are as described in the specification.
摘要翻译： 本发明涉及式I化合物或式I化合物的任何立体异构形式或其抑制酶TAFIa的式I化合物的任何比例或生理学上可接受的盐的这些形式的混合物 活化的凝血酶可激活的纤维蛋白溶解抑制剂），以及它们的制备方法及其用于治疗所述疾病的用途，其中取代基如说明书中所述。
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公开(公告)号：US20070049573A1
公开(公告)日：2007-03-01
申请号：US11467277
申请日：2006-08-25
申请人： Armin BAUER , Michael WAGNER , Marc NAZARE , Volkmar WEHNER , Matthias URMANN , Hans MATTER
发明人： Armin BAUER , Michael WAGNER , Marc NAZARE , Volkmar WEHNER , Matthias URMANN , Hans MATTER
IPC分类号： A61K31/553 , A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/52 , A61K31/4709 , A61K31/405 , A61K31/4025
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention relates to compounds of the formulae (I) and (Ia), wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae (I) and (Ia) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae (I) and (Ia), 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）和（Ia）的化合物，其中R 0， R＆lt; 1＆gt;; R3; R4; R22，Q; V，G和M具有权利要求中所示的含义。 式（I）和（Ia）的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，适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及制备式（I）和（Ia）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。
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