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1.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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2.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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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：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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4.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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5.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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6.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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公开(公告)号：US08143242B2
公开(公告)日：2012-03-27
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 , A61K31/4965 , A61K31/44 , A61K31/426 , A61K31/381 , A61K31/167 , C07D281/06 , C07D241/04 , C07D213/65 , C07D277/24 , C07D409/02 , C07C237/20
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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公开(公告)号：US07429581B2
公开(公告)日：2008-09-30
申请号：US10744744
申请日：2003-12-23
申请人： Marc Nazare , Volkmar Wehner , David W. Will , Hans Matter
发明人： Marc Nazare , Volkmar Wehner , David W. Will , Hans Matter
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor 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 is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.
摘要翻译： 本发明涉及式I化合物，其中R 0为0或0; R＆lt; 1＆gt;; R 2; 3＆lt; 3＆gt; R 4; Q; V，G和M具有以下含义。 式I化合物是药理活性化合物。 它表现出强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于 治疗或预防因素Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法和包含其的药物制剂。
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公开(公告)号：US07196103B2
公开(公告)日：2007-03-27
申请号：US10848743
申请日：2004-05-19
申请人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
发明人： Marc Nazare , Volkmar Wehner , Kurt Ritter , Volker Laux
IPC分类号： A61K31/44 , A61K31/445 , C07D413/00 , C07D401/00 , C07D211/68
CPC分类号： C07D413/14
摘要： The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.
摘要翻译： 本发明涉及可用于抑制因子Xa的活性的式I化合物。 本发明还涉及含有所述化合物的组合物，其制备方法，其用途，例如用于抑制凝血酶的形成或用于治疗或预防性治疗患有或与疾病状态相关的患者或与之相关的患者 伴有心血管疾病。
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公开(公告)号：US20050043302A1
公开(公告)日：2005-02-24
申请号：US10926909
申请日：2004-08-26
申请人： Marc Nazare , Melanie Essrich , David Will , Hans Matter , Kurt Ritter , Volkmar Wehner
发明人： Marc Nazare , Melanie Essrich , David Will , Hans Matter , Kurt Ritter , Volkmar Wehner
IPC分类号： A61K31/404 , A61K31/405 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P43/00 , C07D209/22 , C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/541 , A61K31/4709 , A61K31/502 , A61K31/5377
CPC分类号： C07D413/14 , C04B35/632 , C07D209/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The 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 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 Vila is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.
摘要翻译： 本发明涉及式I化合物，其中R 0; R 1; R 2; R 3; R 4; R 5; R 6; R 7; Q; V，G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。 它们具有强烈的抗血栓形成作用，并且适用于例如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化合物的方法，其用途，特别是作为用于治疗上述病症的药物，以及包含它们的药物制剂。
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