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公开(公告)号：US08097758B2
公开(公告)日：2012-01-17
申请号：US12400189
申请日：2009-03-09
IPC分类号： C07C233/65 , C07C233/05 , C07D217/22 , C07D277/82 , C07D239/72 , A61K31/16 , A61K31/4184 , A61K31/428 , A61K31/47
CPC分类号： C07D277/82 , C07C1/26 , C07C17/10 , C07C2529/40 , C07D207/34 , C07D209/42 , C07D213/56 , C07D215/48 , C07D217/22 , C07D235/30 , C07D239/28 , C07D239/95 , C07D241/44 , C07D307/54 , C07D307/85 , C07D333/38 , C07D333/70 , C07D405/12 , C07C9/00 , C07C19/075
摘要： The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.
摘要翻译： 本发明涉及具有抗血栓形成活性的式（I）化合物，其特别是抑制凝血因子IXa，其制备方法和作为药物的用途。
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公开(公告)号：US08263621B2
公开(公告)日：2012-09-11
申请号：US12400187
申请日：2009-03-09
IPC分类号： A61K31/47
CPC分类号： C07D217/22 , C07C235/16 , C07C257/18 , C07D235/30
摘要： The invention relates to the compounds of formula I having antithrombotic activity which especially inhibits blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.
摘要翻译： 本发明涉及具有抗血栓形成活性的式I化合物，其特别是抑制血液凝固因子IXa，其制备方法及其作为药物的用途。
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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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4.发明授权Substituted amidoalkyl uracils and their use as inhibitors of the poly(adp-ribose) synthetase (PARS) 失效取代的酰氨基烷基尿嘧啶及其作为聚（adp-核糖）合成酶（PARS）的抑制剂的用途公开(公告)号：US07125995B2
公开(公告)日：2006-10-24
申请号：US10416622
申请日：2001-11-02
申请人： Barbara Albrecht , Michael Gerisch , Gabriele Handke-Ergüden , Axel Jensen , Thomas Krahn , Werner Nickl , Felix Oehme , Karl-Heinz Schlemmer , Henning Steinhagen
发明人： Barbara Albrecht , Michael Gerisch , Gabriele Handke-Ergüden , Axel Jensen , Thomas Krahn , Werner Nickl , Felix Oehme , Karl-Heinz Schlemmer , Henning Steinhagen
IPC分类号： C07D239/70 , C07D493/04 , C07D495/04 , A61K31/517 , A61P9/10
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This application relates to compounds of formula (I) below in which the several variable groups are as defined in the specification and claims, to methods of preparing these materials, to pharmaceutical compositions containing these materials, and to methods of using these materials to treat ischaemia or reperfusion damage.
摘要翻译： 本申请涉及以下式（I）的化合物，其中几个可变基团如说明书和权利要求中所定义，制备这些材料的方法，含有这些材料的药物组合物以及使用这些材料来治疗局部缺血的方法 或再灌注损伤。
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5.发明授权Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals 有权环状氮杂吲哚-3-甲酰胺，它们的制备及其作为药物的用途公开(公告)号：US08580813B2
公开(公告)日：2013-11-12
申请号：US12845324
申请日：2010-07-28
申请人： Henning Steinhagen , Bodo Scheiper , Hans Matter , Gary Mccort
发明人： Henning Steinhagen , Bodo Scheiper , Hans Matter , Gary Mccort
IPC分类号： A61K31/44
CPC分类号： C07D471/04
摘要： The present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式I的环状氮杂吲哚-3-甲酰胺，其中A，R，R10，R20，R30，R40，Y1，Y2，Y3，Y4，n，p和q具有权利要求中所示的含义， 这是有价值的药物活性化合物。 具体地说，它们抑制酶肾素并调节肾素 - 血管紧张素系统的活性，并且可用于治疗例如高血压等疾病。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。
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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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7.发明授权Substituted phenylcyclohexane carboxylic acid amides and their use as adenosine uptake inhibitors 失效取代的苯基环己烷羧酸酰胺及其作为腺苷摄取抑制剂的用途公开(公告)号：US06984642B1
公开(公告)日：2006-01-10
申请号：US09980242
申请日：2000-05-16
申请人： Erwin Bischoff , Stephan Lensky , Stephan-Nicholas Müller , Holger Paulsen , Jörg Keldenich , Thomas Krahn , Joachim Schuhmacher , Jan Jänichen , Wolfgang Thielemann , Henning Steinhagen
发明人： Erwin Bischoff , Stephan Lensky , Stephan-Nicholas Müller , Holger Paulsen , Jörg Keldenich , Thomas Krahn , Joachim Schuhmacher , Jan Jänichen , Wolfgang Thielemann , Henning Steinhagen
IPC分类号： A61K31/496 , C07D403/04
CPC分类号： C07D235/24 , A61K31/4184 , A61K31/437 , C07D235/12 , C07D235/14 , C07D235/30 , C07D471/04
摘要： The present invention relates to substituted phenylcyclohexanecaboxamides of the formula (I), to processes for their preparation and to their use in medicaments, in particular for treating cardiovascular disorders.
摘要翻译： 本发明涉及式（I）的取代的苯基环己烷甲酰胺，其制备方法及其在药物中的用途，特别是用于治疗心血管疾病。
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8.发明申请Substituted amidoalkyl uracils and their use as inhibitors of the poly(adp-ribose) synthetase (pars) 失效取代的酰氨基烷基尿嘧啶及其作为聚（adp-核糖）合成酶（pars）抑制剂的用途公开(公告)号：US20050075347A1
公开(公告)日：2005-04-07
申请号：US10416622
申请日：2001-11-02
申请人： Barbara Albrecht , Michael Gerisch , Gabriele Handke-Erguden , Axel Jensen , Thomas Krahn , Werner Nickl , Felix Oehme , Karl-Heinz Schlemmer , Henning Steinhagen
发明人： Barbara Albrecht , Michael Gerisch , Gabriele Handke-Erguden , Axel Jensen , Thomas Krahn , Werner Nickl , Felix Oehme , Karl-Heinz Schlemmer , Henning Steinhagen
IPC分类号： C07D239/96 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D519/00 , C07D521/00 , A61K31/519
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The invention relates to novel amidoalkyl uracil derivatives of formula (I), to a method for the production thereof, and to their use as medicament active substances for the prophylaxis and/or treatment of medical disorders.
摘要翻译： 本发明涉及式（I）的新型酰氨基烷基尿嘧啶衍生物，其制备方法及其作为用于预防和/或治疗医学病症的药物活性物质的用途。
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9.发明申请Substituted piperazine cyclohexane carboxilic acid amides and the use thereof 审中-公开取代的哌嗪环己烷羧酸酰胺及其用途公开(公告)号：US20050054637A1
公开(公告)日：2005-03-10
申请号：US10492337
申请日：2002-10-01
申请人： Erwin Bischoff , Thomas Krahn , Holger Paulsen , Joachim Schuhmacher , Henning Steinhagen , Wolfgang Thielemann
发明人： Erwin Bischoff , Thomas Krahn , Holger Paulsen , Joachim Schuhmacher , Henning Steinhagen , Wolfgang Thielemann
IPC分类号： C07D295/14 , A61K31/495 , A61K31/496 , A61K31/501 , A61P7/02 , A61P7/10 , A61P9/08 , A61P9/10 , A61P19/08 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P35/00 , A61P43/00 , C07D207/34 , C07D207/40 , C07D207/416 , C07D209/08 , C07D209/42 , C07D213/38 , C07D213/71 , C07D213/81 , C07D213/82 , C07D215/12 , C07D215/50 , C07D215/54 , C07D217/26 , C07D231/12 , C07D231/14 , C07D231/56 , C07D233/84 , C07D233/90 , C07D235/04 , C07D237/24 , C07D261/14 , C07D275/04 , C07D295/155 , C07D295/18 , C07D295/192 , C07D295/20 , C07D295/215 , C07D295/22 , C07D295/26 , C07D307/68 , C07D317/58 , C07D317/68 , C07D333/34 , C07D333/38 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D207/416 , C07D213/71 , C07D231/56 , C07D295/155 , C07D295/192 , C07D295/215 , C07D295/26 , C07D333/38
摘要： The present invention relates to substituted piperazinecyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in pharmaceuticals, in particular for the prophylaxis and/or treatment of cardiovascular disorders.
摘要翻译： 本发明涉及式（I）的取代的哌嗪环己烷甲酰胺，其制备方法及其在药物中的用途，特别是用于预防和/或治疗心血管疾病。
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10.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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