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公开(公告)号：US20090233949A1
公开(公告)日：2009-09-17
申请号：US12400189
申请日：2009-03-09
IPC分类号： A61K31/517 , C07D217/22 , A61K31/47 , C07D277/82 , A61K31/428 , C07D235/04 , A61K31/4184 , C07C233/64 , A61K31/16 , C07D239/72 , A61P9/00 , A61P7/00
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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2.发明申请公开(公告)号：US20090233961A1
公开(公告)日：2009-09-17
申请号：US12400187
申请日：2009-03-09
IPC分类号： A61K31/472 , C07D217/22 , A61K31/4184 , C07D235/30 , A61P7/02
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：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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4.发明申请CYCLIC INDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 有权循环吲哚-3-羧酰胺，其制备及其作为药物的用途公开(公告)号：US20110039830A1
公开(公告)日：2011-02-17
申请号：US12845317
申请日：2010-07-28
IPC分类号： A61K31/551 , C07D403/06 , A61K31/454 , C07D401/14 , A61K31/4545 , A61P9/00 , A61P13/12 , A61P27/06
CPC分类号： C07D209/42 , C07D401/04 , C07D403/06 , C07D405/04 , C07D409/04
摘要： The present invention relates to cyclic indole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, 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的环吲哚-3-甲酰胺，其中A，R，R10，R20，R30，R40，n，p和q具有权利要求中所示的含义，它们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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5.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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6.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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7.发明申请Pyrazolopyridine derivatives as inhibitors of beta-Adrenergic Receptor Kinase 1 有权吡唑并吡啶衍生物作为β-肾上腺素能受体激酶1的抑制剂公开(公告)号：US20080227777A1
公开(公告)日：2008-09-18
申请号：US11961282
申请日：2007-12-20
申请人： Henning STEINHAGEN , Jochen HUBER , Kurt RITTER , Bernard PIRARD , Kirsten BJERGARDE , Marcel PATEK , Martin SMRCINA , Linli WEI
发明人： Henning STEINHAGEN , Jochen HUBER , Kurt RITTER , Bernard PIRARD , Kirsten BJERGARDE , Marcel PATEK , Martin SMRCINA , Linli WEI
IPC分类号： A61K31/5377 , C07D471/04 , A61P31/12 , A61P25/36 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) useful as inhibitors of beta-adrenergic receptor kinase 1 (βARK-1), compositions containing such compounds and their use for the treatment and prevention of chronic heart failure, hypertension, myocardial ischemia and hepatitis C virus (HCV) infections, and for the prevention of opiate addiction.
摘要翻译： 本发明涉及可用作β-肾上腺素能受体激酶1（βARK-1）抑制剂的式（I）的6-酰氨基取代的吡唑并吡啶衍生物，含有这些化合物的组合物及其用于治疗和预防慢性心力衰竭，高血压的用途 ，心肌缺血和丙型肝炎病毒（HCV）感染，以及预防鸦片成瘾。
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8.发明申请CYCLIC AZAINDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 有权周期性AZAINDOLE-3-CARBOXAMIDES，其制备及其作为药物的用途公开(公告)号：US20110039861A1
公开(公告)日：2011-02-17
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： A61K31/496 , C07D401/14 , A61P9/00 , A61P13/12 , A61P27/06
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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9.发明申请Aryl- and Heteroaryl-Ethyl-Acylguanidine Derivatives, Their Preparation and Their Application in Therapeutics 有权芳基和杂芳基 - 乙酰基胍衍生物及其制备及其在治疗中的应用公开(公告)号：US20090203696A1
公开(公告)日：2009-08-13
申请号：US12335198
申请日：2008-12-15
IPC分类号： A61K31/5377 , C07D241/04 , A61K31/495 , C07D211/58 , A61K31/4468 , C07D401/12 , A61K31/4545 , C07D239/26 , A61K31/505 , C07D265/30 , A61K31/5375 , C07D401/06 , A61K31/496 , C07D401/04 , A61K31/454 , C07D413/06 , C07D403/06 , C07D405/06 , C07D207/04 , A61K31/40 , C07D403/04 , C07D413/04 , C07D235/04 , A61K31/4184 , A61P9/12 , A61P9/04 , A61P9/00
CPC分类号： C07C279/22 , C07D207/14 , C07D211/46 , C07D211/58 , C07D211/76 , C07D213/38 , C07D213/74 , C07D213/82 , C07D231/12 , C07D231/56 , C07D235/08 , C07D239/26 , C07D239/36 , C07D239/46 , C07D241/08 , C07D241/12 , C07D249/08 , C07D277/30 , C07D295/155 , C07D295/192 , C07D307/14 , C07D307/79 , C07D313/08 , C07D317/60 , C07D319/16 , C07D333/28 , C07D401/12
摘要： Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
摘要翻译： 公开了根据式（I）的化合物：其中A，Q，X，Y，Z，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11如本文所定义。 本公开还涉及含有式（I）化合物的药物组合物，其用于制备式（I）化合物的方法，以及使用式（I）化合物的方法。
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10.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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