-
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。
-
2.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。
-
3.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。
-
4.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。
-
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：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。
-
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。
-
7.发明授权Phenothiazin derivatives, method for the production thereof and use thereof as pharmaceuticals 有权吩噻嗪衍生物，其制备方法和作为药物的用途公开(公告)号：US07732440B2
公开(公告)日：2010-06-08
申请号：US12507202
申请日：2009-07-22
申请人： Stefanie Keil , Elisabeth Defossa , Karl Schoenafinger , Dieter Schmoll , Axel Deitrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
发明人： Stefanie Keil , Elisabeth Defossa , Karl Schoenafinger , Dieter Schmoll , Axel Deitrich , Johanna Kuhlmann-Gottke , Karl-Christian Engel
IPC分类号： C07D417/14 , A61K31/5415
CPC分类号： C07D417/12 , C07D417/14 , C07D513/04
摘要： The invention relates to compounds of the formula I, wherein R1, R2, R3, R4, R5, R6, R7, A and B are as defined herein, the pharmaceutical compositions and the uses as pharmaceuticals.
摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，A和B如本文所定义，药物组合物和用作药物。
-
公开(公告)号：US07713963B2
公开(公告)日：2010-05-11
申请号：US11548501
申请日：2006-10-11
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译： 本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。 这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征， 心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常， 糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药 。
-
公开(公告)号：US07470689B2
公开(公告)日：2008-12-30
申请号：US11513574
申请日：2006-08-31
申请人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Günter Müller , Cécile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
发明人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Günter Müller , Cécile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
IPC分类号： A61K31/501 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D401/14 , A61K31/53 , C07D487/04 , A61P35/00
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04
摘要： Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
摘要翻译： 公开了通式（I）的化合物，其中取代基A，B，D，E，R 1和R 2的定义在说明书中详细描述，以及其生理上可耐受的盐，这些化合物的制备方法和 它们用作药物。 这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。
-
10.发明授权Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals 有权杂环取代的苯甲酰脲，其制备方法及其作为药物的用途公开(公告)号：US07138414B2
公开(公告)日：2006-11-21
申请号：US10617498
申请日：2003-07-11
申请人： Karl Schoenafinger , Elisabeth Defossa , Dieter Kadereit , Erich Von Roedern , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt
发明人： Karl Schoenafinger , Elisabeth Defossa , Dieter Kadereit , Erich Von Roedern , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： C07D235/02 , C07D251/00 , A61K31/395 , A61K31/445
CPC分类号： C07D211/60 , C07D211/62 , C07D231/12 , C07D231/26 , C07D233/56 , C07D235/18 , C07D249/08 , C07D249/12 , C07D253/07 , C07D257/04 , C07D271/10 , C07D271/113 , C07D307/68
摘要： The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives.Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.
摘要翻译： 本发明涉及杂环取代的苯甲酰脲，也涉及其生理上耐受的盐和生理功能衍生物。 化合物描述为其中基团被定义为特定的式I，以及它们的药学上可接受的盐及其制备方法。 该化合物适用于例如治疗2型糖尿病。
-
-
-
-
-
-
-
-
-
搜索结果
67 条记录 (耗时 0.037 秒)
