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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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7.发明申请SUBSTITUTED, BICYCLIC 8-PYRROLIDINOXANTHINES, AND METHODS FOR THEIR USE AS INHIBITORS OF DIPEPTIDYL PEPTIDASE 有权取代的双环8-吡咯烷酮，及其作为胰蛋白酶抑制剂的方法公开(公告)号：US20070197563A1
公开(公告)日：2007-08-23
申请号：US11624511
申请日：2007-01-18
申请人： Karl SCHOENAFINGER , Gerhard JAEHNE , Elisabeth DEFOSSA , Lothar SCHWINK , Holger WAGNER , Christian BUNING , Georg TSCHANK , Ulrich WERNER
发明人： Karl SCHOENAFINGER , Gerhard JAEHNE , Elisabeth DEFOSSA , Lothar SCHWINK , Holger WAGNER , Christian BUNING , Georg TSCHANK , Ulrich WERNER
IPC分类号： A61K31/522 , C07D473/06
CPC分类号： C07D519/00
摘要： The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.
摘要翻译： 本发明涉及取代的双环8-吡咯烷基亚基黄嘌呤及其式I的衍生物：其中各种R基团在本文中定义。 本发明还包括包含它们的药物组合物以及这些化合物的制备方法和通过施用所述组合物治疗代谢紊乱如2型糖尿病，胰岛素抵抗，高血糖症，动脉硬化疾病等的方法 。
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8.发明申请SUBSTITUTED BICYCLIC 8-PYRR0LIDINOXANTHINES, METHODS FOR THEIR PRODUCTION, PHARMACEUTICAL FORMULATIONS AND THEIR USE 有权取代的双相8-吡咯烷酮，其生产方法，药物制剂及其用途公开(公告)号：US20070167468A1
公开(公告)日：2007-07-19
申请号：US11623770
申请日：2007-01-17
申请人： Karl SCHOENAFINGER , Gerhard JAEHNE , Elisabeth DEFOSSA , Lothar SCHWINK , Holger WAGNER , Christian BUNING , Georg TSCHANK , Ulrich WERNER
发明人： Karl SCHOENAFINGER , Gerhard JAEHNE , Elisabeth DEFOSSA , Lothar SCHWINK , Holger WAGNER , Christian BUNING , Georg TSCHANK , Ulrich WERNER
IPC分类号： A61K31/522 , C07D473/04
CPC分类号： C07D519/00
摘要： Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula l: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.
摘要翻译： 公开了用于治疗升高的血糖水平的化合物和由其引起的生理和代谢紊乱，并且包含新颖的取代的双环8-吡咯烷基亚基黄嘌呤及其式I的衍生物：其中各种R基团在下文中定义。 本发明还包括包含它们的药物组合物以及这些化合物的制备方法。 因此可治疗的特定血糖障碍包括2型糖尿病，胰岛素抵抗，高血糖症，动脉硬化疾病等。
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![BICYCLIC ARYL-SULFONIC ACID [1,3,4]-THIADIAZOL-2-YL-AMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE](/abs-image/US/2010/01/28/US20100022603A1/abs.jpg.150x150.jpg)
9.发明申请BICYCLIC ARYL-SULFONIC ACID [1,3,4]-THIADIAZOL-2-YL-AMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE 有权双环芳烃磺酸[1,3,4] - 十二烷基-2-酰胺，其制备方法，药物组合物及其使用方法公开(公告)号：US20100022603A1
公开(公告)日：2010-01-28
申请号：US12566179
申请日：2009-09-24
申请人： Karl SCHOENAFINGER , Stefanie KEIL , Matthias URMANN , Hans MATTER , Maike GLIEN , Wolfgang WENDLER
发明人： Karl SCHOENAFINGER , Stefanie KEIL , Matthias URMANN , Hans MATTER , Maike GLIEN , Wolfgang WENDLER
IPC分类号： A61K31/41 , C07D285/12 , A61P7/12 , A61P25/00
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译： 本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺，它们的功能衍生物及其生理上可接受的盐和药物组合物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARδ 和PPARγ激动剂活性。 本发明化合物的结构由下式I定义，其中各种取代基在本文中定义，包括其生理上可接受的盐。 还公开了制备化合物的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其他神经变性疾病。
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10.发明申请PHENOTHIAZIN DERIVATES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF AS PHARMACEUTICALS 有权苯丙胺衍生物，其生产方法及其作为药物的用途公开(公告)号：US20090325942A1
公开(公告)日：2009-12-31
申请号：US12507202
申请日：2009-07-22
申请人： Stefanie KEIL , Elisabeth DEFOSSA , Karl SCHOENAFINGER , Dieter SCHMOLL , Axel DIETRICH , Johanna KUHLMANN-GOTTKE , Karl-Christian ENGEL
发明人： Stefanie KEIL , Elisabeth DEFOSSA , Karl SCHOENAFINGER , Dieter SCHMOLL , Axel DIETRICH , Johanna KUHLMANN-GOTTKE , Karl-Christian ENGEL
IPC分类号： A61K31/5415 , C07D417/14 , A61P3/00 , A61P25/18 , A61P25/28 , A61P25/34 , A61P25/00 , A61P25/32 , A61P3/10
CPC分类号： C07D417/12 , C07D417/14 , C07D513/04
摘要： The invention relates to compounds of the formula 1, 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1的化合物，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。
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