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1.发明申请SUBSTITUTED TETRAHYDRO-2H-ISOQUINOLIN-1-ONE DERIVATIVES, AND METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开取代的四氢-2H-异喹啉-1-酮衍生物及其生产和使用方法公开(公告)号：US20110021462A1
公开(公告)日：2011-01-27
申请号：US12850328
申请日：2010-08-04
IPC分类号： A61K31/69 , A61K31/472 , A61K31/4725 , A61P9/10 , A61P19/02 , A61P9/00 , A61P25/28 , A61P27/02 , A61P43/00 , A61P25/00 , A61P35/00 , A61P3/10 , A61P21/00
CPC分类号： C07D413/14 , C07D217/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14
摘要： This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.
摘要翻译： 本发明涉及根据通式（I）的化合物，其中取代基R 1，R 2，Ar和X的定义如说明书中所述，及其生理上可耐受的盐，制备这些化合物的方法及其制备方法 用作药物。 这些化合物是聚（ADP-核糖）聚合酶（PARP）抑制剂。
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2.发明申请SUBSTITUTED TETRAHYDRO-2H-ISOQUINOLIN-1-ONE DERIVATIVES, AND METHODS FOR THE PRODUCTION AND USE THEREOF 失效取代的四氢-2H-异喹啉-1-酮衍生物及其生产和使用方法公开(公告)号：US20070142430A1
公开(公告)日：2007-06-21
申请号：US11567352
申请日：2006-12-06
IPC分类号： A61K31/47 , C07D217/22
CPC分类号： C07D413/14 , C07D217/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/14
摘要： This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.
摘要翻译： 本发明涉及根据通式（I）的化合物，其中取代基R 1，R 2，Ar和X的定义如说明书中所述，及其生理上可耐受的盐，制备这些化合物的方法及其制备方法 用作药物。 这些化合物是聚（ADP-核糖）聚合酶（PARP）抑制剂。
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3.发明申请OXYGEN-SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开氧自由基取代的3-异丁酰氨基酸衍生物及其作为药物的用途公开(公告)号：US20140128616A1
公开(公告)日：2014-05-08
申请号：US14151951
申请日：2014-01-10
申请人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Thomas OLPP , Bodo SCHEIPER , Klaus WIRTH
发明人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Thomas OLPP , Bodo SCHEIPER , Klaus WIRTH
IPC分类号： C07D231/22 , C07C229/36
CPC分类号： C07C229/36 , C07D231/20 , C07D231/22 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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化合物，其中A，D，E，G，R 10，R 30，R 40，R 50和R 60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。 它们是蛋白酶组织蛋白酶A的抑制剂，例如可用于治疗动脉粥样硬化，心力衰竭，肾脏疾病，肝脏疾病或炎性疾病等疾病。 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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4.发明申请3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权3-异丁酰氨基酸衍生物及其作为药物的用途公开(公告)号：US20130053416A1
公开(公告)日：2013-02-28
申请号：US13559401
申请日：2012-07-26
申请人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Klaus WIRTH
发明人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Klaus WIRTH
IPC分类号： C07D271/06 , A61K31/42 , C07D263/34 , A61K31/421 , A61K31/4245 , C07D231/14 , A61K31/415 , C07D249/10 , A61K31/4196 , C07D307/68 , A61K31/341 , C07D413/04 , A61K31/4439 , C07D231/38 , C07D401/06 , A61K31/454 , A61P9/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P7/02 , A61P19/02 , A61P29/00 , A61P13/12 , A61P11/00 , A61P11/06 , A61P37/00 , A61P7/10 , A61P25/28 , C07D261/18
CPC分类号： C07D401/06 , A61K31/341 , A61K31/415 , A61K31/4164 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/454 , A61K45/06 , C07D231/14 , C07D233/90 , C07D249/10 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/10 , C07D277/32 , C07D277/56 , C07D285/08 , C07D307/68
摘要： 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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： 3-杂环酰氨基 - 丙酸衍生物及其作为药物的用途本发明涉及式I化合物，其中Ht，G，R10，R30，R40，R50和R60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。 它们是蛋白酶组织蛋白酶A的抑制剂，例如可用于治疗动脉粥样硬化，心力衰竭，肾脏疾病，肝脏疾病或炎性疾病等疾病。 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SUBSTITUTED 3-THIAZOLOAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权取代的3-噻唑烷基 - 丙酸衍生物及其作为药物的用途公开(公告)号：US20130053402A1
公开(公告)日：2013-02-28
申请号：US13559268
申请日：2012-07-26
申请人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Klaus WIRTH
发明人： Sven RUF , Josef PERNERSTORFER , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Klaus WIRTH
IPC分类号： A61K31/426 , C07D417/04 , A61K31/427 , A61K31/4439 , A61K31/497 , A61P9/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/08 , A61P7/10 , A61P7/02 , A61P29/00 , A61P19/08 , A61P13/12 , A61P11/00 , A61P11/06 , A61P37/00 , A61P3/10 , A61P25/00 , A61P25/28 , A61P13/02 , C07D277/56
CPC分类号： C07D277/54 , C07D417/04
摘要： The present invention relates to compounds of the formulae Ia and Ib, wherein G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式Ia和Ib的化合物，其中G，R10，R30，R40，R50和R60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。 它们是蛋白酶组织蛋白酶A的抑制剂，例如可用于治疗动脉粥样硬化，心力衰竭，肾脏疾病，肝脏疾病或炎性疾病等疾病。 本发明还涉及制备式Ia和Ib化合物的方法，其用途和包含它们的药物组合物。
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公开(公告)号：US20100035930A1
公开(公告)日：2010-02-11
申请号：US12480348
申请日：2009-06-08
申请人： Christopher KALLUS , Mark BROENSTRUP , Werngard CZECHTIZKY , Andreas EVERS , Markus FOLLMANN , Nis HALLAND , Herman SCHREUDER
发明人： Christopher KALLUS , Mark BROENSTRUP , Werngard CZECHTIZKY , Andreas EVERS , Markus FOLLMANN , Nis HALLAND , Herman SCHREUDER
IPC分类号： A61K31/195 , A61K31/27 , A61K31/42 , A61K31/40 , A61K31/381 , A61K31/4402 , A61K31/44 , A61K31/445 , A61P7/00 , C07C271/22 , C07C229/12 , C07D261/08 , C07D207/09 , C07D333/22 , C07D213/56 , C07D211/56
CPC分类号： A61K31/4164 , A61K31/17 , A61K31/18 , A61K31/198 , A61K31/223 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4184 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4465 , A61K45/06 , C07C307/06 , C07D207/06 , C07D209/20 , C07D211/34 , C07D211/58 , C07D213/40 , C07D213/55 , C07D213/73 , C07D235/14 , C07D261/08 , C07D295/185 , C07D317/58 , C07D333/20 , C07D487/08 , A61K2300/00
摘要： The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译： 本发明涉及本文定义的式I化合物，其为活化凝血酶可激活的纤维蛋白溶解抑制剂的抑制剂。 式I的化合物适用于制备用于预防，二次预防和治疗与血栓形成，栓塞，高凝状态或纤维变性相关的一种或多种病症的药物。
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7.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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8.发明申请SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权取代的3-异丁酰氨基酸衍生物及其作为药物的用途公开(公告)号：US20120252809A1
公开(公告)日：2012-10-04
申请号：US13357245
申请日：2012-01-24
申请人： Sven RUF , Thorsten SADOWSKI , Klaus WIRTH , Herman SCHREUDER , Christian BUNING
发明人： Sven RUF , Thorsten SADOWSKI , Klaus WIRTH , Herman SCHREUDER , Christian BUNING
IPC分类号： A61K31/44 , C07D401/12 , A61K31/506 , C07D241/28 , A61K31/4965 , C07D239/48 , A61K31/505 , C07D471/04 , A61K31/437 , C07D413/04 , A61K31/5377 , C07D241/24 , A61K31/4375 , A61P9/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P7/10 , A61P7/02 , A61P37/00 , A61P19/02 , A61P13/12 , A61P11/06 , A61P11/00 , A61P29/00 , A61P25/28 , C07D401/04 , C07D213/81
CPC分类号： C07D413/06 , C07D213/81 , C07D213/82 , C07D217/22 , C07D239/28 , C07D241/24 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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化合物，其中A，D，E，L，G，R 10，R 30，R 40，R 50和R 60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。 它们是蛋白酶组织蛋白酶A的抑制剂，例如可用于治疗动脉粥样硬化，心力衰竭，肾脏疾病，肝脏疾病或炎性疾病等疾病。 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AMINO-SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权氨基取代的3-杂环氨基甲酸衍生物及其作为药物的用途公开(公告)号：US20120232112A1
公开(公告)日：2012-09-13
申请号：US13357236
申请日：2012-01-24
申请人： Sven RUF , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Thomas OLPP , Klaus WIRTH
发明人： Sven RUF , Thorsten SADOWSKI , Georg HORSTICK , Herman SCHREUDER , Christian BUNING , Thomas OLPP , Klaus WIRTH
IPC分类号： A61K31/415 , C07D401/04 , A61K31/4439 , A61K31/454 , C07D487/04 , A61P9/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P7/02 , A61P29/00 , A61P19/02 , A61P13/12 , A61P11/08 , A61P11/00 , A61P11/06 , A61P37/00 , A61P3/10 , A61P25/00 , A61P25/28 , A61P7/10 , C07D231/38
CPC分类号： C07D231/38 , C07D275/02 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12 , C07D417/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R11, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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化合物，其中A，D，E，G，R10，R11，R30，R40，R50和R60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。 它们是蛋白酶组织蛋白酶A的抑制剂，例如可用于治疗动脉粥样硬化，心力衰竭，肾脏疾病，肝脏疾病或炎性疾病等疾病。 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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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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