公开(公告)号：US20130046004A1

公开(公告)日：2013-02-21

申请号：US13575008

申请日：2011-01-26

Applicant: Sven Ruf ,  Josef Pernerstorfer ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Bodo Scheiper ,  Klaus Wirth

Inventor： Sven Ruf ,  Josef Pernerstorfer ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Bodo Scheiper ,  Klaus Wirth

IPC: C07D231/22 ,  C07C229/08 ,  A61K31/216 ,  C07D405/12 ,  A61K31/4155 ,  C07D403/12 ,  A61P9/10 ,  A61P9/00 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P37/00 ,  A61P7/10 ,  A61P25/28 ,  A61P13/12 ,  A61P7/02 ,  A61P19/02 ,  A61K31/4152

CPC classification number: C07C229/36 ,  C07D231/20 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08674121B2

公开(公告)日：2014-03-18

申请号：US13321754

申请日：2010-05-26

Applicant: Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

Inventor： Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

IPC: C07D307/80

CPC classification number: C07D307/80 ,  C07C205/45

Abstract: A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.

Abstract translation: 通过2-（2-羟基-5-硝基苯基）-1-芳基乙酰胺的酰化生产2-烷基-3-芳酰基-5-硝基苯并呋喃的方法，随后用碱和质子酸的组合处理酯 或路易斯酸。 该方法可用于生产决奈达隆。 此外，还提供了制备决奈达隆的新型中间体。

公开(公告)号：US08962671B2

公开(公告)日：2015-02-24

申请号：US13357236

申请日：2012-01-24

Applicant: Sven Ruf ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Klaus Wirth

Inventor： Sven Ruf ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Klaus Wirth

IPC: A61K31/4155 ,  C07D231/38 ,  C07D275/02 ,  C07D401/12 ,  C07D403/04 ,  C07D401/04 ,  C07D403/06 ,  C07D405/12 ,  C07D417/04 ,  C07D487/04

CPC classification number: C07D231/38 ,  C07D275/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D417/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08664257B2

公开(公告)日：2014-03-04

申请号：US13575008

申请日：2011-01-26

Applicant: Sven Ruf ,  Josef Pernerstorfer ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Bodo Scheiper ,  Klaus Wirth

Inventor： Sven Ruf ,  Josef Pernerstorfer ,  Thorsten Sadowski ,  Georg Horstick ,  Herman Schreuder ,  Christian Buning ,  Thomas Olpp ,  Bodo Scheiper ,  Klaus Wirth

IPC: C07D231/20 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12

CPC classification number: C07C229/36 ,  C07D231/20 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120232112A1

公开(公告)日：2012-09-13

申请号：US13357236

申请日：2012-01-24

Applicant: Sven RUF ,  Thorsten SADOWSKI ,  Georg HORSTICK ,  Herman SCHREUDER ,  Christian BUNING ,  Thomas OLPP ,  Klaus WIRTH

Inventor： Sven RUF ,  Thorsten SADOWSKI ,  Georg HORSTICK ,  Herman SCHREUDER ,  Christian BUNING ,  Thomas OLPP ,  Klaus WIRTH

IPC: 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 classification number: C07D231/38 ,  C07D275/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D417/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120065411A1

公开(公告)日：2012-03-15

申请号：US13321754

申请日：2010-05-26

Applicant: Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

Inventor： Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

IPC: C07D307/80 ,  C07C205/45 ,  C07C201/12 ,  C07C205/43

CPC classification number: C07D307/80 ,  C07C205/45

Abstract: A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.

Abstract translation: 通过2-（2-羟基-5-硝基苯基）-1-芳基乙酰胺的酰化生产2-烷基-3-芳酰基-5-硝基苯并呋喃的方法，随后用碱和质子酸的组合处理酯 或路易斯酸。 该方法可用于生产决奈达隆。 此外，还提供了制备决奈达隆的新型中间体。

公开(公告)号：US20140128616A1

公开(公告)日：2014-05-08

申请号：US14151951

申请日：2014-01-10

Applicant: Sven RUF ,  Josef PERNERSTORFER ,  Thorsten SADOWSKI ,  Georg HORSTICK ,  Herman SCHREUDER ,  Christian BUNING ,  Thomas OLPP ,  Bodo SCHEIPER ,  Klaus WIRTH

Inventor： Sven RUF ,  Josef PERNERSTORFER ,  Thorsten SADOWSKI ,  Georg HORSTICK ,  Herman SCHREUDER ,  Christian BUNING ,  Thomas OLPP ,  Bodo SCHEIPER ,  Klaus WIRTH

IPC: C07D231/22 ,  C07C229/36

CPC classification number: C07C229/36 ,  C07D231/20 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20130172248A1

公开(公告)日：2013-07-04

申请号：US13734413

申请日：2013-01-04

Applicant: Elisabeth DEFOSSA ,  Viktoria DIETRICH ,  Thomas KLABUNDE ,  Stefanie KEIL ,  Siegfried STENGELIN ,  Guido HASCHKE ,  Andreas HERLING ,  Johanna KUHLMANN-GOTTKE ,  Stefan BARTOSCHEK ,  Simon GESSLER ,  Angela DUDDA ,  Guenter BILLEN ,  Thomas OLPP ,  Joerg RIEKE-ZAPP

Inventor： Elisabeth DEFOSSA ,  Viktoria DIETRICH ,  Thomas KLABUNDE ,  Stefanie KEIL ,  Siegfried STENGELIN ,  Guido HASCHKE ,  Andreas HERLING ,  Johanna KUHLMANN-GOTTKE ,  Stefan BARTOSCHEK ,  Simon GESSLER ,  Angela DUDDA ,  Guenter BILLEN ,  Thomas OLPP ,  Joerg RIEKE-ZAPP

IPC: C07C233/56 ,  A61K38/28 ,  C07C231/02 ,  C07C229/42 ,  A61K31/196 ,  A61K45/06

CPC classification number: C07C233/56 ,  A61K31/196 ,  A61K38/28 ,  A61K45/06 ,  C07C229/42 ,  C07C231/02 ,  A61K2300/00

Abstract: The invention relates to 3-[4-(phenylaminooxalylamino)phenyl]hex-4-ynoic acids, and to physiologically compatible salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3 and R4 are each defined as specified, and to physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

Abstract translation: 本发明涉及3- [4-（苯基氨基草酰氨基）苯基]己-4-炔酸，以及其生理上相容的盐。 本发明涉及式Ⅰ化合物，其中R 1，R 2，R 3和R 4各自定义和其生理上相容的盐。 该化合物适用于例如治疗糖尿病。