公开(公告)号：US09120783B2

公开(公告)日：2015-09-01

申请号：US14202804

申请日：2014-03-10

申请人： SANOFI

发明人： Sven Ruf ,  Thorsten Sadowski ,  Klaus Wirth ,  Herman Schreuder ,  Christian Buning

IPC分类号： C07D213/46 ,  C07D413/06 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D239/28 ,  C07D241/24

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.

公开(公告)号：US20140330009A1

公开(公告)日：2014-11-06

申请号：US14342744

申请日：2011-09-16

申请人： SANOFI

发明人： Laurent Bialy ,  Katrin Lorenz ,  Klaus Wirth ,  Klaus Steinmeyer ,  Gerhard Hessler ,  Josef Pernerstorfer ,  Joachim Brendel

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D471/18

摘要： The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

摘要翻译： 本发明涉及式（I）的取代的4,5,6,7-四氢-1H-吡唑并[4,3-c]吡啶，它们作为药物的用途，以及包含它们的药物制剂。 式（I）化合物作用于TASK-1钾通道。 该化合物特别适用于治疗或预防房性心律失常，例如房颤（AF）或心房扑动。

公开(公告)号：US20140296296A1

公开(公告)日：2014-10-02

申请号：US14227679

申请日：2014-03-27

申请人： SANOFI

发明人： Sven Ruf ,  Thorsten Sadowski ,  Klaus Wirth ,  Herman Schreuder ,  Christian Buning ,  Christopher Kallus ,  Hartmut Strobel ,  Hermut Wehlan

IPC分类号： C07D271/10 ,  C07D413/14 ,  C07D413/10 ,  C07D277/30 ,  C07D263/32

CPC分类号： C07D271/10 ,  C07D263/32 ,  C07D277/30 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 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X，R，R1，R2，D，E1，E2，E3，E4，G1，G2，G3和G4具有权利要求书中所示的含义， 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：US09884860B2

公开(公告)日：2018-02-06

申请号：US15041541

申请日：2016-02-11

申请人： SANOFI

发明人： Laurent Bialy ,  Katrin Lorenz ,  Klaus Wirth ,  Klaus Steinmeyer ,  Gerhard Hessler

IPC分类号： A61K31/5383 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates in fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.

公开(公告)号：US20150018342A1

公开(公告)日：2015-01-15

申请号：US14375273

申请日：2013-02-01

申请人： SANOFI

发明人： Laurent Bialy ,  Katrin Lorenz ,  Klaus Wirth ,  Klaus Steinmeyer ,  Gerhard Hessler

IPC分类号： C07D513/04 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.

摘要翻译： 本发明涉及式（I）的稠合吡咯烷二酰胺，其中R 1至R 9，X，m和n如权利要求中所定义。 式（I）化合物是酸敏感性钾通道TASK-1的抑制剂，适用于治疗TASK-1通道介导的疾病如心律不齐，特别是心房颤动或心房扑动等房性心律失常，呼吸 障碍，特别是睡眠呼吸障碍，例如睡眠呼吸暂停。

公开(公告)号：US20240124408A1

公开(公告)日：2024-04-18

申请号：US18267644

申请日：2021-12-16

申请人： Sanofi

发明人： Paul Justin Mueller ,  Florian Auger ,  Guillaume Begis ,  Yann Foricher ,  Christoph Grebner ,  Stéphane Hourcade ,  Stéphanie Meyfroot ,  Sven Ruf ,  Klaus Wirth

IPC分类号： C07D305/06 ,  A61P11/04 ,  C07C235/40 ,  C07C237/12

CPC分类号： C07D305/06 ,  A61P11/04 ,  C07C235/40 ,  C07C237/12

摘要： Compounds of formula (1):




wherein R1 represents a —C(R2)(R3)—[C(R4)(R5)]m-L-R6 group or —R7; and the preparation and the therapeutic uses of the compounds of formula (1) as agonists of TRPM8 receptors, useful especially in the treatment of oropharyngeal dysphagia.

公开(公告)号：US09284333B2

公开(公告)日：2016-03-15

申请号：US14375273

申请日：2013-02-01

申请人： SANOFI

发明人： Laurent Bialy ,  Katrin Lorenz ,  Klaus Wirth ,  Klaus Steinmeyer ,  Gerhard Hessler

IPC分类号： C07D513/04 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D471/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.

摘要翻译： 本发明涉及式（I）的稠合吡咯烷二酰胺，其中R 1至R 9，X，m和n如权利要求中所定义。 式（I）化合物是酸敏感性钾通道TASK-1的抑制剂，适用于治疗TASK-1通道介导的疾病如心律不齐，特别是心房颤动或心房扑动等房性心律失常，呼吸 障碍，特别是睡眠呼吸障碍，例如睡眠呼吸暂停。

公开(公告)号：US09150526B2

公开(公告)日：2015-10-06

申请号：US14227679

申请日：2014-03-27

申请人： SANOFI

发明人： Sven Ruf ,  Thorsten Sadowski ,  Klaus Wirth ,  Herman Schreuder ,  Christian Buning ,  Christopher Kallus ,  Hartmut Strobel ,  Hermut Wehlan

IPC分类号： C07D271/10 ,  C07D413/06 ,  C07D413/04 ,  C07D413/10 ,  C07D263/32 ,  C07D277/30 ,  C07D413/14

CPC分类号： C07D271/10 ,  C07D263/32 ,  C07D277/30 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 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X，R，R1，R2，D，E1，E2，E3，E4，G1，G2，G3和G4具有权利要求中所示的含义， 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：US20140349986A1

公开(公告)日：2014-11-27

申请号：US14339957

申请日：2014-07-24

申请人： SANOFI

发明人： Nils Rackelmann ,  Laurent Bialy ,  Heinrich Englert ,  Klaus Wirth ,  Petra Arndt ,  John Weston ,  Uwe Heinelt ,  Markus Follmann

IPC分类号： C07D487/10 ,  C07D487/04 ,  C07D401/12 ,  C07D211/56 ,  C07D411/12 ,  C07D413/12 ,  C07D405/12 ,  C07D403/04 ,  C07D205/04 ,  C07D243/08 ,  C07D487/08 ,  C07D417/12

CPC分类号： C07D487/10 ,  C07D205/04 ,  C07D207/08 ,  C07D211/56 ,  C07D243/08 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D487/08

摘要： The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

摘要翻译： 本发明涉及式I的取代氨基茚满及其类似物及其药学用途。 包含这种类型化合物的药物适用于预防或治疗多种疾病，例如呼吸系统疾病，囊性纤维化疾病，急性或慢性肾脏疾病或排便障碍。

公开(公告)号：US20140296239A1

公开(公告)日：2014-10-02

申请号：US14227737

申请日：2014-03-27

申请人： SANOFI

发明人： Sven Ruf ,  Thorsten Sadowski ,  Klaus Wirth ,  Herman Schreuder ,  Christian Buning ,  Christopher Kallus ,  Hartmut Strobel ,  Hermut Wehlan

IPC分类号： C07D263/32 ,  C07D413/14 ,  C07D413/10 ,  C07D417/10 ,  C07D277/30 ,  C07D271/10

CPC分类号： C07D263/32 ,  C07D271/10 ,  C07D277/30 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

摘要： The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 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X，R，R1，R2，D，E1，E2，E3，E4，G1，G2，G3和G4具有权利要求中所示的含义， 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。