公开(公告)号：US11098102B2

公开(公告)日：2021-08-24

申请号：US16709208

申请日：2019-12-10

申请人： SANOFI

发明人： Maria Mendez Perez ,  Nils Rackelmann ,  Laurent Bialy ,  Stefan Guessregen ,  Martin Will ,  Thomas Boehme ,  Ana Villar Garea ,  Marcus Hermann Korn ,  Melissa Besenius ,  Jens Riedel ,  Ulrich Werner ,  Michael Podeschwa

IPC分类号： A61K47/64 ,  C07K14/62 ,  A61K31/18

摘要： The present invention relates to a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient such as an insulin analog comprising at least one mutation relative to the parent insulin, wherein the insulin analog comprises a mutation at position B16 which is substituted with a hydrophobic amino acid and/or a mutation at position B25 which is substituted with a hydrophobic amino acid. The present invention further relates to a sulfonamide of formula (A). Moreover, the present invention relates to an insulin analog comprising at least one mutation relative to the parent insulin.

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：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：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：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：US09598410B2

公开(公告)日：2017-03-21

申请号：US14822361

申请日：2015-08-10

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： C07D221/02 ,  C07D471/04 ,  C07D471/18

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 arterial flutter.

公开(公告)号：US09550788B2

公开(公告)日：2017-01-24

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 ,  C07D207/08 ,  C07D403/12

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的取代氨基茚子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。