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公开(公告)号：US20190177279A1
公开(公告)日：2019-06-13
申请号：US16211486
申请日：2018-12-06
发明人： Stefan Bäurle , Jens Nagel , Andrea Rotgeri , Adam James Davenport , Christopher Charles Stimson
IPC分类号： C07D231/12 , C07D213/55 , A61P29/00
摘要： The present invention relates to carboxylic acid aromatic 1,2-cyclopropylamides of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20190177284A1
公开(公告)日：2019-06-13
申请号：US16211572
申请日：2018-12-06
发明人： Stefan Bäurle , Jens Nagel , Andrea Rotgeri , Adam James Davenport , Christopher Charles Stimson
IPC分类号： C07D257/04 , C07D405/12 , C07D401/12
摘要： The present invention relates to tetrazolyl-containing cyclopropanecarboxamides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US09890147B2
公开(公告)日：2018-02-13
申请号：US14421994
申请日：2013-08-13
发明人： Stephan Siegel , Stefan Bäurle , Arwed Cleve , Bernard Haendler , Amaury Ernesto Fernandez-Montalvan , Ursula Mönning , Sabine Krause , Pascale Lejeune , Norbert Schmees , Matthias Busemann , Simon Holton , Joachim Kuhnke
IPC分类号： A61K31/551 , C07D243/02 , C07D401/04 , C07D403/04 , C07D417/10 , C07D401/14 , C07D413/14 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , A61K31/5513
CPC分类号： C07D417/10 , A61K31/551 , A61K31/5513 , C07D243/02 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D413/14
摘要： What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
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公开(公告)号：US12023319B2
公开(公告)日：2024-07-02
申请号：US17478192
申请日：2021-09-17
发明人： Stefan Bäurle , Adam James Davenport , Christopher Stimson , Jens Nagel , Nicole Schmidt , Andrea Rotgeri , Ina Gröticke , Alexandra Rausch , Juergen Klar , Thomas Dyrks
IPC分类号： A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4164 , A61K31/426 , A61K31/4365 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61P3/04 , A61P3/10 , A61P13/10 , A61P19/02 , A61P25/02 , A61P29/00 , A61P35/00 , C07D213/56 , C07D231/12 , C07D231/56 , C07D233/64 , C07D241/12 , C07D277/56 , C07D333/28 , C07D333/38 , C07D333/58 , C07D405/04 , C07D495/04
CPC分类号： A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4164 , A61K31/426 , A61K31/4365 , A61K31/4418 , A61K31/4439 , A61K31/4965 , A61P3/04 , A61P3/10 , A61P13/10 , A61P19/02 , A61P25/02 , A61P29/00 , A61P35/00 , C07D213/56 , C07D231/12 , C07D231/56 , C07D233/64 , C07D241/12 , C07D277/56 , C07D333/28 , C07D333/38 , C07D333/58 , C07D405/04 , C07D495/04
摘要： The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20190194148A1
公开(公告)日：2019-06-27
申请号：US16211456
申请日：2018-12-06
发明人： Stefan Bäurle , Jens Nagel , Andrea Rotgeri , Adam James Davenport , Christopher Charles Stimson
IPC分类号： C07D257/04 , C07D403/12 , C07D401/10 , C07D409/10 , C07D401/14
CPC分类号： C07D257/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D409/10
摘要： The present invention relates to N-(tetrazolylaryl) amide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20150203483A1
公开(公告)日：2015-07-23
申请号：US14421994
申请日：2013-08-13
发明人： Stephan Siegel , Stefan Bäurle , Arwed Cleve , Bernard Haendler , Amaury Ernesto Fernandiez-Montalvan , Ursula Mönning , Sabine Krause , Pascale Lejeune , Norbert Schmees , Matthias Busemann , Simon Holton , Joachim Kuhnke
IPC分类号： C07D417/10 , A61K31/551 , C07D413/10 , C07D403/10 , C07D413/14 , C07D409/10 , C07D401/04 , C07D401/14 , A61K31/5513 , C07D401/12 , C07D243/02 , C07D401/10
CPC分类号： C07D417/10 , A61K31/551 , A61K31/5513 , C07D243/02 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/14 , C07D409/10 , C07D413/04 , C07D413/10 , C07D413/14
摘要： What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
摘要翻译： 描述了通式（I）的BET蛋白抑制性特别是BRD4抑制性2,3-苯二氮卓类，其中R1a，R1b，R1c，R2，R3，R4，R5，A和X具有 描述，用于制备根据本发明的化合物的中间体，包含根据本发明的化合物的药物组合物及其对过度增殖性疾病，特别是肿瘤病症的预防和治疗用途。 还描述了BET蛋白抑制剂用于良性增生，动脉粥样硬化性疾病，败血症，自身免疫性疾病，血管病症，病毒感染，神经变性疾病，炎症性疾病，动脉粥样硬化性疾病和用于控制雄性生育力的用途。
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