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公开(公告)号：US09663523B2
公开(公告)日：2017-05-30
申请号：US14432158
申请日：2013-09-25
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , Helga Künzer , Klara Muno , Erich Künzer , Martin Künzer , Christel Bernsdorf
发明人： Norbert Schmees , Joachim Kuhnke , Bernard Haendler , Roland Neuhaus , Pascale Lejeune , Stephan Siegel , Martin Krüger , Amaury Ernesto Fernandez-Montalvan , Hermann Künzer , Daniel Gallenkamp
IPC分类号： A61K31/55 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/55 , C07D519/00
摘要： The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.
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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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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：US20150299201A1
公开(公告)日：2015-10-22
申请号：US14432158
申请日：2013-09-25
申请人： Helga Künzer , Klara Muno , Erich Künzer , Martin Künzer , Christel Bernsdorf , BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Norbert Schmees , Joachim Kuhnke , Bernard Haendler , Roland Neuhaus , Pascale Lejeune , Stephan Siegel , Martin Krüger , Amaury Ernesto Fernandez-Montalvan , Hermann Künzer , Daniel Gallenkamp
IPC分类号： C07D487/04 , C07D519/00 , A61K31/55
CPC分类号： C07D487/04 , A61K31/55 , C07D519/00
摘要： The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.
摘要翻译： 本发明涉及通式（I）中具有通式（I）给出的含义的具有通式（I）的BRD4抑制性5-芳基三氮杂吖庚因的药物组合物 包括根据本发明的化合物，以及用于过度增殖性疾病，特别是对于肿瘤性疾病的预防和治疗用途。 本发明还涉及BET蛋白抑制剂在病毒感染，神经变性疾病，炎性疾病，动脉粥样硬化疾病和雄性生育调控中的用途。
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![4H-pyrrolo[3,2-c]pyridin-4-one derivatives](/abs-image/US/2022/05/24/US11339157B1/abs.jpg.150x150.jpg)
公开(公告)号：US11339157B1
公开(公告)日：2022-05-24
申请号：US16758018
申请日：2018-10-23
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft , Dana-Farber Cancer Institute, Inc. , The Broad Institute, Inc.
发明人： Stephan Siegel , Franziska Siegel , Volker Schulze , Markus Berger , Keith Graham , Ulrich Klar , Knut Eis , Detlev Sülzle , Ulf Bömer , Daniel Korr , Kirstin Petersen , Ursula Mönning , Uwe Eberspächer , Dieter Moosmayer , Matthew Meyerson , Heidi Greulich , Bethany Kaplan , Hassan Youssef Harb , Phi Manh Dinh
IPC分类号： C07D471/04 , A61P35/00 , A61K45/06
摘要： Compounds of formula (I) processes for their production and their use as pharmaceuticals.
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公开(公告)号：US11161825B2
公开(公告)日：2021-11-02
申请号：US16638683
申请日：2018-08-09
发明人： Jörg Weiske , Carlo Stresemann , Stefan Nikolaus Gradl , Ulrike Röhn , Clara Christ , Holger Steuber , Manfred Husemann , Norbert Schmees , Kai Thede , Stephan Siegel , Antonius Ter Laak
IPC分类号： C07D243/12 , C07D401/06 , C07D403/06 , C07D409/06 , C07D413/06
摘要： The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.
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