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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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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：US10654818B2
公开(公告)日：2020-05-19
申请号：US15779691
申请日：2016-11-30
发明人： Markus Berger , Jan Hübner , Antonius Ter Laak , Matyas Gorjanacz , Amaury Ernesto Fernandez-Montalvan , Vincent Rodeschini , Didier Roche
IPC分类号： C07D307/52 , A61K31/341 , C07D405/12 , C07D487/10 , A61K31/397 , A61K31/4025 , A61K31/403 , A61K31/4178 , A61K31/4196 , A61K31/4525 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The invention relates to furane derivatives of formula (I) as inhibitors of ATAD2, a process for their preparation and use thereof.
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公开(公告)号：US10266548B2
公开(公告)日：2019-04-23
申请号：US15438254
申请日：2017-02-21
发明人： Marion Hitchcock , Anne Mengel , Vera Pütter , Gerhard Siemeister , Antje Margret Wengner , Hans Briem , Knut Eis , Volker Schulze , Amaury Ernesto Fernandez-Montalvan , Stefan Prechtl , Simon Holton , Jörg Fanghänel , Philip Lienau , Cornelia Preusse , Mark Jean Gnoth
IPC分类号： C07D401/14 , C07D498/04 , C07D405/14 , C07D413/14 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D403/04
摘要： Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
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公开(公告)号：US20210079018A1
公开(公告)日：2021-03-18
申请号：US16764563
申请日：2018-11-15
发明人： Steven J. Ferrara , Michael H. Serrano-Wu , Christopher Lemke , David McKinney , Mark Fitzgerald , Christopher Nasveschuk , Kiel Lazarski , Laura Furst , Guo Wei , Patrick Ryan MacCarren , Kai Thede , Anne Mengel , Clara Christ , Joachim Kuhnke , Sarah Anna Liesa Johannes , Philipp Buchgraber , Ulrich Klar , Ulrike Sack , Stefan Kaulfuss , Amaury Ernesto Fernandez-Montalvan , Nicolas Werbeck , Ursula Mönning
IPC分类号： C07D498/14 , C07D487/14 , A61P35/00
摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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 hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US11286263B2
公开(公告)日：2022-03-29
申请号：US16764563
申请日：2018-11-15
发明人： Steven James Ferrara , Michael H. Serrano-Wu , Chris Lemke , David McKinney , Mark Fitzgerald , Christopher Nasveschuk , Kiel Lazarski , Laura Furst , Guo Wei , Patrick Ryan McCarren , Kai Thede , Anne Mengel , Clara Christ , Joachim Kuhnke , Sarah Anna Liesa Johannes , Philipp Buchgraber , Ulrich Klar , Ulrike Sack , Stefan Kaulfuss , Amaury Ernesto Fernandez-Montalvan , Nicolas Werbeck , Ursula Mönning
IPC分类号： C07D487/14 , C07D403/14 , C07D498/14 , A61K31/4162 , A61P35/00
摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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 hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US10604532B2
公开(公告)日：2020-03-31
申请号：US16360811
申请日：2019-03-21
发明人： Marion Hitchcock , Anne Mengel , Vera Pütter , Gerhard Siemeister , Antje Margret Wengner , Hans Briem , Knut Eis , Volker Schulze , Amaury Ernesto Fernandez-Montalvan , Stefan Prechtl , Simon Holton , Jörg Fanghänel , Philip Lienau , Cornelia Preusse , Mark Jean Gnoth
IPC分类号： C07D401/14 , C07D498/04 , C07D405/14 , C07D413/14 , A01H6/36 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D403/04
摘要： Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
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公开(公告)号：US09745285B2
公开(公告)日：2017-08-29
申请号：US14900548
申请日：2014-06-17
发明人： Anne Mengel , Marion Hitchcock , Anja Richter , Lars Bärfacker , Hans Briem , Gerhard Siemeister , Wilhelm Bone , Amaury Ernesto Fernandez-Montalvan , Jens Schröder , Simon Holton , Cornelia Preuβe , Ursula Mönning
IPC分类号： C07D401/14 , A61K31/506 , A61K45/06 , C07D413/14
CPC分类号： C07D401/14 , A61K31/506 , A61K45/06 , C07D413/14
摘要： Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
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公开(公告)号：US11891404B2
公开(公告)日：2024-02-06
申请号：US17940617
申请日：2022-09-08
发明人： Kai Thede , Anne Mengel , Clara Christ , Joachim Kuhnke , Sarah Anna Liesa Johannes , Philipp Buchgraber , Ulrich Klar , Ulrike Rauh , Stefan Kaulfuss , Amaury Ernesto Fernandez-Montalvan , Nicolas Werbeck , Ursula Moenning , Katrin Nowak-Reppel , Sven Wittrock , David McKinney , Michael H. Serrano-Wu , Chris Lemke , Mark Fitzgerald , Christopher Nasveschuk , Kiel Lazarski , Steven James Ferrara , Laura Furst , Guo Wei , Patrick Ryan McCarren , Rebecca Ann Harvey
IPC分类号： C07D498/14 , A61P35/02 , A61P35/00 , A61K31/4162 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D471/22 , C07D487/14 , C07D487/22 , C07D498/22
CPC分类号： C07D498/14 , A61K31/4162 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P35/00 , A61P35/02 , C07D471/22 , C07D487/14 , C07D487/22 , C07D498/22
摘要： The present invention relates to substituted macrocyclic indole derivatives of general formula (I):
in which R1, R2, R3, R4, R5, R6, A and L 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 hyperproliferative disorders, as a sole agent or in combination with other active ingredients.-
公开(公告)号：US20230112244A1
公开(公告)日：2023-04-13
申请号：US17940617
申请日：2022-09-08
发明人： Kai Thede , Anne Mengel , Clara Christ , Joachim Kuhnke , Sarah Anna Liesa Johannes , Philipp Buchgraber , Ulrich Klar , Ulrike Rauh , Stefan Kaulfuss , Amaury Ernesto Fernandez-Montalvan , Nicolas Werbeck , Ursula Moenning , Katrin Nowak-Reppel , Sven Wittrock , David McKinney , Michael H. Serrano-Wu , Chris Lemke , Mark Fitzgerald , Christopher Nasveschuk , Kiel Lazarski , Steven James Ferrara , Laura Furst , Guo Wei , Patrick Ryan McCarren , Rebecca Ann Harvey
IPC分类号： C07D498/14 , A61P35/02 , A61P35/00 , A61K31/4162 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D471/22 , C07D487/14 , C07D487/22 , C07D498/22
摘要： The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L 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 hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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