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。

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.

公开(公告)号：US20200087322A1

公开(公告)日：2020-03-19

申请号：US16301871

申请日：2017-05-17

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  The Broad Institute, Inc.

发明人： Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Clara Christ ,  Kai Thede ,  Joachim Kuhnke ,  Manfred Moewes ,  Knut Eis ,  Amaury Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Moenning ,  Philip Lienau ,  Ulrike Sack ,  Arne Scholz ,  Michael H. Serrano-Wu ,  Chris Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick R. McCarren

IPC分类号： C07D498/16 ,  C07D487/16 ,  C07D498/22 ,  C07D498/06

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.

公开(公告)号：US11286263B2

公开(公告)日：2022-03-29

申请号：US16764563

申请日：2018-11-15

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

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.

公开(公告)号：US20140288035A1

公开(公告)日：2014-09-25

申请号：US14356165

申请日：2012-11-02

申请人： Bayer Intellectual Property Gmbh ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Jan Hübner ,  Rolf Bohlmann ,  Isabella Gashaw ,  Oliver Martin Fischer ,  Joachim Kuhnke ,  Norbert Gallus ,  Reinhard Nubbemeyer ,  Ildiko Terebesi

IPC分类号： C07J53/00 ,  A61K31/585

CPC分类号： C07J53/007 ,  A61K31/585

摘要： The present invention relates to 18-methyl-6,7-methylene-17-pregn-4-ene-21,17β-carbolactones of general formula I wherein the 6,7-methylene group can be in α- or β position, pharmaceutical preparations containing at least one isomer of formula I and use thereof in the treatment of endometriosis.

摘要翻译： 本发明涉及通式I的18-甲基-6,7-亚甲基-17-孕-4-烯-21,17-二碳代内酯，其中该6,7-亚甲基可以是α-或β- 位置，含有至少一种式I异构体的药物制剂及其用于治疗子宫内膜异位症的用途。

公开(公告)号：US20210079018A1

公开(公告)日：2021-03-18

申请号：US16764563

申请日：2018-11-15

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

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.

公开(公告)号：US20150203483A1

公开(公告)日：2015-07-23

申请号：US14421994

申请日：2013-08-13

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

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。

公开(公告)号：US11891404B2

公开(公告)日：2024-02-06

申请号：US17940617

申请日：2022-09-08

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  The Broad Institute, Inc.

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

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  The Broad Institute, Inc.

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.

公开(公告)号：US20220281891A1

公开(公告)日：2022-09-08

申请号：US17691862

申请日：2022-03-10

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Steven J. 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 Rauh ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning

IPC分类号： C07D498/14 ,  A61P35/00 ,  C07D487/14

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.