公开(公告)号：US20210292341A1

公开(公告)日：2021-09-23

申请号：US16764672

申请日：2018-11-15

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

发明人： Laura Furst ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  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 ,  Katrin Nowak-Reppel

IPC分类号： C07D513/14 ,  A61K31/5377 ,  A61K31/4162 ,  A61K31/454 ,  A61K45/06 ,  A61P35/02 ,  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：US20210269456A1

公开(公告)日：2021-09-02

申请号：US16764668

申请日：2018-11-15

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 Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Katrin Nowak-Reppel ,  Sven Wittrock ,  David McKinney ,  Michael H. Serrano-Wu ,  Christopher 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 ,  A61K31/4162 ,  A61K31/5377 ,  C07D498/22 ,  C07D487/14 ,  C07D471/22 ,  C07D487/22 ,  A61P35/00 ,  A61P35/02 ,  A61K45/06 ,  A61K31/496 ,  A61K31/437

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：US09890147B2

公开(公告)日：2018-02-13

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 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.

公开(公告)号：US11492358B1

公开(公告)日：2022-11-08

申请号：US17186820

申请日：2021-02-26

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 Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Philip Lienau ,  Ulrike Sack ,  Arne Scholz ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick Ryan McCarren

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

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：US11478451B1

公开(公告)日：2022-10-25

申请号：US16764565

申请日：2018-11-15

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 ,  Chris Lemke ,  Michael H. Serrano-Wu ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven J. Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick R. McCarren ,  Rebecca Ann Harvey ,  Daniel Payne ,  Thomas Pesnot ,  Craig Wilson

IPC分类号： A61K31/4162 ,  A61K45/06 ,  A61P35/00 ,  A61K31/496 ,  C07D487/18 ,  A61K31/5377 ,  C07D498/18

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：US11447504B2

公开(公告)日：2022-09-20

申请号：US16764675

申请日：2018-11-15

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 ,  Jérémie Xavier Mortier ,  Patrick R. McCarren ,  Michael H. Serrano-Wu ,  Chris Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven J. Ferrara ,  Laura Furst ,  Guo Wei ,  Rebecca Ann Harvey ,  Daniel Payne ,  Thomas Pesnot ,  Craig Wilson

IPC分类号： C07D498/14 ,  A61K45/06 ,  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.

公开(公告)号：US11440923B2

公开(公告)日：2022-09-13

申请号：US16764668

申请日：2018-11-15

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 Mönning ,  Katrin Nowak-Reppel ,  Sven Wittrock ,  David McKinney ,  Michael H. Serrano-Wu ,  Chris Lemke ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven J. Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick R. 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：US20210277022A1

公开(公告)日：2021-09-09

申请号：US16764675

申请日：2018-11-15

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 Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Katrin Nowak-Reppel ,  Jeremie Xavier Mortier ,  Patrick Ryan McCarren ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Laura Furst ,  Guo Wei ,  Rebecca Ann Flarvey ,  Daniel Payne ,  Thomas Pesnot ,  Craig Wilson

IPC分类号： C07D498/14 ,  C07D487/14 ,  A61K45/06

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：US20210253598A1

公开(公告)日：2021-08-19

申请号：US16764560

申请日：2018-11-15

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 Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Steven James Ferrara ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Laura Furst ,  Guo Wei ,  Patrick Ryan MacCarren ,  Rebecca Ann Harvey ,  Craig Wilson

IPC分类号： C07D498/14 ,  A61K45/06 ,  C07D498/22 ,  A61K31/437 ,  A61K31/4162 ,  A61K31/4985 ,  C07D487/14 ,  A61K31/424 ,  A61P35/00 ,  A61P35/02

摘要： The present invention relates to aryl annulated 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：US10981932B2

公开(公告)日：2021-04-20

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 ,  C07D498/06 ,  C07D498/22 ,  C07D487/16

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 2019 compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.