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：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：US20230322767A1

公开(公告)日：2023-10-12

申请号：US18018207

申请日：2021-07-27

申请人： Bayer Aktiengesellschaft ,  The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc.

发明人： Volker Schulze ,  Anne Mengel ,  Adelaide Clara Faria Alvares De Lemos ,  Ulrike Rauh ,  Ulf Bömer ,  Roman Hillig ,  Christian Lechner ,  Jérémie Xavier Mortier ,  Stefan Kaulfuss ,  Steven Corsello ,  Katarzyna Handing ,  Amael Madec ,  Laura Furst ,  Mrinal Shekhar ,  David McKinney

IPC分类号： C07D471/04 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K45/06

摘要： Compounds of formula (I), process for their production and their use as pharmaceuticals.

公开(公告)号：US20220289762A1

公开(公告)日：2022-09-15

申请号：US17612019

申请日：2020-05-15

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

发明人： Kai Thede ,  Sven Wittrock ,  Anne Mengel ,  David McKinney ,  Christopher Lemke ,  Steven J. Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick R. McCarren

IPC分类号： C07D498/16 ,  C07D403/04

摘要： The present invention relates to methods of preparing substituted indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, and intermediate compounds useful for preparing said compounds. These compounds are useful 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：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：US20230391769A1

公开(公告)日：2023-12-07

申请号：US18018216

申请日：2021-07-27

申请人： Bayer Aktiengesellschaft ,  The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc.

发明人： Volker Schulze ,  Anne Mengel ,  Adelaide Clara Faria Alvares De Lemos ,  Sven Christian ,  Ulf Bömer ,  Roman Hillig ,  Christian Lechner ,  Jérémie Xavier Mortier ,  Stefan Kaulfuss ,  Steven Corsello ,  Katarzyna Handing ,  Amael Madec ,  Laura Furst ,  Mrinal Shekhar ,  Markus Berger ,  Rajesha Rupaimoole ,  Philip Lienau ,  Douglas Orsi ,  David McKinney ,  Krzysztof Brezezinka

IPC分类号： C07D471/04 ,  C07D401/06 ,  C07F7/08 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D401/06 ,  C07F7/0812 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  A61P35/00

摘要： Compounds of formula (I), process for their production and their use as pharmaceuticals.

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.