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：US20230339939A1

公开(公告)日：2023-10-26

申请号：US18018221

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 ,  v 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 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

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

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：US20230046077A1

公开(公告)日：2023-02-16

申请号：US17428730

申请日：2020-02-06

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

发明人： Volker Schulze ,  Anne Mengel ,  Jens Schroeder ,  Adelaide Clara Faria Alvares De Lemos ,  Wilhelm Bone ,  Ulf Bomer ,  Detlev Sulzle ,  Clara Christ ,  Roman Hillig ,  Christian Lechner ,  Steven Corsello ,  Kasia Handing ,  Alisha Caliman ,  Ulrike Rauh ,  Stefan Kaulfuss ,  Jérémie Mortier

IPC分类号： C07D471/04 ,  A61P35/00

摘要： The present invention relates to compounds of formula (I) processes for their production and their use as pharmaceuticals. The compounds are inhibitors of Casein kinase 1 alpha and/or delta (CSNK1α and/or β) useful for the treatment of proliferative disorders.

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.

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：US20230365554A1

公开(公告)日：2023-11-16

申请号：US18018148

申请日：2021-07-27

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  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 ,  Jeremie Xavier G. Mortier ,  Detlev Sülzle ,  Stefan Kaulfuss ,  Steven Corsello ,  Katarzyna Handing ,  Alisha Caliman ,  Amael Madec

IPC分类号： C07D471/04 ,  A61P35/00

CPC分类号： C07D471/04 ,  A61P35/00

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

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.