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：US11427553B2

公开(公告)日：2022-08-30

申请号：US16635504

申请日：2018-08-02

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

发明人： Manuel Ellermann ,  Stefan Nikolaus Gradl ,  Charlotte Christine Kopitz ,  Martin Lange ,  Adrian Tersteegen ,  Philip Lienau ,  Christa Hegele-Hartung ,  Detlev Sülzle ,  Timothy A. Lewis ,  Heidi Greulich ,  Xiaoyun Wu ,  Matthew Meyerson ,  Alex Burgin

IPC分类号： C07D273/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  C07D491/107 ,  C07D495/10

摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, 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 diseases, 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：US20200369633A1

公开(公告)日：2020-11-26

申请号：US16635504

申请日：2018-08-02

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

发明人： Manuel Ellermann ,  Stefan Nikolaus Gradl ,  Charlotte Christine Kopitz ,  Martin Lange ,  Adrian Tersteegen ,  Philip Lienau ,  Christa Hegele-Hartung ,  Detlev Sülzle ,  Timothy A. Lewis ,  Heidi Greulich ,  Xiaoyun Wu ,  Matthew Meyerson ,  Alex Burgin

IPC分类号： C07D273/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D491/107 ,  C07D495/10 ,  C07D471/04

摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, 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 diseases, as a sole agent or in combination with other active ingredients.

公开(公告)号：US11142522B2

公开(公告)日：2021-10-12

申请号：US16480498

申请日：2018-02-01

申请人： THE BROAD INSTITUTE, INC. ,  DANA-FARBER CANCER INSTITUTE, INC. ,  BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Timothy A. Lewis ,  Xiaoyun Wu ,  Heidi Greulich ,  Matthew Meyerson ,  Manuel Ellermann ,  Philip Lienau ,  Knut Eis ,  Antje Margret Wengner ,  Charlotte Christine Kopitz ,  Martin Lange

IPC分类号： C07D413/10 ,  A61P35/02

摘要： The present invention features improved compounds, especially the compound having the structure (1). Compositions and methods of identifying patients having cancer using biomarkers (e.g., PDE3A, PDE3B, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention.

公开(公告)号：US11773070B2

公开(公告)日：2023-10-03

申请号：US17865236

申请日：2022-07-14

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

发明人： Manuel Ellermann ,  Stefan Nikolaus Gradl ,  Charlotte Christine Kopitz ,  Martin Lange ,  Adrian Tersteegen ,  Philip Lienau ,  Christa Hegele-Hartung ,  Detlev Sülzle ,  Timothy A. Lewis ,  Heidi Greulich ,  Xiaoyun Wu ,  Matthew Meyerson ,  Alex Burgin

IPC分类号： C07D273/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  C07D491/107 ,  C07D495/10

CPC分类号： C07D273/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  C07D491/107 ,  C07D495/10

摘要： The present invention provides dihydrooxydiazinone compounds of general formula (I)




in which R1, R2, R3, and R4, 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 diseases, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20200247783A1

公开(公告)日：2020-08-06

申请号：US16635513

申请日：2018-08-02

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

发明人： Manuel Ellermann ,  Stefan Nikolaus Gradl ,  Charlotte Christine Kopitz ,  Martin Lange ,  Adrian Tersteegen ,  Philip Lienau ,  Detlev Sülzle ,  Timothy Lewis ,  Heidi Greulich ,  Xiaoyun Wu ,  Matthew Meyerson

IPC分类号： C07D403/10 ,  C07D405/10 ,  C07D401/10 ,  C07D237/04 ,  C07D413/10 ,  A61P35/04

摘要： The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I):

公开(公告)号：US10966986B2

公开(公告)日：2021-04-06

申请号：US16075077

申请日：2017-02-03

申请人： BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  DANA-FARBER CANCER INSTITUTE, INC.

发明人： Timothy A. Lewis ,  Alex Burgin ,  Monica Schenone ,  Xiaoyun Wu ,  Heidi Greulich ,  Matthew Meyerson ,  Luc De Waal ,  Antje Margret Wengner ,  Knut Eis ,  Philip Lienau ,  Ulrike Sack ,  Martin Lange

IPC分类号： A61K31/5377 ,  A61K31/50 ,  C07D413/10 ,  A61P35/00

摘要： The present invention features improved Compounds, especially (I) methods of identifying patients having Cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein).

公开(公告)号：US12053476B2

公开(公告)日：2024-08-06

申请号：US17161612

申请日：2021-01-28

申请人： BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  DANA-FARBER CANCER INSTITUTE, INC.

发明人： Timothy A. Lewis ,  Alex Burgin ,  Monica Schenone ,  Xiaoyun Wu ,  Heidi Greulich ,  Matthew Meyerson ,  Luc De Waal ,  Antje Margret Wengner ,  Knut Eis ,  Philip Lienau ,  Ulrike Sack ,  Martin Lange

IPC分类号： A61K31/5377 ,  A61K31/50 ,  A61P35/00 ,  C07D413/10

CPC分类号： A61K31/5377 ,  A61K31/50 ,  A61P35/00 ,  C07D413/10

摘要： The present invention features improved compounds, especially




methods of identifying patients having cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein).

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.