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：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：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：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：US11339157B1

公开(公告)日：2022-05-24

申请号：US16758018

申请日：2018-10-23

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

发明人： Stephan Siegel ,  Franziska Siegel ,  Volker Schulze ,  Markus Berger ,  Keith Graham ,  Ulrich Klar ,  Knut Eis ,  Detlev Sülzle ,  Ulf Bömer ,  Daniel Korr ,  Kirstin Petersen ,  Ursula Mönning ,  Uwe Eberspächer ,  Dieter Moosmayer ,  Matthew Meyerson ,  Heidi Greulich ,  Bethany Kaplan ,  Hassan Youssef Harb ,  Phi Manh Dinh

IPC分类号： C07D471/04 ,  A61P35/00 ,  A61K45/06

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

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：US11207320B2

公开(公告)日：2021-12-28

申请号：US15752130

申请日：2016-08-12

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

发明人： Luc De Waal ,  Matthew Meyerson ,  Heidi Greulich ,  Monica Schenone ,  Alex Burgin ,  Xiaoyun Wu ,  Ulrike Sack

IPC分类号： A61K31/50 ,  G01N33/574 ,  A61P35/00 ,  A61K9/00 ,  A61K31/519

摘要： The present invention features improved methods of identifying patients having cancer (e.g., melanoma, adenocarcinoma, lung, cervical, liver or breast cancer) using biomarkers (e.g., PDE3A, SLFN12) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., DNMDP, zardaverine, and anagrelide).

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：US20220071995A1

公开(公告)日：2022-03-10

申请号：US17530402

申请日：2021-11-18

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

发明人： Luc De Waal ,  Matthew Meyerson ,  Heidi Greulich ,  Monica Schenone ,  Alex Burgin ,  Xiaoyun Wu ,  Ulrike Sack

IPC分类号： A61K31/50 ,  G01N33/574 ,  A61P35/00 ,  A61K9/00 ,  A61K31/519

摘要： The present invention features improved methods of identifying patients having cancer (e.g., melanoma, adenocarcinoma, lung, cervical, liver or breast cancer) using biomarkers (e.g., PDE3A, SLFN12) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., DNMDP, zardaverine, and anagrelide).