公开(公告)号：US11130745B2

公开(公告)日：2021-09-28

申请号：US16996721

申请日：2020-08-18

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Müller ,  Sherif El Sheikh ,  David B. Sykes ,  Steven James Ferrara ,  Michael Kröber ,  Claudia Merz ,  Michael Niehues ,  Martina Schäfer ,  Katja Zimmermann ,  Carl Friedrich Nising

IPC分类号： A61P35/00 ,  A61K45/06 ,  C07D401/12 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 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：US10815215B2

公开(公告)日：2020-10-27

申请号：US16345168

申请日：2017-10-25

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Müller ,  Sherif El Sheikh ,  Han Jie Zhou ,  Changjia Zhao ,  David B. Sykes ,  Steven James Ferrara ,  Kery Liu ,  Michael Kröber ,  Claudia Merz ,  Michael Niehues ,  Martina Schäfer ,  Katja Zimmermann ,  Carl Friedrich Nising

IPC分类号： C07D401/12 ,  A61P35/00 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K45/06

摘要： The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 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：US11787797B2

公开(公告)日：2023-10-17

申请号：US17161615

申请日：2021-01-28

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Mueller ,  Sherif El Sheikh ,  Han Jie Zhou ,  Changjia Zhao ,  David B. Sykes ,  Steven James Ferrara ,  Kery Liu ,  Simon Anthony Herbert ,  Claudia Merz ,  Michael Niehues ,  Carl Friedrich Nising ,  Martina Schäfer ,  Katja Zimmermann ,  Jörg Knäblein ,  Kai Thede ,  Thomas Faupel

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18

CPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18 ,  C12P17/182 ,  C12P17/188

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




in which R1, R2, R3, R4 and R5 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：US11713304B2

公开(公告)日：2023-08-01

申请号：US17407951

申请日：2021-08-20

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Müller ,  Sherif El Sheikh ,  David B. Sykes ,  Steven James Ferrara ,  Michael Kröber ,  Claudia Merz ,  Michael Niehues ,  Martina Schäfer ,  Katja Zimmermann ,  Carl Friedrich Nising

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K45/06

CPC分类号： C07D401/12 ,  A61P35/00 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K45/06

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




in which R1, R2, R3, R4, and R5 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 and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US10968216B2

公开(公告)日：2021-04-06

申请号：US16345178

申请日：2017-10-25

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Mueller ,  Sherif El Sheikh ,  Han Jie Zhou ,  Changjia Zhao ,  David B. Sykes ,  Steven James Ferrara ,  Kery Liu ,  Simon Anthony Herbert ,  Claudia Merz ,  Michael Niehues ,  Carl Friedrich Nising ,  Martina Schäfer ,  Katja Zimmermann ,  Jörg Knäblein ,  Kai Thede ,  Thomas Faupel

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18

摘要： The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 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：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：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：US20210032212A1

公开(公告)日：2021-02-04

申请号：US17046143

申请日：2019-04-03

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Jorma Hassfeld ,  Stefan Nikolaus Gradl ,  Philipp Rubenbauer ,  Henricus Nicolaas Sebastiaan VAN DER HAAS ,  Reinerus Gerardus GIELING

IPC分类号： C07D249/12 ,  C07D405/12

摘要： The present invention provides methods for the preparation of Compound (I): Compound (I), the use of intermediates for the preparation of said compound and its crystalline form A.