公开(公告)号：US20220396554A1

公开(公告)日：2022-12-15

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

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：US20240182452A1

公开(公告)日：2024-06-06

申请号：US18399092

申请日：2023-12-28

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 ,  A61P35/04 ,  C07D237/04 ,  C07D401/10 ,  C07D405/10 ,  C07D413/10

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

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






in which R1, R2 and R3 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：US20230017200A1

公开(公告)日：2023-01-19

申请号：US17862255

申请日：2022-07-11

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：US20230416249A1

公开(公告)日：2023-12-28

申请号：US18315472

申请日：2023-05-10

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

发明人： Stephan SIEGEL ,  Franziska SIEGEL ,  Volker SCHULZE ,  Markus BERGER ,  Keith GRAHAM ,  Ulrich KLAR ,  Jeremie Xavier G. MORTIER ,  Detlev SÜLZLE ,  Ulf BÖMER ,  Daniel KORR ,  Jens SCHRÖDER ,  Matthew MEYERSON ,  Heidi GREULICH ,  Bethany KAPLAN

IPC分类号： C07D471/04 ,  A61P35/00 ,  G01N33/574

CPC分类号： C07D471/04 ,  A61P35/00 ,  G01N33/57492 ,  G01N2333/71

摘要： Compounds of formula (I)




processes for their production and their use as pharmaceuticals.

公开(公告)号：US20240150277A1

公开(公告)日：2024-05-09

申请号：US18241190

申请日：2023-08-31

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

发明人： Stephan SIEGEL ,  Knut EIS ,  Timo STELLFELD ,  Léa Aurelie BOUCHÉ ,  Elisabeth POOK ,  Joseph Peter BLUCK ,  Philip LIENAU ,  Constantia PANTELIDOU ,  Isabel Sophie JERCHEL-FURAU ,  Ulf BRÜEGGEMEIER ,  Sven CHRISTIAN ,  Detlev SÜLZLE ,  Anders Roland FRIBERG ,  Simon HOLTON ,  Christian LECHNER ,  Stefan KAULFUSS ,  Hanna MEYER ,  Douglas ORSI ,  Steven James FERRARA ,  Jonathan GOLDSTEIN ,  Matthew MEYERSON ,  Christopher LEMKE

IPC分类号： C07C237/42 ,  A61P35/00 ,  C07D211/22 ,  C07D213/40 ,  C07D241/20 ,  C07D263/57 ,  C07D271/06 ,  C07D271/10 ,  C07D305/06 ,  C07D405/04

CPC分类号： C07C237/42 ,  A61P35/00 ,  C07D211/22 ,  C07D213/40 ,  C07D241/20 ,  C07D263/57 ,  C07D271/06 ,  C07D271/10 ,  C07D305/06 ,  C07D405/04 ,  C07C2601/16 ,  C07C2602/10

摘要： The present invention includes compounds of formula (I)




and methods for its preparation and treatment of disorders with activated peroxisome preoliferator-activated receptor gamma (PPARG), particularly cancer.

公开(公告)号：US20230064983A1

公开(公告)日：2023-03-02

申请号：US17934553

申请日：2022-09-22

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

发明人： Stephan SIEGEL ,  Franziska SIEGEL ,  Volker SCHULZE ,  Markus BERGER ,  Jeremie Xavier G. MORTIER ,  Detlev SÜLZLE ,  Ulf BÖMER ,  Daniel KORR ,  Jens SCHRÖDER ,  Ursula MÖNNING ,  Michael NIEHUES ,  Matthew MEYERSON ,  Heidi GREULICH ,  Bethany KAPLAN

IPC分类号： A61K31/444 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/4545 ,  A61K45/06

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

公开(公告)号：US20240307362A1

公开(公告)日：2024-09-19

申请号：US17605956

申请日：2020-04-22

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

发明人： Stephan SIEGEL ,  Franziska SIEGEL ,  Volker SCHULZE ,  Markus BERGER ,  Keith GRAHAM ,  Stefan Nikolaus GRADL ,  Detlev SÜLZLE ,  Ulf BÖMER ,  Daniel KORR ,  Jens SCHRÖDER ,  Ursula MÖNNING ,  Michael NIEHUES ,  Matthew MEYERSON ,  Heidi GREULICH ,  Bethany KAPLAN ,  Hassan Youssef HARB ,  Phi Manh DINH

IPC分类号： A61K31/444 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C12Q1/6886 ,  G01N33/574

CPC分类号： A61K31/444 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C12Q1/6886 ,  G01N33/57484 ,  C12Q2600/106 ,  C12Q2600/156 ,  G01N2333/71

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

公开(公告)号：US20240109850A1

公开(公告)日：2024-04-04

申请号：US18241147

申请日：2023-08-31

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

发明人： Knut EIS ,  Elisabeth POOK ,  Ulf BRÜGGEMEIER ,  Adelaide Clara F. A. DE LEMOS ,  Sven CHRISTIAN ,  Isabel Sophie JERCHEL-FURAU ,  Ulrike RAUH ,  Nico BRÄUER ,  Timo STELLFELD ,  Anders Roland FRIBERG ,  Christian LECHNER ,  Stefan KAULFUSS ,  Hanna MEYER ,  Charlotte Christine KOPITZ ,  Steven James FERRARA ,  Jonathan GOLDSTEIN ,  Matthew MEYERSON ,  Christopher LEMKE ,  Timothy A. LEWIS

IPC分类号： C07D263/57 ,  C07D235/18 ,  C07D249/20 ,  C07D413/04 ,  C07D413/12

CPC分类号： C07D263/57 ,  C07D235/18 ,  C07D249/20 ,  C07D413/04 ,  C07D413/12

摘要： The present invention includes compounds of formula (I)




and methods for its preparation and treatment of disorders with activated peroxisome preoliferator-activated receptor gamma (PPARG), particularly cancer.

公开(公告)号：US20230405015A1

公开(公告)日：2023-12-21

申请号：US18241186

申请日：2023-08-31

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

发明人： Martin LANGE ,  Stefan KAULFUSS ,  Charlotte Christine KOPITZ ,  Heidi GREULICH ,  Xiaoyun WU ,  Matthew MEYERSON

IPC分类号： A61K31/5395 ,  A61P35/00

CPC分类号： A61K31/5395 ,  A61P35/00

摘要： The present invention provides a method of treatment of sarcoma comprising administering to a patient in need thereof a compound of general formula (I),




in which R1, R2, R3, and R4, are as defined herein, alone or in pharmaceutical compositions or combinations comprising said compounds as a sole agent or in combination with other active ingredients.

公开(公告)号：US20220378762A1

公开(公告)日：2022-12-01

申请号：US17605990

申请日：2020-04-22

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

发明人： Franziska SIEGEL ,  Daniel KORR ,  Jens SCHRÖDER ,  Stephan SIEGEL ,  Heidi GREULICH ,  Bethany KAPLAN ,  Matthew MEYERSON

IPC分类号： A61K31/444 ,  A61K38/17 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/4545

摘要： Compounds of formula (I) for use in the treatment or prophylaxis of a disease, which is a hyperproliferative disease and/or a disorder responsive to induction of cell death, selected from a haematological tumour, a solid tumour and/or metastases thereof, said tumour harbouring a mutant EGFR with exon 19 or 21 mutations, and their use as pharmaceuticals.