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：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：US20210353630A1

公开(公告)日：2021-11-18

申请号：US17389940

申请日：2021-07-30

申请人： BAYER AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC.

发明人： Stefan Nikolaus GRADL ,  Manuel ELLERMANN ,  Philip LIENAU ,  Charlotte Christine KOPITZ ,  Martin LANGE ,  Adrian TERSTEEGEN ,  Detlev SÜLZLE ,  Timothy A. LEWIS ,  Heidi GREULICH ,  Xiaoyun WU

IPC分类号： A61K31/53 ,  A61P35/00 ,  C07D403/10 ,  C07D403/12 ,  C07D253/06

摘要： The present invention includes name compounds of general formula (I): (I) in which R1, R2, R3 and R4 are as defined herein, methods for their preparation, pharmaceutical compositions and combinations comprising said compounds, and their use for the treatment of hyperproliferative diseases.

公开(公告)号：US20210371935A1

公开(公告)日：2021-12-02

申请号：US17290673

申请日：2019-11-01

申请人： THE BROAD INSTITUTE, INC.

发明人： Xiaoyun WU ,  Heidi GREULICH

IPC分类号： C12Q1/6886 ,  A61K31/50 ,  A61P35/00

摘要： The present disclosure features methods for identifying pateints having a hyperproliferative disease, disorder, or condition responsive to phosphodiesterase 3 (PDE3) and schlafen family member 12 (SLFN12) complex formation. The hyperproliferative disease, disorder, or condition may be cancer in a patient including glioblastoma, melanoma, ovarian cancer, cervical cancer, sarcoma, or hematopoietic cancers, such as acute myeloid leukemia. Those responsive diseases, disorders, or conditions may be identified using the biomarker AIP and/or TRRAP in combination with those biomarkers pertinent to phosphodieseterase 3 and schlafen family member 12 complexes which may be formed by PDE3 modulation with certain active compounds. Expression of combinations of these biomarkers have been shown to correlate with active compound (e.g., PDE3 modulator, PDE3A modulator, PDE3B modulator) sensitivity.