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公开(公告)号：US20200299269A1
公开(公告)日：2020-09-24
申请号：US16765709
申请日：2018-11-16
发明人： Ludwig ZORN , Ulrike RÖHN , Ilona GUTCHER , Lars RÖSE , Benjamin BADER , Christina KOBER , Rafael CARRETERO , Detlef STÖCKIGT , Michael PLATTEN
IPC分类号： C07D403/04 , C07D237/14 , C07D417/14 , C07D409/12 , C07D409/14 , A61P35/00
摘要： The present invention covers sulphur substituted 3-oxo-2,3-dihydropyridazine-4 carboxamide compounds of general formula (I): (I) in which R1, R2, A, X, Y and Z 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 cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20200283395A1
公开(公告)日：2020-09-10
申请号：US16765780
申请日：2018-11-16
发明人： Julien LEFRANC , Norbert SCHMEES , Ulrike RÖHN , Ludwig ZORN , Judith GÜNTHER , Ilona GUTCHER , Lars RÖSE , Benjamin BADER , Detlef STÖCKIGT , Michael PLATTEN
IPC分类号： C07D239/28 , C07D405/12 , A61P35/04
摘要： The present invention covers 2-phenylpyrimidine-4-carboxamide compounds of general formula (I): (I) 5 in which X, Y, Z, R1, R2, R4, R5 and R6 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 cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20200289509A1
公开(公告)日：2020-09-17
申请号：US16765778
申请日：2017-11-16
发明人： Julien LEFRANC , Norbert SCHMEES , Ulrike RÖHN , Ludwig ZORN , Judith GÜNTHER , Ilona GUTCHER , Lars RÖSE , Benjamin BADER , Detlef STÖCKIGT , Michael PLATTEN
IPC分类号： A61K31/506 , C07D403/04 , C07D401/04 , C07D409/04 , C07D413/04 , C07D401/14 , C07D409/14 , C07D405/14
摘要： The present invention covers 2-hetarylpyrimidine-4-carboxamide compounds of general formula (I): in which X, Y, Z, R1, R2 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20240294505A1
公开(公告)日：2024-09-05
申请号：US16485049
申请日：2018-02-02
发明人： Ilona GUTCHER , Ulrike RÖHN , Norbert SCHMEES , Ludwig ZORN , Lars RÖSE , Benjamin BADER , Christina KOBER , Rafael CARRETERO , Detlef STÖCKIGT , Horst IRLBACHER , Michael PLATTEN
IPC分类号： C07D403/04 , A61K31/501 , A61K31/506 , A61K45/06 , A61P35/00 , C07D237/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
CPC分类号： C07D403/04 , A61K31/501 , A61K31/506 , A61K45/06 , A61P35/00 , C07D237/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I), in which X, 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20230121195A1
公开(公告)日：2023-04-20
申请号：US17819602
申请日：2022-08-12
发明人： Ilona GUTCHER , Ulrike RÖHN , Norbert SCHMEES , Ludwig ZORN , Lars RÖSE , Benjamin BADER , Christina KOBER , Rafael CARRETERO , Detlef STÖCKIGT , Horst IRLBACHER , Michael PLATTEN
IPC分类号： C07D417/04 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D409/14 , C07D401/14
摘要： The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (1): in which X, 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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![[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES](/abs-image/US/2023/04/13/US20230113037A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230113037A1
公开(公告)日：2023-04-13
申请号：US17634930
申请日：2020-08-10
发明人： Julien LEFRANC , Norbert SCHMEES , Ludwig ZORN , Robin Michael MEIER , Simon Anthony HERBERT , Judith GÜNTHER , Ilona GUTCHER , Lars RÖSE , Benjamin BADER , Detlef STÖCKIGT , Mátyás GORJÁNÁCZ , Christina KOBER , Bernd BUCHMANN , Stephan BÖHME , Ulrich BOTHE , Michael PLATTEN , Daniel BAUMANN
IPC分类号： C07D487/04
摘要： The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20200283402A1
公开(公告)日：2020-09-10
申请号：US16765806
申请日：2018-11-16
发明人： Ilona GUTCHER , Ulrike RÖHN , Ludwig ZORN , Lars RÖSE , Benjamin BADER , Christina KOBER , Rafael CARRETERO , Detlef STÖCKIGT , Michael PLATTEN
IPC分类号： C07D401/04 , C07D403/04 , C07D409/14 , C07D405/14 , A61P35/04
摘要： The present invention covers 3-oxo-6-heteromyl-2-phenyl-2,3-dihydropyri-dazine-4-carboxamide compounds of general formula (I): in which R1, R2, R4, R5, R6, X, Y and Z 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20200237757A1
公开(公告)日：2020-07-30
申请号：US16303539
申请日：2017-05-23
发明人： Norbert SCHMEES , Ilona GUTCHER , Horst IRLBACHER , Benjamin BADER , Na ZHAO , Michael PLATTEN , Ulrike ROEHN , Ludwig ZORN , Lars ROESE , Detlef STOECKIGT
IPC分类号： A61K31/501 , A61K45/06 , C07D237/24 , C07D405/12 , C07D403/12 , A61K31/50 , A61P35/00
摘要： The present invention covers 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and R6 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 cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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9.发明申请公开(公告)号：US20230084899A1
公开(公告)日：2023-03-16
申请号：US17785860
申请日：2020-12-14
发明人： Ilona GUTCHER
IPC分类号： A61K31/501 , C07K16/28 , A61K31/506 , A61K31/381 , A61P35/00
摘要： The present invention relates to combinations of at least two components, component A and component B, component A being an AhR inhibitor, and component B being pembrolizumab or nivolumab. A further aspect of the present invention relates to combinations of three components, component A, component B, and component C; component A being an AhR inhibitor, component B being pembrolizumab or nivolumab, and component C being a further pharmaceutical agent. The present invention further relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment or prophylaxis of cancers of the breast, respiratory tract, brain, reproductive organs, digestive tract, urinary tract, eye, liver, skin, kidney, head and neck, thyroid, parathyroid, and their distant metastases, lymphomas, sarcomas and leukemias.
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