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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：US20200369769A1
公开(公告)日：2020-11-26
申请号：US16766224
申请日：2018-11-28
发明人： Lars RÖSE , Uwe GRITZAN , Julia HÜTTER , Spencer LIANG , Andrew POW , John HUNTER , Ofer LEVY , Ilan VAKNIN
IPC分类号： C07K16/28 , A61K31/337 , A61K31/713 , A61P35/00
摘要： The present invention relates to a novel pharmaceutical combination comprising an ILDR2 antagonist according to any of the aforementioned claims, plus one or more other therapeutically active compounds, and to novel specific ILDR2 antagonists.
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公开(公告)号：US20220133888A1
公开(公告)日：2022-05-05
申请号：US17576522
申请日：2022-01-14
发明人： Sabine HOFF , Lars RÖSE , Dieter ZOPF , Fabian KIESSLING , Wiltrud LEDERLE , Dennis DOLESCHEL
IPC分类号： A61K39/395 , A61P35/00 , A61K9/00 , A61K31/44
摘要： The present invention relates to pharmaceutical compositions and combinations comprising regorafenib or its hydrate, solvate, metabolite or pharmaceutically acceptable salt or a polymorph thereof and a PD-1/PD-L1(2) inhibitor for treating, preventing or managing diseases and conditions including hyperproliferative disorders such as cancer in humans and other mammals.
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公开(公告)号：US20220169736A1
公开(公告)日：2022-06-02
申请号：US17594269
申请日：2020-04-06
发明人： Lars RÖSE , Uwe GRITZAN , Spencer LIANG , Andrew POW , John HUNTER , Ofer LEVY , Ilan VAKNIN
摘要： The present invention relates to an anti-ILDR2 antibody, a fragment or derivative thereof, a modified antibody format, or an antibody mimetic for use in combination with a PD-1 antagonist in the treatment of cancer. Other aspects of the present invention relate to a combination comprising an anti-ILDR2 antibody and a PD-1 antagonist and the use of such combination as a medicament, as well as methods of treatment or prophylaxis of a cancer in a subject, comprising administering to said subject a therapeutically effective amount of the antibodies as described herein. Further, the present invention relates to a kit comprising anti-ILDR2 antibodies and PD-1 antagonists and optionally one or more further pharmaceutical agents.
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