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公开(公告)号：US11459312B2
公开(公告)日：2022-10-04
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 , C07D409/12 , C07D409/14 , C07D419/14 , A61P35/00 , C07D417/14 , A61K45/06
摘要： Disclosed are compounds of general formula (I): wherein R1, R2, A, X, Y and Z are as defined herein, methods of preparing the compounds, intermediate compounds useful for preparing the compounds, pharmaceutical compositions and combinations comprising the compounds and the use of the 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：US11591311B2
公开(公告)日：2023-02-28
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 , A61P35/04 , C07D403/04 , C07D405/14 , C07D409/14 , A61K45/06
摘要： The present invention covers 3-oxo-6-heteroaryl-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：US11524944B2
公开(公告)日：2022-12-13
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 , A61P35/04 , C07D405/12 , A61K45/06
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：US11304946B2
公开(公告)日：2022-04-19
申请号：US16765778
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： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , A61K31/506
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：US11795164B2
公开(公告)日：2023-10-24
申请号：US17819602
申请日：2022-08-12
发明人： Ilona Gutcher , Norbert Schmees , Lars Röse , Benjamin Bader , Christina Kober , Rafael Carretero , Detlef Stöckigt , Horst Irlbacher , Michael Platten
IPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , A61P35/00
CPC分类号： C07D417/04 , A61P35/00 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04
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.-
公开(公告)号：US11040035B2
公开(公告)日：2021-06-22
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 Röhn , Ludwig Zorn , Lars Röse , Detlef Stöckigt
IPC分类号： C07D237/14 , C07D237/20 , C07D401/10 , C07D405/12 , A61K31/501 , A61P35/00 , A61K31/50 , A61K45/06 , C07D237/24 , C07D403/12
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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公开(公告)号：US10894784B2
公开(公告)日：2021-01-19
申请号：US16063370
申请日：2016-12-15
发明人： Volker Schulze , Tobias Heinrich , Florian Prinz , Julien Lefranc , Jens Schröder , Anne Mengel , Wilhelm Bone , Joszef Bálint , Antje Margret Wengner , Knut Eis , Horst Irlbacher , Marcus Koppitz , Ulf Bömer , Benjamin Bader , Hans Briem , Philip Lienau , Clara Christ , Detlef Stöckigt , Roman Hillig
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D451/14 , C07D471/08 , C07D487/08 , A61P35/00
摘要： The present invention covers heteroarylbenzimidazole 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 and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US10023539B2
公开(公告)日：2018-07-17
申请号：US15534404
申请日：2015-12-08
发明人： Jeffrey Stuart Mowat , Timo Stellfeld , Carlo Stresemann , Roman Hillig , Silke Köhr , Detlef Stöckigt , Jörg Weiske , Thomas Brumby , Naomi Barak , Clara Christ , Antonius Ter Laak , Volker Badock , Rosemary Helen Crampton , Ian Stefanuti
IPC分类号： C07D231/06 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R1, R2, R3, R4, R5, X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyper-proliferative disorders, in particular for cancer, respectively tumor disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.
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公开(公告)号：US20180263970A1
公开(公告)日：2018-09-20
申请号：US15756469
申请日：2016-08-29
申请人： THE BROAD INSTITUTE, INC. , THE GENERAL HOSPITAL CORPORATION , PRESIDENT AND FELLOWS OF HARVARD COLLEGE , BAYER PHARMA AKTIENGESELLSCHAFT
发明人： David B. Sykes , David Scadden , Timothy A. Lewis , Andreas Janzer , Hanna Meyer , Detlef Stöckigt
IPC分类号： A61K31/47 , A61P35/02 , A61K33/36 , A61K31/42 , A61K31/277
CPC分类号： A61K31/47 , A61K31/27 , A61K31/277 , A61K31/42 , A61K31/505 , A61K33/36 , A61P35/02
摘要： The present invention includes methods of treating patients with acute myeloid leukemia across a range of genetic subtypes with DHODH inhibitors, such as 6-fluoro-2-(2′-fluoro-[1,1′-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid).
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公开(公告)号：US09682995B2
公开(公告)日：2017-06-20
申请号：US14764853
申请日：2014-01-28
发明人： Lars Bärfacker , Stefan Prechtl , Gerhard Siemeister , Antje Margret Wengner , Jens Ackerstaff , Katrin Nowak-Reppel , Benjamin Bader , Philip Lienau , Detlef Stöckigt , Tobias Heinrich
IPC分类号： C07D417/12 , C07D417/14 , C07D495/04 , C07D487/04 , C07D513/04
CPC分类号： C07D495/04 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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