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公开(公告)号：US20230201186A1
公开(公告)日：2023-06-29
申请号：US18072490
申请日：2022-11-30
发明人： Norbert SCHMEES , Lars WORTMANN , Dennis KIRCHOFF , Thi Thanh Uyen NGUYEN , Nicolas WERBECK , Ulf BÖMER , Kirstin PETERSEN , Christina KOBER , Detlef STÖCKIGT , Christian LECHNER , Robin Michael MEIER , Simon Anthony HERBERT , Isabel Patrizia KERSCHGENS , Dirk KOSEMUND , Rienk OFFRINGA , Mareike GREES
IPC分类号： A61K31/4545 , C07D401/14 , A61K31/498 , C07D413/14 , A61P37/04 , A61K31/55 , C07D401/04 , C07D405/14 , C07D417/14 , A61K31/496 , A61K31/4725 , A61P35/00 , A61K31/4709 , A61K45/06
CPC分类号： A61K31/4545 , C07D401/14 , A61K31/498 , C07D413/14 , A61P37/04 , A61K31/55 , C07D401/04 , C07D405/14 , C07D417/14 , A61K31/496 , A61K31/4725 , A61P35/00 , A61K31/4709 , A61K45/06
摘要： The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n 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 and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20230064809A1
公开(公告)日：2023-03-02
申请号：US17780814
申请日：2020-11-24
发明人： Norbert SCHMEES , Lars WORTMANN , Dennis KIRCHHOFF , Thi Thanh Uyen NGUYEN , Nicolas WERBECK , Ulf BÖMER , Kirstin PETERSEN , Christina KOBER , Detlef STÖCKIGT , Christian LECHNER , Rienk OFFRINGA
IPC分类号： A61K31/4709 , C07D471/10 , C07D487/10 , A61K31/5377 , A61K31/496 , A61P37/04 , A61P35/00 , A61K45/06
摘要： The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, m, n, o and p 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 and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20230148194A1
公开(公告)日：2023-05-11
申请号：US17780890
申请日：2020-11-24
发明人： Norbert SCHMEES , Lars WORTMANN , DENNIS KIRCHHOFF , Thi Thanh Uyen NGUYEN , Nicolas WERBECK , Ulf BÖMER , Kirstin PETERSEN , Christina KOBER , Detlef STÖCKIGT , Christian LECHNER , Robin Michael MEIER , Simon Anthony HERBERT , Isabel Patrizia KERSCHGENS , DIRK KOSEMUND , Rienk OFFRINGA , Mareike GREES
IPC分类号： A61K31/4545 , C07D413/14 , C07D401/14 , C07D401/04 , C07D417/14 , C07D405/14 , A61K31/4709 , A61K31/496 , A61K31/4725 , A61K31/498 , A61K31/55 , A61K45/06 , A61P35/00 , A61P37/04
CPC分类号： A61K31/4545 , C07D413/14 , C07D401/14 , C07D401/04 , C07D417/14 , C07D405/14 , A61K31/4709 , A61K31/496 , A61K31/4725 , A61K31/498 , A61K31/55 , A61K45/06 , A61P35/00 , A61P37/04
摘要： The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8 and n 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 and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20230062100A1
公开(公告)日：2023-03-02
申请号：US17780903
申请日：2020-11-24
发明人： Norbert SCHMEES , Lars WORTMANN , DENNIS KIRCHOFF , Thi Thanh Uyen NGUYEN , Nicolas WERBECK , Ulf BÖMER , Kirstin PETERSEN , Christina KOBER , Detlef STÖCKIGT , Christian LECHNER , Robin Michael MEIER , Simon Anthony HERBERT , Isabel Patrizia KERSCHGENS , DIRK KOSEMUND , Julien LEFRANC , Rienk OFFRINGA
IPC分类号： A61K31/4709 , C07D401/04 , C07D401/14 , C07D413/14 , C07D405/14 , C07F9/6558 , C07D417/14 , A61K31/513 , A61K31/496 , A61K31/506 , A61K31/675 , A61K31/55 , A61P37/04 , A61P35/00 , A61K45/06
摘要： The present invention covers aminoquinolone compounds of general formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8, X and n 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 and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20210017174A1
公开(公告)日：2021-01-21
申请号：US16978060
申请日：2019-03-01
发明人： Duy NGUYEN , Lars WORTMANN , Adelaide Clara FARIA ALVARES DE LEMOS , Ulf BOEMER , Detlev SUELZLE , Simon HOLTON , Christian LECHNER
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14
摘要： The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 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 cancer disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20240174683A1
公开(公告)日：2024-05-30
申请号：US18275978
申请日：2022-02-04
发明人： Ulrich LÜCKING , Jeffrey Stuart MOWAT , Ludwig ZORN , Lars WORTMANN , Steffen MÜLLER , Gabriele LEDER , Sandra BERNDT , Judith GÜNTHER , Lara KUHNKE , Antje Margret WENGNER , Rafael CARRETERO , Gerd WOHLFAHRT , Anders FRIBERG , Ulf BÖMER , Roland NEUHAUS , Maren OSMERS , Hideki Miyatake ONDOZABAL , Martina SCHÄFER , Louise EAGLING , Julien LEFRANC , Katrin NOWAK-REPPEL , Rienk OFFRINGA , Peng CHEN , Xuewei WANG , Yuanyuan YAN , Kai THEDE , Nikolay SITNIKOV , Berndt BUCHMANN , Dirk KOSEMUND , Detlef STOECKIGT
IPC分类号： C07D487/20 , A61K45/06 , C07B59/00 , C07D498/20
CPC分类号： C07D487/20 , A61K45/06 , C07B59/002 , C07D498/20 , C07B2200/13
摘要： The present invention relates to Map4K1 inhibitors of formula (I) (I), wherein A, E, G, Q, R1, R2 and R4 have the same meaning as defined in the description, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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公开(公告)号：US20220235013A1
公开(公告)日：2022-07-28
申请号：US16496825
申请日：2018-03-19
发明人： Lars WORTMANN , Brice SAUTIER , Knut EIS , Hans BRIEM , Niels BOHNKE , Franz VON NUSSBAUM , Roman HILLIG , Benjamin BADER , Jens SCHRODER , Kirstin PETERSEN , Philip LIENAU , Antje Margret WENGNER , Dieter MOOSMAYER , Qiuwen WANG , Hans SCHICK
IPC分类号： C07D239/94 , C07D409/12 , C07D405/12 , C07D403/12 , C07D417/12 , C07D471/04 , C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14
摘要： The present invention describes 2-methyl-quinazoline compounds of general formula (I), 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.
The 2-methyl substituted quinazoline compounds of general formula (I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.-
公开(公告)号：US20160297833A1
公开(公告)日：2016-10-13
申请号：US15037949
申请日：2014-11-17
发明人： Ulrich KLAR , Lars WORTMANN , Georg KETTSCHAU , Keith GRAHAM , Anja RICHTER , Philip LIENAU , Florian PUEHLER , Kirstin PETERSEN , Franziska SIEGEL , Detlev SÜLZLE
IPC分类号： C07D495/04 , A61K31/655 , A61K31/5377 , C07D519/00 , A61K31/519 , A61K45/06
CPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D519/00
摘要： The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, 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 a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20160002245A1
公开(公告)日：2016-01-07
申请号：US14765373
申请日：2014-01-29
发明人： Ulrich KLAR , Lars WORTMANN , Georg KETTSCHAU , Florian PÜHLER , Philip LIENAU , Detlev SÜLZLE
IPC分类号： C07D487/04 , A61K45/06 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention relates to substituted pyrazolopyrimidinylamino-indazole compounds of general formula I as described and defined herein, 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 a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及如本文所述和定义的通式I的取代的吡唑并嘧啶基氨基 - 吲唑化合物，制备所述化合物的方法，可用于制备所述化合物的中间体化合物，包含所述化合物的药物组合物和组合，以及所述 用于制造用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的化合物。
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公开(公告)号：US20220274979A1
公开(公告)日：2022-09-01
申请号：US17048561
申请日：2019-04-15
发明人： Lars WORTMANN , Brice SAUTIER , Knut EIS , Hans BRIEM , Niels BÖHNKE , Franz VON NUSSBAUM , Roman HILIG , Benjamin BADER , Jens SCHRÖDER , Kirstin PETERSEN , Philip LIENAU , Antje Margret WENGNER , Dieter MOOSMAYER , Qiuwen WANG , Hans SCHICK
IPC分类号： C07D471/04 , C07D487/04
摘要： The present invention covers 2-methyl-aza-quinazoline compounds of general formula (I) as described and 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 disorders, as a sole agent or in combination with other active ingredients
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