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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：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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公开(公告)号：US20180256591A1
公开(公告)日：2018-09-13
申请号：US15974536
申请日：2018-05-08
发明人： Lars WORTMANN , Ulrich LÜCKING , Julien LEFRANC , Hans BRIEM , Marcus KOPPITZ , Knut EIS , Franz VON NUSSBAUM , Benjamin BADER , Antje Margret WENGNER , Gerhard SIEMEISTER , Wilhelm BONE , Philip LIENAU , Joanna GRUDZINSKA-GOEBEL , Dieter MOOSMAYER , Uwe EBERSPÄCHER , Hans SCHICK
IPC分类号： A61K31/541 , A61K31/55 , A61K31/5377 , A61K31/5386 , C07D471/04 , A61K31/675 , A61K45/06 , C07D491/22 , C07D519/00 , C07F9/6561
摘要： The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), 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 hyperproliferative disease as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20170216304A1
公开(公告)日：2017-08-03
申请号：US15501079
申请日：2015-08-03
发明人： Lars WORTMANN , Ulrich LÜCKING , Julien LEFRANC , Hans BRIEM , Marcus KOPPITZ , Knut EIS , Franz VON NUSSBAUM , Benjamin BADER , Antje Margret WENGNER , Gerhard SIEMEISTER , Wilhelm BONE , Philip LIENAU , Joanna GRUDZINSKA-GOEBEL , Dieter MOOSMAYER , Uwe EBERSPÄCHER , Hans SCHICK
IPC分类号： A61K31/541 , A61K31/5386 , A61K31/5377 , C07D491/22 , C07F9/6561 , C07D471/04 , C07D519/00 , A61K31/55 , A61K31/675
CPC分类号： A61K31/541 , A61K31/5377 , A61K31/5386 , A61K31/55 , A61K31/675 , A61K45/06 , C07D471/04 , C07D491/22 , C07D519/00 , C07F9/6561
摘要： The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), 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 hyperproliferative disease as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20240083857A1
公开(公告)日：2024-03-14
申请号：US18350246
申请日：2023-07-11
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 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D405/14 , C07D405/10 , C07D495/04 , C07D403/04 , C07D487/04 , A61P35/00
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D405/14 , C07D405/10 , C07D495/04 , C07D403/04 , C07D487/04 , A61P35/00
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.
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公开(公告)号：US20190142812A1
公开(公告)日：2019-05-16
申请号：US16067830
申请日：2017-01-06
发明人： Ulrich LÜCKING , Marcus KOPPITZ , Julien LEFRANC , Lars WORTMANN , Antje Margret WENGNER , Gerhard SIEMEISTER , Ulf BÖMER , Benjamin BADER , Philip LIENAU , Hans SCHICK
IPC分类号： A61K31/4375 , A61P35/00 , A61K45/06
摘要： The present invention relates to 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), 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 hyperproliferative disease as a sole agent or in combination with other active ingredients.
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