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公开(公告)号：US20240076300A1
公开(公告)日：2024-03-07
申请号：US18144800
申请日：2023-05-08
发明人： Christopher G. Nasveschuk , Martin Duplessis , Jae Young Ahn , Alexander W. Hird , Ryan E. Michael , Kiel Lazarski , Yanke Liang , Georg Jaeschke , Antonio Ricci , Annick Goergler , Daniel Rueher
IPC分类号： C07D519/00 , A61K9/00 , A61K9/02 , A61K9/08 , A61K9/20 , A61K9/48 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/32 , A61K47/38 , C07D487/04
CPC分类号： C07D519/00 , A61K9/009 , A61K9/02 , A61K9/08 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/4825 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/32 , A61K47/38 , C07D487/04
摘要： The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
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公开(公告)号：US20210070763A1
公开(公告)日：2021-03-11
申请号：US17103621
申请日：2020-11-24
IPC分类号： C07D487/10 , C07D519/00
摘要： The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
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公开(公告)号：US20230416251A1
公开(公告)日：2023-12-28
申请号：US18100992
申请日：2023-01-24
发明人： Christopher G. Nasveschuk , Fabian Dey , Annick Goergler , Bernd Kuhn , Roger Norcross , Stephan Roever , Philipp Schmid
IPC分类号： C07D471/10 , C07D519/00
CPC分类号： C07D471/10 , C07D519/00
摘要： The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
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公开(公告)号：US20230192643A1
公开(公告)日：2023-06-22
申请号：US17878753
申请日：2022-08-01
发明人： Roger Norcross , Adrian Britschgi , Fabian Dey , Annick Goergler , Eric Andre Kusznir , Moreno Attilio Wichert
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D471/04 , C07D519/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D471/04 , C07D519/00
摘要： The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
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公开(公告)号：US20200207764A1
公开(公告)日：2020-07-02
申请号：US16809325
申请日：2020-03-04
IPC分类号： C07D471/04 , C07D235/26 , C07D401/14 , C07D403/10 , C07D403/14 , C07D401/10 , C07D417/10 , C07D405/12 , C07D487/08 , C07D405/14
摘要： The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
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公开(公告)号：US12091397B2
公开(公告)日：2024-09-17
申请号：US17878753
申请日：2022-08-01
发明人： Roger Norcross , Adrian Britschgi , Fabian Dey , Annick Goergler , Eric Andre Kusznir , Moreno Attilio Wichert
IPC分类号： C07D401/04 , A61K31/4375 , A61K31/4704 , A61K47/55 , A61P35/00 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/14 , C07D519/00
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4704 , A61K47/55 , A61P35/00 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/14 , C07D519/00
摘要： The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
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公开(公告)号：US20240199638A1
公开(公告)日：2024-06-20
申请号：US18385277
申请日：2023-10-30
IPC分类号： C07D495/14 , C07D211/88 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
CPC分类号： C07D495/14 , C07D211/88 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： The present invention provides selected glutarimides which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
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公开(公告)号：US20240109889A1
公开(公告)日：2024-04-04
申请号：US18370186
申请日：2023-09-19
IPC分类号： C07D471/04 , C07D235/26 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/12 , C07D405/14 , C07D417/10 , C07D487/08
CPC分类号： C07D471/04 , C07D235/26 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/12 , C07D405/14 , C07D417/10 , C07D487/08
摘要： The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
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公开(公告)号：US11673902B2
公开(公告)日：2023-06-13
申请号：US17843769
申请日：2022-06-17
发明人： Christopher G. Nasveschuk , Martin Duplessis , Jae Young Ahn , Alexander W. Hird , Ryan E. Michael , Kiel Lazarski , Yanke Liang , Georg Jaeschke , Antonio Ricci , Annick Goergler , Daniel Rueher
IPC分类号： C07D519/00 , A61K47/32 , A61K9/20 , A61K9/48 , A61K9/02 , A61K9/08 , A61K47/10 , A61K47/12 , A61K9/00 , A61K47/26 , A61K47/38 , C07D487/04
CPC分类号： C07D519/00 , A61K9/009 , A61K9/02 , A61K9/08 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/485 , A61K9/4825 , A61K9/4858 , A61K9/4866 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/32 , A61K47/38 , C07D487/04
摘要： The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
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公开(公告)号：US20230110648A1
公开(公告)日：2023-04-13
申请号：US17843769
申请日：2022-06-17
发明人： Christopher G. Nasveschuk , Martin Duplessis , Jae Young Ahn , Alexander W. Hird , Ryan E. Michael , Kiel Lazarski , Yanke Liang , Georg Jaeschke , Antonio Ricci , Annick Goergler , Daniel Rueher
IPC分类号： C07D519/00 , C07D487/04 , A61K9/20 , A61K9/48 , A61K9/02 , A61K9/08 , A61K47/10 , A61K47/12 , A61K9/00 , A61K47/26 , A61K47/38 , A61K47/32
摘要： The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
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