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公开(公告)号：US20240158418A1
公开(公告)日：2024-05-16
申请号：US18516589
申请日：2023-11-21
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 , A61P35/04
CPC分类号： C07D519/00 , A61P35/04
摘要： The invention provides for the treatment of mutant epidermal growth factor receptor (EGFR) mediated cancer that has metastasized to the brain or other area of the central nervous system with a compound that degrades a mutant form of EGFR via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The invention also provides advantageous drug combinations for the treatment of such cancer that include a compound herein that degrades a mutant form of EGFR in combination with a second anti-cancer agent.
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公开(公告)号：US11185592B2
公开(公告)日：2021-11-30
申请号：US16882236
申请日：2020-05-22
发明人： Andrew J. Phillips , Christopher G. Nasveschuk , James A. Henderson , Yanke Liang , Kiel Lazarski , Ryan E. Michael
IPC分类号： A61K31/545 , A61K47/54 , C07D498/20 , C07D471/10 , C07D519/00 , A61K31/435 , A61K31/438
摘要： This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
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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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公开(公告)号：US20230233692A1
公开(公告)日：2023-07-27
申请号：US18105735
申请日：2023-02-03
发明人： James A. Henderson , Christopher G. Naveschuk , Kiel Lazarski , Victoria Garza , Moses Moustakim , Jae Young Ahn , Gesine Kerstin Veits , Morgan Welzel O'Shea , Ryan E. Michael , Jeremy L. Yap , Yanke Liang , Andrew Charles Good , Mark E. Fitzgerald , Robert T. Yu
IPC分类号： A61K47/55
CPC分类号： A61K47/55
摘要： Novel compounds which act as protein degradation inducing moieties for proto-oncogene tyrosine-protein kinase receptor (RET), which may be either wild type RET or a mutant form of RET.
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公开(公告)号：US20210106688A1
公开(公告)日：2021-04-15
申请号：US16882236
申请日：2020-05-22
发明人： Andrew J. Phillips , Chris G. Nasveschuk , James A. Henderson , Yanke Liang , Kiel Lazarski , Ryan E. Michael
IPC分类号： A61K47/54 , C07D498/20 , C07D471/10 , C07D519/00 , A61K31/435 , A61K31/438
摘要： This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
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公开(公告)号：US12076405B2
公开(公告)日：2024-09-03
申请号：US17164446
申请日：2021-02-01
发明人： Andrew J. Phillips , Christopher G. Nasveschuk , James A. Henderson , Yanke Liang , Mark E. Fitzgerald , Minsheng He , Ryan E. Michael
IPC分类号： A61K47/54 , A61K31/4035 , A61K31/438 , A61K31/439 , A61K31/454 , A61K31/547 , A61K31/55 , C07D401/04 , C07D403/04
CPC分类号： A61K47/545 , A61K31/4035 , A61K31/438 , A61K31/439 , A61K31/454 , A61K31/547 , A61K31/55 , A61K47/554 , C07D403/04
摘要： This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
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公开(公告)号：US10905768B1
公开(公告)日：2021-02-02
申请号：US16872225
申请日：2020-05-11
发明人： Andrew J. Phillips , Chris G. Nasveschuk , James A. Henderson , Yanke Liang , Mark E. Fitzgerald , Minsheng He , Ryan E. Michael
IPC分类号： C07D403/04 , A61K47/54 , A61K31/454 , A61K31/55 , A61K31/438 , A61K31/439 , A61K31/547 , A61K31/4035
摘要： This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
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公开(公告)号：US10646575B2
公开(公告)日：2020-05-12
申请号：US16186339
申请日：2018-11-09
发明人： Andrew J. Phillips , Chris G. Nasveschuk , James A. Henderson , Yanke Liang , Mark E. Fitzgerald , Minsheng He , Ryan E. Michael
IPC分类号： A61K47/54 , A61K31/438 , A61K31/439 , A61K31/547 , A61K31/55 , A61K31/4035 , C07D403/04 , A61K31/454
摘要： This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
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公开(公告)号：US12048748B2
公开(公告)日：2024-07-30
申请号：US17524558
申请日：2021-11-11
发明人： Andrew J. Phillips , Christopher G. Nasveschuk , James A. Henderson , Yanke Liang , Kiel Lazarski , Ryan E. Michael
IPC分类号： A61K31/435 , A61K31/438 , A61K47/54 , C07D471/10 , C07D498/20 , C07D519/00
CPC分类号： A61K47/545 , A61K31/435 , A61K31/438 , A61K47/554 , C07D471/10 , C07D498/20 , C07D519/00
摘要： This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
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