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公开(公告)号：US11584746B2
公开(公告)日：2023-02-21
申请号：US16970931
申请日：2019-02-20
发明人： Nathanael S. Gray , Dries De Clercq , Jaebong Jang , Pasi Janne , Ciric To , Michael Eck , Eunyoung Park , David Heppner
IPC分类号： C07D471/04 , C07D243/38 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/14
摘要： The application relates to a compound having Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US10550112B2
公开(公告)日：2020-02-04
申请号：US15742113
申请日：2016-07-20
发明人： Nathanael S. Gray , Jaebong Jang , Pasi Janne
IPC分类号： C07D413/14 , C07D403/12 , C07D401/14 , C07D403/14 , C07D409/14 , A61P31/12
摘要： The application relates to a compound having Formula (I′): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US10450310B2
公开(公告)日：2019-10-22
申请号：US16163254
申请日：2018-10-17
发明人： Nathanael Gray , Jaebong Jang , Dries De Clercq , Michael Eck , Pasi Janne
IPC分类号： C07D417/14 , A61K47/54 , A61P35/00 , A61K47/18
摘要： The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.
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公开(公告)号：US10385019B2
公开(公告)日：2019-08-20
申请号：US15580088
申请日：2016-06-30
发明人： Nathanael S. Gray , Michael Eck , Pasi Janne , Hwan Geun Choi , Jaebong Jang , Kwok-Kin Wong
IPC分类号： A61P35/00 , C07D209/46 , C07D277/46 , C07D401/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04 , C07D403/12
摘要： The disclosure relates to a compound having Formula (I′): and in particular, Compound I-126: which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US10266517B2
公开(公告)日：2019-04-23
申请号：US15536486
申请日：2015-12-23
发明人： Nathanael S. Gray , Pasi Janne , Hwan Geun Choi , Jaebong Jang
IPC分类号： C07D471/04 , A61K31/506 , C07D403/04 , C07D403/14 , C07D487/04
摘要： The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
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公开(公告)号：US11186574B2
公开(公告)日：2021-11-30
申请号：US16643092
申请日：2018-08-31
发明人： John M. Hatcher , Nathanael S. Gray , Jaebong Jang , Dries De Clercq , Pasi Janne , Jamie A. Saxon , Michael Eck , David A. Scott , Alyssa Verano
IPC分类号： A61K31/519 , A61P35/00 , C07D471/04 , C07D487/04
摘要： The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.
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公开(公告)号：US20210230101A1
公开(公告)日：2021-07-29
申请号：US17055366
申请日：2019-05-15
发明人： Priscilla L. Yang , Nathanael S. Gray , Jaebong Jang , Jinhua Wang , Nicholas Paul Kwiatkowski , Wenlong Lian , Zhengnian Li
IPC分类号： C07C233/75 , A61P31/14 , C07C255/44 , C07D209/08 , C07C323/31 , C07D295/03 , C07D235/08 , C07D213/65
摘要： Provided herein are compounds, pharmaceutical compositions, methods, and kits for treating viral infections (e.g., Dengue viral infections). In certain embodiments, compounds useful in the methods described herein are of Formula (I) or (II).
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公开(公告)号：US11945816B2
公开(公告)日：2024-04-02
申请号：US17451538
申请日：2021-10-20
发明人： John M. Hatcher , Nathanael S. Gray , Jaebong Jang , Dries De Clercq , Pasi Janne , Jamie A. Saxon , Michael Eck , David A. Scott , Alyssa Verano
IPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , A61P35/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.
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公开(公告)号：US20220106310A1
公开(公告)日：2022-04-07
申请号：US17451538
申请日：2021-10-20
发明人： John M. Hatcher , Nathanael S. Gray , Jaebong Jang , Dries De Clercq , Pasi Janne , Jamie A. Saxon , Michael Eck , David A. Scott , Alyssa Verano
IPC分类号： C07D471/04 , C07D487/04
摘要： The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.
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公开(公告)号：US11161842B2
公开(公告)日：2021-11-02
申请号：US16588750
申请日：2019-09-30
发明人： Nathanael Gray , Jaebong Jang , Dries De Clercq , Michael Eck , Pasi Janne
IPC分类号： C07D417/14 , A61K47/54 , A61P35/00 , A61K47/18
摘要： The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.
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