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公开(公告)号:US20220177466A1
公开(公告)日:2022-06-09
申请号:US17601536
申请日:2020-04-07
发明人: Nathanael Gray , Tinghu Zhang , Guangyan Du , Nathaniel Henning , Jie Jiang , Eric Fischer , Katherine Donovan
IPC分类号: C07D419/04 , C07D401/14 , C07D401/04 , A61K47/54
摘要: The present invention relates to bifunctional compounds, compositions, and methods for treating diseases or conditions mediated by Kelch-like ECH-associated protein 1 (KEAP1). In some aspects, the present invention is directed to methods of treating diseases or disorders involving dysfunctional (e.g., dysregulated) KEAP1 activity, that entails administration of a therapeutically effective amount of a bifunctional compound of formula I or a pharmaceutically acceptable salt or stereoisomer thereof, to a subject in need thereof.
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公开(公告)号:US20220378919A1
公开(公告)日:2022-12-01
申请号:US17761096
申请日:2020-09-24
发明人: Nathanael S. Gray , Jinhua Wang , Fleur Marcia Ferguson , Jie Jiang , Inchul You
摘要: Disclosed are bispecific compounds (degraders) that target ERK5 for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat cancer and inflammatory diseases.
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公开(公告)号:US20220280649A1
公开(公告)日:2022-09-08
申请号:US17631774
申请日:2020-08-04
发明人: Nathanael S. Gray , Guangyan Du , Tinghu Zhang , Zhixiang He , Nicholas Kwiatkowski , Jie Jiang
摘要: Disclosed are bispecific compounds (degraders) that target CDK7 for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.
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公开(公告)号:US20220089611A1
公开(公告)日:2022-03-24
申请号:US17418353
申请日:2019-12-27
发明人: Nathanael S. Gray , Tinghu Zhang , Nicholas Paul Kwiatkowski , Jie Jiang , Mingfeng Hao , Zhixiang He
IPC分类号: C07D519/00 , C07D487/04
摘要: The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds of the present disclosure are inhibitors of kinases (e.g., a cyclin-dependent kinase (CDK) (e.g., CDK7)). The compounds may be selective for inhibiting the activity of a kinase (e.g., CDK7) over certain other kinases (e.g., CDK2, CDK9, CDK12). Also provided are pharmaceutical compositions, kits, methods of use, and uses that involve the compounds. The compounds may be useful in inhibiting the activity of a kinase, down-regulating the transcription of MYC or MCL-1, inhibiting the growth of a cell, inducing apoptosis of a cell, treating a disease, and/or preventing a disease (e.g., proliferative disease, cystic fibrosis).
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公开(公告)号:US20240277852A1
公开(公告)日:2024-08-22
申请号:US18559655
申请日:2022-05-19
发明人: Nathanael S. Gray , Mingxing Teng , Eric Wang , Jie Jiang , Tinghu Zhang , Lewis C. Cantley , Eric S. Fischer , Katherine A. Donovan
IPC分类号: A61K47/55 , A61K31/505 , A61K31/506 , A61K31/5383 , A61K47/54 , C07D239/42 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D409/04 , C07D409/10 , C07D417/04 , C07D498/14
CPC分类号: A61K47/55 , A61K31/505 , A61K31/506 , A61K31/5383 , A61K47/545 , C07D239/42 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D409/04 , C07D409/10 , C07D417/04 , C07D498/14
摘要: The present invention relates to compounds, compositions, and methods for treating diseases or conditions by modulating (e.g., reducing) the level or activity of at least one of PIP4K2A, PIP4K2B, and PIP4K2C.
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公开(公告)号:US20220175722A1
公开(公告)日:2022-06-09
申请号:US17601605
申请日:2020-04-09
发明人: Nathanael Gray , Tinghu Zhang , Guangyan Du , Nathaniel Henning , Jie Jiang
IPC分类号: A61K31/403 , A61K31/426 , A61K31/473 , A61K31/519 , A61K47/54 , A61K47/55
摘要: The present invention relates to bispecific compounds, compositions, and methods for treating diseases or conditions characterized or mediated by aberrant fibroblast growth factor receptor 2 (FGFR2) activity.
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公开(公告)号:US20220153722A1
公开(公告)日:2022-05-19
申请号:US17442923
申请日:2020-04-02
发明人: Nathanael Gray , Nicholas Kwiatkowski , Eric Fischer , Katherine Donovan , Tinghu Zhang , Mingxing Teng , Jie Jiang
IPC分类号: C07D401/14 , C07D417/12 , A61K47/55
摘要: The present invention relates to bifunctional compounds, compositions, and methods for treating diseases or conditions mediated by dysfunctional cyclin-dependent kinase 2 (CDK2) and CDK5 activity.
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