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公开(公告)号：US12098154B2
公开(公告)日：2024-09-24
申请号：US17715874
申请日：2022-04-07
IPC分类号： C07D487/04 , A61K45/06 , A61P43/00 , C07D473/16 , C07D473/34 , C07K14/47
CPC分类号： C07D473/16 , A61K45/06 , A61P43/00 , C07D473/34 , C07D487/04 , C07K14/4738
摘要： The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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公开(公告)号：USRE50030E1
公开(公告)日：2024-07-02
申请号：US17534896
申请日：2021-11-24
发明人： Steven P. Treon , Sara Jean Buhrlage , Nathanael S. Gray , Li Tan , Guang Yang
IPC分类号： C07D239/47 , A61K31/506 , A61K45/06 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D487/04
CPC分类号： C07D239/47 , A61K31/506 , A61K45/06 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D487/04
摘要： The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating Waldenström's macroglobulinemia (WM) and other B cell neoplasm in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase-1 (TAK1), and/or a Src family kinase.
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公开(公告)号：US11827636B2
公开(公告)日：2023-11-28
申请号：US17561032
申请日：2021-12-23
IPC分类号： C07D471/04 , C07D471/10 , A61K47/18 , A61K47/54 , A61P35/00
CPC分类号： C07D471/04 , A61K47/18 , A61K47/545 , C07D471/10 , A61P35/00
摘要： The present application provides bifunctional compounds of Formula (Ia) or (Ib):
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.-
公开(公告)号：US11814379B2
公开(公告)日：2023-11-14
申请号：US16973276
申请日：2019-06-14
发明人： Nathanael S. Gray , Jaebong Jang , Pasi Janne , Jieun Son
IPC分类号： C07D215/54 , C07D401/12 , C07D471/04 , C07D487/04 , A61P35/00 , C07D417/12
CPC分类号： C07D471/04 , A61P35/00 , C07D215/54 , C07D401/12 , C07D417/12 , C07D487/04
摘要： The application relates to a compound having Formula I:
which modulates the activity of HER2 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 plays a role.-
公开(公告)号：US20230348434A1
公开(公告)日：2023-11-02
申请号：US18309164
申请日：2023-04-28
发明人： Nathanael S. Gray , Pasi Janne , Hwan Geun Choi , Jaebong Jang
IPC分类号： C07D403/04 , C07D471/04 , C07D403/14 , C07D487/04
CPC分类号： C07D403/04 , C07D471/04 , 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.-
公开(公告)号：US11712458B2
公开(公告)日：2023-08-01
申请号：US16963993
申请日：2019-01-29
CPC分类号： A61K38/05 , A61K47/54 , A61K47/545 , A61K47/62
摘要： The present application provides bifunctional compounds of Formula X or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
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公开(公告)号：US20230192644A1
公开(公告)日：2023-06-22
申请号：US17926074
申请日：2021-05-20
发明人： Nathanael S. Gray , Eric S. Fischer , Alyssa Verano , Hu Liu , Tinghu Zhang , Lyn H. Jones , Eric S. Wang , Radoslaw Nowak , Jianwei Che
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, and tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with Helios and which may benefit from Helios degradation.
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公开(公告)号：US20230183240A9
公开(公告)日：2023-06-15
申请号：US17715874
申请日：2022-04-07
IPC分类号： C07D473/16 , C07D473/34 , C07D487/04 , C07K14/47 , A61K45/06 , A61P43/00
CPC分类号： C07D473/16 , C07D473/34 , C07D487/04 , C07K14/4738 , A61K45/06 , A61P43/00
摘要： The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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公开(公告)号：US11673882B2
公开(公告)日：2023-06-13
申请号：US16950465
申请日：2020-11-17
发明人： Nathanael S. Gray , Pasi Janne , Hwan Geun Choi , Jaebong Jang
IPC分类号： C07D403/04 , C07D471/04 , C07D403/14 , C07D487/04
CPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , 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.-
公开(公告)号：US20230158157A1
公开(公告)日：2023-05-25
申请号：US17801709
申请日：2021-02-24
发明人： John M. Hatcher , Nathanael S. Gray , Baishan Jiang , Tinghu Zhang , Jianwei Che , Yang Gao , Lyn Howard Jones
IPC分类号： A61K47/55
CPC分类号： A61K47/55
摘要： Disclosed are bispecific compounds (degraders) that target ALK or ALK and FAK for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the bispecific compounds to treat diseases and disorders characterized or mediated by aberrant ALK or ALK and FAK activity.
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