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1.发明公开公开(公告)号：US20240342173A1
公开(公告)日：2024-10-17
申请号：US18439926
申请日：2024-02-13
发明人： James BRADNER , Jun QI , Dennis BUCKLEY , Leonard I. ZON , Elizabeth MACARI
IPC分类号： A61K31/517 , A61K31/225 , A61K31/403 , A61K31/506 , A61K31/519 , A61K31/5415 , A61K31/55 , A61K31/7048 , A61K45/06 , A61P7/06
CPC分类号： A61K31/517 , A61K31/225 , A61K31/403 , A61K31/506 , A61K31/519 , A61K31/5415 , A61K31/55 , A61K31/7048 , A61P7/06 , A61K45/06
摘要： The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.
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2.发明申请公开(公告)号：US20190263823A1
公开(公告)日：2019-08-29
申请号：US16343977
申请日：2017-11-22
IPC分类号： C07D487/04 , C07D417/14 , C07D401/14 , C07D471/04 , C07D513/04 , A61K47/54
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 protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
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公开(公告)号：US20220008420A1
公开(公告)日：2022-01-13
申请号：US17175079
申请日：2021-02-12
发明人： James BRADNER , Jun QI , Dennis BUCKLEY , Leonard I. ZON , Elizabeth MACARI
IPC分类号： A61K31/517 , A61P7/06 , A61K31/225 , A61K31/403 , A61K31/506 , A61K31/519 , A61K31/5415 , A61K31/55 , A61K31/7048
摘要： The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.
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4.发明申请公开(公告)号：US20190314374A1
公开(公告)日：2019-10-17
申请号：US16315899
申请日：2017-07-13
发明人： James BRADNER , Jun QI , Dennis BUCKLEY , Leonard I. ZON , Elizabeth MACARI
IPC分类号： A61K31/517 , A61K31/55 , A61K31/403 , A61K31/5415 , A61K31/225 , A61P7/06 , A61K31/7048 , A61K31/519 , A61K31/506
摘要： The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.
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公开(公告)号：US20190209535A1
公开(公告)日：2019-07-11
申请号：US16312591
申请日：2017-06-23
发明人： James BRADNER , Dennis BUCKLEY , Lara GECHIJIAN
IPC分类号： A61K31/4365 , A61K31/4184 , A61K47/55 , 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 tripartite motif-containing 24 (TRIM24). The present application also relates to methods for the targeted degradation of TRIM24 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to TRIM24 which can be utilized in the treatment of disorders modulated by TRIM24.
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公开(公告)号：US20230131952A1
公开(公告)日：2023-04-27
申请号：US18082195
申请日：2022-12-15
IPC分类号： C07D487/04 , A61K47/54 , C07D401/14 , C07D417/14 , C07D471/04 , C07D513/04 , C07D495/04 , A61K45/06 , C07D209/34
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 protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
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公开(公告)号：US20210061811A1
公开(公告)日：2021-03-04
申请号：US17096026
申请日：2020-11-12
IPC分类号： C07D487/04 , A61K47/54 , C07D401/14 , C07D417/14 , C07D471/04 , C07D513/04 , C07D495/04 , A61K45/06 , C07D209/34
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 protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
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公开(公告)号：US20200216454A1
公开(公告)日：2020-07-09
申请号：US16066149
申请日：2016-12-29
发明人： Nathanael S. GRAY , James BRADNER , Pasi JANNE , Jaebong JANG , Dennis BUCKLEY , Dennis DOBROVOLSKY
IPC分类号： C07D487/04
摘要： The invention provides bifunctional compounds which act as protein degradation inducing moieties for a HER family protein, such as Her3. The invention also provides methods for the targeted degradation of a HER family protein through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to the HER family protein which can be utilized in the treatment of disorders modulated by a HER family protein.
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公开(公告)号：US20190247509A1
公开(公告)日：2019-08-15
申请号：US16312586
申请日：2017-06-23
IPC分类号： A61K47/55 , A61K47/54 , C07D495/04 , C07D471/04
CPC分类号： A61K47/55 , A61K47/545 , C07D471/04 , C07D495/04
摘要： The present application provides bifunctional compounds of Formula (I): or Targeting Ligand or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for bromodomain-containing protein 9 (BRD9). The present application also provides methods for the targeted degradation of BRD9 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BRD9 which can be utilized in the treatment of disorders modulated by BRD9.
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