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公开(公告)号：US20190016703A1
公开(公告)日：2019-01-17
申请号：US16066150
申请日：2016-12-29
发明人： Nathanael S. GRAY , James BRADNER , Pasi JANNE , Jaebong JANG , Hwan Geun CHOI , Eunhwa KO , Joong-Heui CHO
IPC分类号： C07D401/14 , A61P35/00 , A61K47/54 , A61K47/18 , A61K47/08
摘要： The present invention provides bifunctional compounds which act as protein degradation inducing moieties for a HER family protein, such as Her3. The present 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：US20200010418A1
公开(公告)日：2020-01-09
申请号：US16575733
申请日：2019-09-19
发明人： James BRADNER , Michael ERB , Jun QI
IPC分类号： C07D211/44 , C07D401/14 , C07D401/04 , C07D413/04 , C07D239/78 , C07D471/04 , C07D211/58 , C07D213/30 , A61P35/00
摘要： The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof.
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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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6.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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7.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：US20180148410A1
公开(公告)日：2018-05-31
申请号：US15577845
申请日：2016-06-03
发明人： James BRADNER , Michael ERB , Jun QI
IPC分类号： C07D211/44 , C07D471/04 , C07D413/04 , C07D401/14 , A61P35/00 , C07D239/78 , C07D213/30 , C07D211/58 , C07D401/04
CPC分类号： C07D211/44 , A61P35/00 , C07D211/58 , C07D213/30 , C07D239/78 , C07D401/04 , C07D401/14 , C07D413/04 , C07D471/04
摘要： The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof.
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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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