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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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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：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：US20160332993A1
公开(公告)日：2016-11-17
申请号：US15115038
申请日：2015-02-02
发明人： James E. BRADNER , Jun QI , Minoru TANAKA
IPC分类号： C07D403/12 , C07D239/48
CPC分类号： C07D403/12 , C07D239/42 , C07D239/48
摘要： The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
摘要翻译： 本发明提供式（II）的化合物（例如式（I）的化合物）及其药学上的组合物。 认为式（II）的化合物是溴结构域和/或含溴结构域的蛋白质（例如溴和额外末端（BET）蛋白）的结合物）。 还提供了使用化合物和药物组合物抑制溴结构域和/或含溴结构域蛋白的活性（例如，增加的活性）以及用于治疗和/或预防与溴结构域或溴结构域相关的疾病的方法，用途和试剂盒 （例如，增殖性疾病，心血管疾病，病毒感染，纤维化疾病，代谢疾病，内分泌疾病和放射线中毒）。 化合物，药物组合物和试剂盒也可用于男性避孕。
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公开(公告)号：US20200255422A1
公开(公告)日：2020-08-13
申请号：US16604030
申请日：2018-04-27
发明人： Jun QI , Cheng-kui PEI
IPC分类号： C07D471/04
摘要： The application relates to a compound of Formula (I): which modulates the activity of TRIM33, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which TRIM33 plays a role.
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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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