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1. 发明公开

EP3579847A1 TUNABLE ENDOGENOUS PROTEIN DEGRADATION WITH HETEROBIFUNCTIONAL COMPOUNDS 审中-实审转让
公开(公告)号：EP3579847A1
公开(公告)日：2019-12-18
申请号：EP18751395.7
申请日：2018-02-08
申请人： Dana Farber Cancer Institute, Inc.
发明人： BUCKLEY, Dennis , WINTER, Georg , PHILLIPS, Andrew, J. , HEFFERNAN, Timothy, P. , BRADNER, James , ROBERTS, Justin , NABET, Behnam.
IPC分类号： A61K35/17 , A61K35/15 , A61K35/12 , A61K38/16 , C12N9/64 , C12N5/10 , C12N5/071 , A61P35/00 , A61P35/04

2. 发明公开

EP3177626A1 DIAZEPANE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：二氮杂环庚烷衍生物及其用途
公开(公告)号：EP3177626A1
公开(公告)日：2017-06-14
申请号：EP15830298.4
申请日：2015-08-07
申请人： Dana Farber Cancer Institute, Inc.
发明人： BRADNER, James E. , BUCKLEY, Dennis
IPC分类号： C07D487/04 , C07D243/06
CPC分类号： C07D487/04
摘要： The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of 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, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
摘要翻译：本公开提供了式（I）的化合物及其药学组合物。已发现式（I）的化合物结合含溴结构域和/或含溴结构域的蛋白质（例如溴和额外末端（BET）蛋白质）。还提供了用于抑制溴结构域和/或含溴结构域的蛋白质的活性（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化合物和药物组合物的方法，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，神经疾病，代谢性疾病，内分泌疾病和放射性中毒）。化合物，药物组合物和试剂盒也可用于男性避孕。

3. 发明公开

EP3099696A1 DIAZEPANE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：二氮杂环庚烷衍生物及其用途
公开(公告)号：EP3099696A1
公开(公告)日：2016-12-07
申请号：EP15744026.4
申请日：2015-02-02
申请人： Dana-Farber Cancer Institute, Inc.
发明人： BRADNER, James, E. , GRAY, Nathanael , QI, Jun , MCKEOWN, Michael, R. , BUCKLEY, Dennis
IPC分类号： C07D487/04 , A61K45/06
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D495/14
摘要： The present invention provides compounds of any one of Formulae (I), (II-C) (
e.g. , Formula (II)), and (III), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I), (II-C), and (III) 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：本发明提供了式（I），（II-C）（例如式（II））和（III）中任何一个的化合物及其药物组合物。式（I），（II-C）和（III）中任一个的化合物被认为是溴结构域和/或含溴结构域的蛋白质（例如溴和额外末端（BET）蛋白质）的结合剂。还提供了使用所述化合物和药物组合物抑制溴结构域和/或含溴结构域的蛋白质的活性（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，代谢性疾病，内分泌疾病和放射性中毒）。化合物，药物组合物和试剂盒也可用于男性避孕。

4. 发明公开

EP3331905A1 TARGETED PROTEIN DEGRADATION TO ATTENUATE ADOPTIVE T-CELL THERAPY ASSOCIATED ADVERSE INFLAMMATORY RESPONSES 有权
公开(公告)号：EP3331905A1
公开(公告)日：2018-06-13
申请号：EP16754061.6
申请日：2016-08-08
申请人： Dana-Farber Cancer Institute, Inc.
发明人： BRADNER, James , ROBERTS, Justin , NABET, Behnam , WINTER, Georg , PHILLIPS, Andrew J. , HEFFERNAN, Timothy P. , BUCKLEY, Dennis
IPC分类号： C07K16/00 , A61K35/17 , A61P35/00
CPC分类号： C12N15/11 , A61K31/4525 , A61K31/4545 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/551 , A61K31/5513 , A61K31/575 , A61K31/58 , A61K35/17 , A61K48/00 , A61K2035/122 , C07K14/47 , C07K14/7051 , C07K14/70517 , C07K14/70521 , C07K16/00 , C07K16/2863 , C07K2317/622 , C07K2319/03 , C07K2319/20 , C07K2319/95 , C12N15/907 , C12N2310/20 , C12N2800/80
摘要： The present invention provides a means to modulate gene expression in vivo in a manner that avoids problems associated with CRISPR endogenous protein knock-out or knock-in strategies and strategies that provide for correction, or alteration, of single nucleotides. The invention includes inserting into the genome a nucleotide encoding a heterobifunctional compound targeting protein (dTAG) in-frame with the nucleotide sequence of a gene encoding an endogenously expressed protein of interest which, upon expression, produces an endogenous protein-dTAG hybrid protein. This allows for targeted protein degradation of the dTAG and the fused endogenous protein using a heterobifunctional compound.

5. 发明公开

EP3256470A1 METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES 有权转让
标题翻译：通过双功能分子诱导目标蛋白降解的方法
公开(公告)号：EP3256470A1
公开(公告)日：2017-12-20
申请号：EP15825649.5
申请日：2015-12-23
申请人： Dana Farber Cancer Institute, Inc.
发明人： BRADNER, James , BUCKLEY, Dennis , WINTER, Georg
IPC分类号： C07D471/04 , C07D471/14
CPC分类号： C07D401/04 , C07D401/14 , C07D471/04 , C07D471/14 , C07D475/00 , C07D487/04 , C07D495/14 , C07J43/003
摘要： The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

7. 发明公开

EP3474900A1 DEGRADATION OF BROMODOMAIN-CONTAINING PROTEIN 9 (BRD9) BY CONJUGATION OF BRD9 INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE 无效
公开(公告)号：EP3474900A1
公开(公告)日：2019-05-01
申请号：EP17816295.4
申请日：2017-06-23
申请人： Dana-Farber Cancer Institute, Inc.
发明人： BUCKLEY, Dennis , BRADNER, James , REMILLARD, David Ian
IPC分类号： A61K47/50 , C07D401/14 , A61K31/4365 , A61K31/4035

8. 发明公开

EP3474899A1 DEGRADATION OF TRIPARTITE MOTIF-CONTAINING PROTEIN 24 (TRIM24) BY CONJUGATION OF TRIM24 INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE 无效转让
公开(公告)号：EP3474899A1
公开(公告)日：2019-05-01
申请号：EP17816274.9
申请日：2017-06-23
申请人： Dana Farber Cancer Institute, Inc.
发明人： BRADNER, James , BUCKLEY, Dennis , GECHIJIAN, Lara
IPC分类号： A61K47/50 , C07D401/14 , A61K31/4365 , A61K31/4184

9. 发明公开

EP4119552A1 REGULATING CHIMERIC ANTIGEN RECEPTORS 审中-实审
公开(公告)号：EP4119552A1
公开(公告)日：2023-01-18
申请号：EP22182901.3
申请日：2018-02-08
申请人： Dana-Farber Cancer Institute, Inc.
发明人： BRADNER, James , ROBERTS, Justin , NABET, Behnam , WINTER, Georg , PHILLIPS, Andrew J. , HEFFERNAN, Timothy P. , BUCKLEY, Dennis
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , A61K31/454 , A61K35/17 , C12N5/0783 , C12N9/64 , C12N9/90
摘要： This invention is in the area of compositions and methods for regulating chimeric antigen receptor immune effector cell, for example T-cell (CAR-T), therapy to modulate associated adverse inflammatory responses, for example, cytokine release syndrome and tumor lysis syndrome, using targeted protein degradation.

10. 发明公开

EP3580212A1 REGULATING CHIMERIC ANTIGEN RECEPTORS 审中-公开
公开(公告)号：EP3580212A1
公开(公告)日：2019-12-18
申请号：EP18750939.3
申请日：2018-02-08
申请人： Dana Farber Cancer Institute, Inc.
发明人： BRADNER, James , ROBERTS, Justin , NABET, Behnam , WINTER, Georg , PHILLIPS, Andrew, J. , HEFFERNAN, Timothy, P. , BUCKLEY, Dennis
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , A61K31/454 , A61K35/17

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