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    Small molecules for inducing selective protein degradation and uses thereof
    1.
    发明授权
    Small molecules for inducing selective protein degradation and uses thereof 有权

    公开(公告)号：US11802132B2

    公开(公告)日：2023-10-31

    申请号：US16969772

    申请日：2019-02-22

    Applicant: DANA-FARBER CANCER INSTITUTE, INC.

    Inventor： Jun Qi ,  Lei Wu ,  Kenneth C. Anderson ,  Yan Song ,  Paul Park ,  Dharminder Chauhan

    IPC: C07D495/14 ,  C07D211/60 ,  A61P35/00

    CPC classification number: C07D495/14 ,  A61P35/00 ,  C07D211/60

    Abstract: Provided herein are bifunctional compounds that bind a target protein (e.g., a selected protein) and/or induce ubiquitination for degradation of the target protein. In particular, provided are compounds that bind a bromodomain or bromodomain-containing protein (e.g., BET proteins) or histone methyltransferases (HMTs, e.g., enhancer of zeste homolog 1 (EZH1), or FKBP12) and can promote its degradation by recruiting it to the ubiquitin receptor RPN13 (e.g., RA190), for proteasomal degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating and/or preventing diseases (e.g., proliferative diseases, cancers, benign neoplasms, pathological angiogenesis, inflammatory diseases, and autoimmune diseases) and musculoskeletal diseases, and methods of inducing the degradation of a target (e.g., a target protein) by recruiting it to the ubiquitin receptor RPN13 of the proteasome in a subject by administering a compound or composition described herein.

    CYANO THIENOTRIAZOLODIAZEPINES AND USES THEREOF
    4.
    发明申请
    CYANO THIENOTRIAZOLODIAZEPINES AND USES THEREOF 有权

    公开(公告)号：US20210206779A9

    公开(公告)日：2021-07-08

    申请号：US15758822

    申请日：2016-09-09

    Applicant: Dana-Farber Cancer Institute, Inc.

    Inventor： James E. Bradner ,  Jun Qi ,  Minoru Tanaka ,  Dennis Buckley

    IPC: C07D495/14

    Abstract: The present invention provides compounds and pharmaceutically compositions thereof. The compounds and compositions are 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.

    EZH2 INHIBITORS AND USES THEREOF
    5.
    发明申请
    EZH2 INHIBITORS AND USES THEREOF 审中-公开

    公开(公告)号：US20190135796A1

    公开(公告)日：2019-05-09

    申请号：US16095188

    申请日：2017-04-21

    Applicant: Dana-Farber Cancer Institute, Inc.

    Inventor： James E. Bradner ,  Joshiawa Paulk ,  Jun Qi

    IPC: C07D405/14

    Abstract: The present disclosure provides compounds of any one of Formulae (I), (II), and (III). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

    USES OF DIAZEPANE DERIVATIVES
    8.
    发明申请
    USES OF DIAZEPANE DERIVATIVES 审中-公开
    DIAZEPANE DERIVATIVES的用途

    公开(公告)号：US20170008895A1

    公开(公告)日：2017-01-12

    申请号：US15115085

    申请日：2015-02-02

    Applicant: DANA-FARBER CANCER INSTITUTE, INC.

    Inventor： James E. Bradner ,  Nathanael S. Gray ,  Jun Qi ,  Michael R. McKeown ,  Dennis Buckley

    IPC: C07D487/04 ,  A61K31/5513

    Abstract: 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.

    Abstract translation: 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。

    DOT1L PROBES
    9.
    发明申请
    DOT1L PROBES 有权

    公开(公告)号：US20160146817A1

    公开(公告)日：2016-05-26

    申请号：US14904572

    申请日：2014-07-28

    Applicant: DANA-FARBER CANCER INSTITUTE, INC.

    Inventor： James E. Bradner ,  Alexander Federation ,  Jun Qi

    IPC: G01N33/573 ,  C07H19/16 ,  G01N33/58

    CPC classification number: G01N33/573 ,  A61K31/7076 ,  C07H19/16 ,  G01N33/582 ,  G01N2333/91017 ,  G01N2500/02

    Abstract: The present invention relates to compound that bind Histone H3-lysine79 (H3K79) methyl transferase (DOTIL). The disclosed compounds are useful as for assessing the activity of DOTIL and for identifying inhibitors of DOTIL. Described herein are probes useful for both assessing the activity of DOTIL and identifying inhibitors of DOTIL. These probes can be used in various assays, including Amplified Luminescent Proximity Homogeneous Assays (“ALPHA” assays), Differential Scanning Fluorimetry (DFS) Assay, and Fluorescence Polarization (FP) assays used for high-throughput screening (HTS) for small molecule drug discovery. The compounds can also be used as a pull down agent for target identification.

    Abstract translation: 本发明涉及结合组蛋白H3-赖氨酸79（H3K79）甲基转移酶（DOTIL）的化合物。 所公开的化合物可用于评估DOTIL的活性和用于鉴定DOTIL的抑制剂。 本文描述的是可用于评估DOTIL的活性和鉴定DOTIL抑制剂的探针。 这些探针可用于各种测定，包括用于小分子药物的高通量筛选（HTS）的扩增发光近似均质测定（“ALPHA”测定），差示扫描荧光测定（DFS）测定和荧光偏振（FP）测定） 发现。 这些化合物也可以用作目标识别的下拉剂。

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