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    Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof
    1.
    发明授权
    Small molecules that block proteasome-associated ubiquitin receptor RPN13 function and uses thereof 有权

    公开(公告)号：US11702402B2

    公开(公告)日：2023-07-18

    申请号：US16969458

    申请日：2019-02-22

    Applicant: DANA-FARBER CANCER INSTITUTE, INC.

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

    IPC: C07D401/14 ,  A61P35/04 ,  C07D495/04

    CPC classification number: C07D401/14 ,  A61P35/04 ,  C07D495/04

    Abstract: Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety (e.g., RA190) that is a binder of the ubiquitin receptor RPN13 to induce degradation of RPN13 and thereby inhibit proteasome function. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, cancers, benign neoplasms, pathological angiogenesis, inflammatory diseases, and autoimmune diseases). Provided also are methods of inducing the degradation of ubiquitin receptor RPN13 by administering a bifunctional compound or composition described herein, wherein one component of the bifunctional compound is a binder of an E3 ubiquitin ligase (e.g., lenalidomide, thalidomide) and another component of the compound is a binder of ubiquitin receptor RPN13 (e.g., RA190) in a subject.

    Small molecules for inducing selective protein degradation and uses thereof
    3.
    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.

    SMALL MOLECULES THAT BLOCK PROTEASOME-ASSOCIATED UBIQUITIN RECEPTOR RPN13 FUNCTION AND USES THEREOF
    5.
    发明申请
    SMALL MOLECULES THAT BLOCK PROTEASOME-ASSOCIATED UBIQUITIN RECEPTOR RPN13 FUNCTION AND USES THEREOF 有权

    公开(公告)号：US20210130324A1

    公开(公告)日：2021-05-06

    申请号：US16969458

    申请日：2019-02-22

    Applicant: DANA-FARBER CANCER INSTITUTE, INC.

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

    IPC: C07D401/14 ,  A61P35/04 ,  C07D495/04

    Abstract: Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety (e.g., RA190) that is a binder of the ubiquitin receptor RPN13 to induce degradation of RPN13 and thereby inhibit proteasome function. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, cancers, benign neoplasms, pathological angiogenesis, inflammatory diseases, and autoimmune diseases). Provided also are methods of inducing the degradation of ubiquitin receptor RPN13 by administering a bifunctional compound or composition described herein, wherein one component of the bifunctional compound is a binder of an E3 ubiquitin ligase (e.g., lenalidomide, thalidomide) and another component of the compound is a binder of ubiquitin receptor RPN13 (e.g., RA190) in a subject.

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