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    RAPIDLY ACCELERATING FIBROSARCOMA PROTEIN DEGRADING COMPOUNDS AND ASSOCIATED METHODS OF USE
    2.
    发明申请
    RAPIDLY ACCELERATING FIBROSARCOMA PROTEIN DEGRADING COMPOUNDS AND ASSOCIATED METHODS OF USE 有权

    公开(公告)号：US20230081501A1

    公开(公告)日：2023-03-16

    申请号：US17459179

    申请日：2021-08-27

    申请人： Arvinas Operations, Inc.

    发明人： Keith R. Hornberger ,  Lawrence B. Snyder ,  Jing Wang

    IPC分类号： A61K31/454 ,  A61K47/55 ,  A61K31/437 ,  A61K47/54 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/45

    摘要： Bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-Raf), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds Raf, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

    COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR AND ASSOCIATED METHODS OF USE
    5.
    发明申请
    COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR AND ASSOCIATED METHODS OF USE 有权

    公开(公告)号：US20220144809A1

    公开(公告)日：2022-05-12

    申请号：US17512219

    申请日：2021-10-27

    申请人： Arvinas Operations, Inc.

    发明人： Hanqing Dong ,  Lawrence B. Snyder ,  Jing Wang

    IPC分类号： C07D401/14 ,  A61K45/06

    摘要： Bifunctional compounds, which find utility as modulators of androgen receptor (AR), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds AR, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

    MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
    7.
    发明公开
    MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE 审中-公开

    公开(公告)号：US20240325547A1

    公开(公告)日：2024-10-03

    申请号：US18610001

    申请日：2024-03-19

    申请人： Arvinas Operations, Inc.

    发明人： MICHAEL BERLIN ,  Hanqing Dong ,  Dan Sherman ,  Lawrence B. Snyder ,  Jing Wang ,  Wei Zhang

    IPC分类号： A61K47/55 ,  A61K45/06 ,  A61K47/54 ,  A61P35/00

    CPC分类号： A61K47/55 ,  A61K45/06 ,  A61K47/545 ,  A61P35/00

    摘要： Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a cereblon ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.