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    Modulators of estrogen receptor proteolysis and associated methods of use
    3.
    发明授权
    Modulators of estrogen receptor proteolysis and associated methods of use 有权

    公开(公告)号：US11384063B2

    公开(公告)日：2022-07-12

    申请号：US16810764

    申请日：2020-03-05

    申请人： Arvinas Operations, Inc.

    发明人： Andrew P. Crew ,  Hanqing Dong ,  Jing Wang ,  Yimin Qian

    IPC分类号： C07D401/14 ,  C07D471/04 ,  C07D409/12 ,  C07D403/06 ,  A61P35/00 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D403/14

    摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which 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 present disclosure exhibits 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.

    COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR AND ASSOCIATED METHODS OF USE
    4.
    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 proteolysis and associated methods of use
    7.
    发明授权
    Modulators of proteolysis and associated methods of use 有权

    公开(公告)号：US11161841B2

    公开(公告)日：2021-11-02

    申请号：US16375643

    申请日：2019-04-04

    申请人： Arvinas Operations, Inc.

    发明人： Andrew P. Crew ,  Keith R. Hornberger ,  Jing Wang ,  Hanqing Dong

    IPC分类号： C07D417/14 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

    摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which 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 present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.