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    MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
    2.
    发明申请
    MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE 审中-公开

    公开(公告)号：US20190315732A1

    公开(公告)日：2019-10-17

    申请号：US16375643

    申请日：2019-04-04

    申请人： Arvinas Operations, Inc. ,  Yale University

    发明人： Andrew P. Crew ,  Keith R. Hornberger ,  Jing Wang ,  Hanging Dong ,  Michael Berlin ,  Craig M. Crews

    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.

    MODULATORS OF FAK PROTEOLYSIS AND ASSOCIATED METHODS OF USE
    8.
    发明申请
    MODULATORS OF FAK PROTEOLYSIS AND ASSOCIATED METHODS OF USE 审中-公开

    公开(公告)号：US20200038513A1

    公开(公告)日：2020-02-06

    申请号：US16523219

    申请日：2019-07-26

    申请人： ARVINAS OPERATIONS, INC. ,  YALE UNIVERSITY

    发明人： Craig M. Crews ,  Philipp M. Cromm ,  Andrew P. Crew

    IPC分类号： A61K47/54 ,  A61K45/06 ,  A61K31/505 ,  A61K31/427 ,  A61K31/454

    摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of focal adhesion kinase (FAK) or protein tyrosine kinase 2 (PTK2). 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 or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.