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    Imide-based modulators of proteolysis and associated methods of use
    2.
    发明授权
    Imide-based modulators of proteolysis and associated methods of use 有权

    公开(公告)号：US11834460B2

    公开(公告)日：2023-12-05

    申请号：US17554831

    申请日：2021-12-17

    申请人： YALE UNIVERSITY

    发明人： Craig M. Crews ,  George Burslem ,  Philipp M. Cromm ,  Saul Jaime-Figueroa ,  Momar Toure

    IPC分类号： C07D495/14 ,  C07D261/08 ,  C07D413/14 ,  C07D417/14 ,  A61P35/00

    CPC分类号： C07D495/14 ,  A61P35/00 ,  C07D261/08

    摘要： The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

    COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES
    5.
    发明申请
    COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES 审中-公开

    公开(公告)号：US20180256586A1

    公开(公告)日：2018-09-13

    申请号：US15840950

    申请日：2017-12-13

    申请人： Arvinas, Inc. ,  Yale University

    发明人： Andrew P. Crew ,  Keith R. Hornberger ,  Craig M. Crews ,  George Burslem

    IPC分类号： A61K31/529 ,  A61K31/429 ,  A61K31/454 ,  A61K45/06 ,  A61P35/02

    摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, 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 the 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.

    Imide-based modulators of proteolysis and associated methods of use
    6.
    发明授权
    Imide-based modulators of proteolysis and associated methods of use 有权

    公开(公告)号：US11220515B2

    公开(公告)日：2022-01-11

    申请号：US16258563

    申请日：2019-01-26

    申请人： YALE UNIVERSITY

    发明人： Craig M. Crews ,  George Burslem ,  Philipp M. Cromm ,  Saul Jaime-Figueroa ,  Momar Toure

    IPC分类号： C07D495/14 ,  C07D261/08 ,  A61P35/00 ,  C07D417/14 ,  C07D413/14

    摘要： The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.