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    HYDROPHOBICALLY TAGGED SMALL MOLECULES AS INDUCERS OF PROTEIN DEGRADATION
    4.
    发明申请
    HYDROPHOBICALLY TAGGED SMALL MOLECULES AS INDUCERS OF PROTEIN DEGRADATION 有权
    作为蛋白质降解的诱导剂的疏水性标签小分子

    公开(公告)号：US20150274738A1

    公开(公告)日：2015-10-01

    申请号：US14436657

    申请日：2013-10-18

    申请人： DANA-FARBER CANCER INSTITUTE, INC. ,  YALE UNIVERSITY

    发明人： Nathanael Gray ,  Ting Xie ,  Sang Min Lim ,  Pasi A. Janne ,  Craig M. Crews

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.

    摘要翻译： 提供式（I）的双功能小分子：或其药学上可接受的盐，其中M表示共价或非共价地结合激酶例如Her3蛋白激酶的小有机分子; L1表示连接体; RH表示疏水基。 式（I）化合物的实例是式（II）的化合物：还提供了包含式（I）或（II）的化合物的药物组合物和使用这些化合物治疗增殖性疾病的方法。

    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.

    MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
    7.
    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 BTK PROTEOLYSIS AND METHODS OF USE
    8.
    发明申请
    MODULATORS OF BTK PROTEOLYSIS AND METHODS OF USE 审中-公开

    公开(公告)号：US20190276459A1

    公开(公告)日：2019-09-12

    申请号：US16297282

    申请日：2019-03-08

    申请人： Yale University

    发明人： Craig M. Crews ,  Saul Jaime-Figueroa ,  Momar Toure

    IPC分类号： C07D487/04 ,  A61K47/54 ,  A61K47/14 ,  A61K47/10 ,  C07D401/14 ,  A61P35/02

    摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.