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    HYDROPHOBICALLY TAGGED SMALL MOLECULES AS INDUCERS OF PROTEIN DEGRADATION
    1.
    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。

    RAS INHIBITORS AND USES THEREOF
    6.
    发明申请
    RAS INHIBITORS AND USES THEREOF 审中-公开
    RAS抑制剂及其用途

    公开(公告)号：US20160046661A1

    公开(公告)日：2016-02-18

    申请号：US14775162

    申请日：2014-03-13

    申请人： DANA-FARBER CANCER INSTITUTE, INC.

    发明人： Nathanael Gray ,  Sang Min Lim ,  Hwan Geun Choi ,  Kenneth Dale Westover

    IPC分类号： C07H19/16 ,  C07F9/6561 ,  C07H19/20

    摘要： Described herein are compounds of Formulae (I)-(II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., lung cancer, large bowel cancer, pancreas cancer, biliary tract cancer, or endometrial cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject.

    摘要翻译： 本文描述了式（I） - （II）的化合物及其药学上可接受的盐及其药物组合物。 还提供了涉及用于治疗或预防增殖性疾病如癌症（例如肺癌，大肠癌，胰腺癌，胆道癌或子宫内膜癌），良性肿瘤，血管生成，炎性疾病的本发明化合物或组合物的方法和试剂盒 ，自身炎症性疾病和自身免疫性疾病。