发明名称 |
MDM2-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE |
摘要 |
The description relates to MDM2 binding 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 MDM2 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. |
申请公布号 |
WO2017011371(A1) |
申请公布日期 |
2017.01.19 |
申请号 |
WO2016US41691 |
申请日期 |
2016.07.11 |
申请人 |
ARVINAS, INC |
发明人 |
CREW, Andrew, P.;CREWS, Craig, M.;DONG, Hanqing;QIAN, Yimin;WANG, Jing |
分类号 |
C07D223/00;C07D231/12;C07D261/00;G01N33/50;G01N33/53 |
主分类号 |
C07D223/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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