发明名称 |
COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE. |
摘要 |
The present invention relates to bifunctional compounds, 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 present invention is directed to compounds, which contain on one end a VHL ligand which binds to the 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. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides. |
申请公布号 |
MX2014008520(A) |
申请公布日期 |
2015.08.14 |
申请号 |
MX20140008520 |
申请日期 |
2013.01.11 |
申请人 |
YALE UNIVERSITY |
发明人 |
CRAIG M. CREWS;DENNIS BUCKLEY;ALESSIO CIULLI;WILLIAM JORGENSEN;PETER C. GAREISS;INGE VAN MOLLE;JEFFREY GUSTAFSON;HYUN-SEOP TAE;JULIEN MICHEL;DENTIN WADE HOYER;ANKE G. ROTH;JOHN DAVID HARLING;IAN EDWARD DAVID SMITH;AFJAL HUSSAIN MIAH;SEBASTIEN ANDRE CAMPOS;JOELLE LE |
分类号 |
C07K19/00;C07D207/26;C07D413/12;C07D413/14;C07J9/00 |
主分类号 |
C07K19/00 |
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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