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 that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end 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 that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides. |
申请公布号 |
US2014356322(A1) |
申请公布日期 |
2014.12.04 |
申请号 |
US201314371956 |
申请日期 |
2013.01.11 |
申请人 |
YALE UNIVERSITY ;GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ;CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE |
发明人 |
Crews Craig M.;Buckley Dennis;Ciulli Alessio;Jorgensen William;Gareiss Peter C.;Van Molle Inge;Gustafson Jeffrey;Tae Hyun-Seop;Michel Julien;Hoyer Dentin Wade;Roth Anke G.;Harling John David;Smith Ian Edward David;Miah Afjal Hussain;Campos Sebastien Andre;Le Joelle |
分类号 |
C07D413/14;A61K38/05;A61K31/5377;A61K31/437;A61K31/454;A61K31/4439;A61K31/427;A61K31/422;C07K5/08;C07J43/00;C07D471/04;C07D417/14;C07D413/06;A61K45/06;A61K38/06 |
主分类号 |
C07D413/14 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
NEW HAVEN CT US |