| 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. |
| 申请人 |
YALE UNIVERSITY;GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT;CAMBRIDGE ENTERPRISE LIMITED |
发明人 |
CREWS, CRAIG, M. CM;BUCKLEY, DENNIS D;CIULLI, ALESSIO A;JORGENSEN, WILLIAM W;GAREISS PETER, C. PC;VAN MOLLE, INGE I;GUSTAFSON, JEFFREY J;TAE, HYUN-SEOP H-S;MICHEL, JULIEN J;HOYER, DENTON, WADE DW;ROTH, ANKE, G. AG;HARLING, JOHN, DAVID JD;SMITH, IAN EDWARD, DAVID IED;MIAH, AFJAL, HUSSAIN AH;CAMPOS, SEBASTIEN, ANDRE SA;LE, JOELLE J |
