| 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 DEVELOPMENTLIMITED;CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE |
发明人 |
CREWS, CRAIG, M.;BUCKLEY, DENNIS;CIULLI, ALESSIO;JORGENSEN, WILLIAM;GAREISS, PETER, C.;MOLLE, INGE, VAN;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 |
