Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase

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United States of America Patent

APP PUB NO 20240317729A1
SERIAL NO

18667078

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Abstract

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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.

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International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
BUCKLEY, DENNIS New Haven, US 40 1242
CAMPOS, SEBASTIEN ANDRE STEVENAGE, HERTFORDSHIRE, GB 17 313
CIULLI, ALESSIO CAMBRIDGE, GB 13 169
CREWS, CRAIG M New Haven, US 73 2174
GAREISS, PETER C New Haven, US 5 162
GUSTAFSON, JEFFREY New Haven, US 4 277
HARLING, JOHN DAVID STEVENAGE, HERTFORDSHIRE, GB 38 489
HOYER, DENTON WADE New Haven, US 8 37
JORGENSEN, WILLIAM L New Haven, US 23 234
LE, JOELLE STEVENAGE, HERTFORDSHIRE, GB 45 655
MIAH, AFJAL HUSSAIN STEVENAGE, HERTFORDSHIRE, GB 7 229
MICHEL, JULIEN EDINBURGH, GB 5 162
ROTH, ANKE G LEVENHAGEN, DE 3 162
SMITH, IAN EDWARD DAVID STEVENAGE, HERTFORDSHIRE, GB 22 345
TAE, HYUN-SEOP New Haven, US 4 162
VAN, MOLLE INGE CAMBRIDGE, GB 4 162

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