Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase

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United States of America Patent

PATENT NO 10730862
APP PUB NO 20140356322A1
SERIAL NO

14371956

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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 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.

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Patent Owner(s)

Patent OwnerAddress
CAMBRIDGE ENTERPRISE LIMITEDCAMBRIDGE CB2 1TN

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Buckley, Dennis New Haven, US 40 1242
Campos, Sebastien Andre Stevenage, GB 17 313
Ciulli, Alessio Cambridge, GB 13 169
Crews, Craig M New Haven, US 73 2174
Gareiss, Peter C Milford, US 5 162
Gustafson, Jeffrey New Haven, US 4 277
Harling, John David Stevenage, GB 38 489
Hoyer, Denton Wade Niantic, US 8 37
Jorgensen, William Deep River, US 12 157
Le, Joelle Stevenage, GB 45 655
Miah, Afjal Hussain Stevenage, GB 7 229
Michel, Julien Edinburgh, GB 5 162
Roth, Anke G Levenhagen, DE 3 162
Smith, Ian Edward David Stevenage, GB 22 345
Tae, Hyun-Seop New Haven, US 4 162
Van, Molle Inge Cambridge, GB 4 162

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