COMPOUNDS AND METHODS FOR ENHANCING DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES, USING E3 UBIQUITIN LIGASE Russian patent published in 2022 - IPC C07D413/12 C07D413/14 C07D417/12 C07D417/14 A61K31/422 A61K31/427 A61P35/00 

Abstract RU 2781452 C2

FIELD: biotechnology.

SUBSTANCE: invention relates to bifunctional compounds represented by a chemical structure: PTM-L-ULM, where PTM is a small molecule of a protein-targeting fragment, which binds to intracellular target protein selected from a group consisting of focal adhesion kinase, tyrosine kinase, estrogen receptor, androgen receptor, BET protein containing bromodomain, Ras, Raf, and epidermal growth factor receptor; L is a chemical linker group binding ULM to PTM; and ULM is a small molecule of a binding fragment of ubiquitin ligase E3 Von Hippel Lindau (VHL).

EFFECT: obtaining compounds enhancing the degradation of target proteins.

16 cl, 19 dwg, 2 tbl, 1 ex

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RU 2 781 452 C2

Authors

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

Dates

2022-10-12Published

2013-01-11Filed