COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE Russian patent published in 2018 - IPC C07D413/06 C07D413/14 C07D417/14 C07D207/16 C07D405/06 C07D401/06 C07D403/06 C07D413/12 C07D417/12 C07D405/12 C07J43/00 A61K31/422 A61K31/427 A61P35/00 

Abstract RU 2666530 C2

FIELD: chemistry.

SUBSTANCE: invention relates to bifunctional compounds. In particular, the invention relates to compounds which contain, at one end, a VHL ligand attached to ubiquitin ligase, and at the other end, a group that binds the target protein, so that the target protein is placed in close proximity to the ubiquitin ligase to effect degradation (and inhibition) of this protein, exhibits a wide range of pharmacological activity associated with compounds according to the present invention, associated with degradation / inhibition of target polypeptides.

EFFECT: inventions can be used as modulators of target ubiquitination, especially inhibitors of different polypeptides and other proteins that are degraded and / or otherwise inhibited by bifunctional compounds in accordance with the present invention.

32 cl, 19 dwg, 2 tbl, 1 ex

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RU 2 666 530 C2

Authors

Kruz Krejg M.

Bakli Dennis

Chulli Alessio

Jergensen Uillyam

Geriss Piter S.

Van Molle Inge

Gustafson Dzheffri

Tkhe Khen-Sop

Mishel Zhyulen

Khojer Dentin Uejd

Rot Anke G.

Kharling Dzhon Devid

Smit Yan Edvard Devid

Miakh Afdzhal Khussejn

Kampo Sebastyan Andre

Le Zhoell

Dates

2018-09-11Published

2013-01-11Filed