SUBSTANCES PROVIDING PROTEIN DEGRADATION AND USE THEREOF Russian patent published in 2024 - IPC C07D401/14 C07D417/14 C07D487/04 C07D495/04 C07D495/14 A61K9/08 A61K9/10 A61K9/107 A61K31/517 A61K47/55 A61P35/00 

Abstract RU 2830281 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, which can be used to treat a disorder, a disease or a condition mediated by a BRD4 target protein. In formula I, X1 is a divalent fragment selected from -C(O)-; R1 is hydrogen; each R2 is independently hydrogen or -R6; ring A is , where ring B is a fused ring selected from 6-member aryl containing 0–2 nitrogen atoms; each R4 is independently hydrogen or -R6; each R6 is C1-6 alkyl; L is a divalent saturated linear C1-20 hydrocarbon chain, where 0–6 methylene links of L are independently replaced with -O- or -NR-; TBM is a target binding moiety, wherein the target binding moiety is a BRD4 binding moiety, wherein the BRD4 binding moiety is ; m is 0, 1, 2, 3 or 4; and each R is independently hydrogen. Invention also relates to a pharmaceutical composition containing said compound, and to a method of destroying a target protein in a biological sample using the same, wherein the target protein is BRD4.

EFFECT: substances providing degradation of proteins and their application are disclosed.

6 cl, 4 tbl, 11 ex

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RU 2 830 281 C1

Authors

Mejnolfi, Nello

Tszi, Nan

Chzhan, I

Vajss, Mettyu M.

Dates

2024-11-18Published

2018-09-21Filed