TRANSTHYRETIN STABILISATION Russian patent published in 2009 - IPC C07D307/91 A61K31/343 A61P7/00 

FIELD: chemistry.

SUBSTANCE: invention relates to new derivatives of dibenzofuran-4,6-dicarboxylic acid of formula 1 , where: X is absent or represents a diradical, which is chosen from a group containing -O-, -S- and -NH-, R² and R⁴ are independently chosen from a group which contains -H, -OH, -F, -CI, -Br, -CF₃ and -CO₂H, and R³ and R⁵ are independently chosen from a group which contains -H, -OH, -F, -Cl, -Br and -CO₂H, which are extremely efficient inhibitors of amyloidogenesis, exhibit high affinity and considerably high selectivity when bonding to transthyretin (TTR) compared to the rest of plasmatic proteins and compared to control compound 1. The said compounds also increase kinetic stability of the tetrameric structure of TTR.

EFFECT: design of an effective method of inhibiting formation of amyloid fibrils.

16 cl, 11 dwg