BENZOFURAZAN ANTIMYLOID COMPOUNDS AND METHODS Russian patent published in 2018 - IPC C07D413/04 C07D271/12 A61K31/4245 A61P25/28 

FIELD: pharmacology.

SUBSTANCE: invention relates to compounds of formula I

,

where R₁₁ is selected from the group consisting of benzylamino, N-methylbenzylamino, N-methyl(4-fluorobenzyl)amino, N-methyl(4-methoxybenzyl)amino, N-methyl(3,5-dimethoxybenzyl)amino, N-methyl(pyridine-2-yl)amino, N-methyl(pyridin-3-yl)amino, piperidino, 4-methylpiperazin-1-yl, morpholino, thiomorpholino, pyrrolidino, 3-methoxypyrrolidin-1-yl, pyrrolidin-3-ol-1-yl, 2-(2-methanol-1-yl)pyrrolid-1-yl, 2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl, 2-(2-propanol-2-yl)pyrrolidin-1-yl, isoindolin-2-yl, 4-(pyrrolidin-1-yl)piperidin-1-yl, N,N-diethylamino, N-methyl-N-ethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-ethynylamino, N-(thiazol-2-ylmethyl)-N-methylamino, azetidin-1-yl, 3-methyl-3-ol-azetidin-1-yl, 3-(ethanol-2-yl)azetidin-1-yl, 3-methoxyazetidin-1-yl, 3-hydroxyazetidin-1-yl, 3-ethoxyazetidin-1-yl, 3-isopropoxyazetidin-1-yl, 3-(2-propanol-2-yl)azetidin-1-yl, 3-(morpholinomethyl)azetidin-1-yl, 3-morpholinoazetidin-1-yl, 3-(pyrrolidin-1-yl)azetidin-1-yl, 3-(pyrrolidin-1-ylmethyl)azetidin-1-yl, 3-(1-methoxyethyl)azetidin-1-yl, N-(3-(N,N-dimethylamino)propyl)-N-methylamino and 4-(N,N-dimethylamino)piperidin-1-yl; R₁₃ is selected from the group consisting of 3-(ethanol-1-yl)phenyl, 3-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 2-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 4-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 3-(3-ol-oxetan-3-yl)phenyl, 3-((piperazin-1-yl)methanon-2-yl)phenyl, 3-((morpholin-1-yl)methanon-2-yl)phenyl, 3-((pyrrolidin-1-yl)methanon-2-yl)phenyl, 3-((N-cyclopropyl)amide-2-yl)phenyl, 3-ol-oxetan-3-yl, 2-ol-but-3-en-4-yl and 2-ol-2-trifluoromethyl-(1,1,1-trifluoro)but-3-en-4-yl; and R₁₂ and R₁₄ each independently is hydrogen.

EFFECT: new compounds are obtained that are useful for treatment of an amyloid disease, such as Alzheimer's disease.

11 cl, 2 tbl, 7 dwg