BENZOFURAZAN ANTI-AMYLOID COMPOUNDS AND METHODS

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15

申请(专利)号:

CA2883221

申请日期:

2013-08-22

公开/公告号:

CA2883221C

公开/公告日期:

2020-01-21

申请(专利权)人:

TREVENTIS CORPORATION

发明人:

MA ReedTK WoodSC BanfieldCJ Barden

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摘要:

Herein is provided a compound of Formula I: (see formula I) or a pharmaceutically acceptable salt thereof, in which 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(pyridin-2-yl)amino, N-methyl(pyridin-3-yl)amino, piperidino, 4-methylpiperzin- 1 -yl, morpholino, thiomorpholino, pyrrolidino, 3-methylpyrrolidin-1-yl, 3-methoxypyrrolidin-1-yl, pyrrolidin-3-ol-1-yl, 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-(2-methoxyethyl)-N- methylamino, N-(thiazol-2-ylmethyl)-N-methylamino, azetidin-1-yl, 3-methyl-3-ol-azetidin-1- yl, 3-(ethanol-1-yl) azetidine-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-(pyyrolidin-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-ylphenyl, 2-(1-ol-2,2,2,trifluoroethane- 1 - yl)phenyl, 4-(1-ol-2,2,2,-trifluoroethan-1-yl)phenyl, 3-(3-ol-oxetan-3-yl)phenyl, 3- acetylphenyl, 3-((piperazin-1-yl) methanonyl)phenyl, 3-((morpholin-1-yl)methanonyl)phenyl, 3-((pyrrolidine-1- yl)methanonylphenyl, 3-((N-cyclopropyl)amid-2-yl)phenyl, acetyl, trifluoroacetyl, 1-ol-2,2,2- trifluoroethan-1-yl, 3-ol-oxetan-3-yl, 1,ol-2,2,2-trifluoroethan-1-yl)thiophen-2-yl,1-ol-prop-2-en-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 are each independently hydrogen or alkyl. Uses in the treatment of amyloid disease, including Alzheimer's disease and progressive supranuclear palsy, are also provided.

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