SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

摘要

The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

主权项

1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein X is O or S; R1 and R2 are H, or R1 is H and R2 is F, or R1 is F and R2 is H, or R1 is OR5 and R2 is H, or R1 is H and R2 is OR5; R3 is OR5 and R4 is H, or R3 is H and R4 is OR5; R6 is H, F, or OR5; each R5 is independently H or C1-6 acyl; each R7 is independently H or F; and each R8 is independently selected from the group consisting of: H, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, and C1-6 alkoxy, wherein the C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, or C1-6 alkoxy are optionally substituted from one up to the maximum number of substituents with one or more of fluoro, OH, or methyl, or the two R8 groups are connected together with the nitrogen atom to which they are attached to form a ring, said ring optionally independently substituted from one up to the maximum number of substituents with one or more of fluoro, OH, or methyl, wherein when R6 is OR5, then each R7 is H; and wherein when R1 is OR5, then R6 is H or F; and wherein when R6 is OR5, then R1 is H or F.