Selective glycosidase inhibitors and uses thereof

摘要

The invention provides compounds of formula (I) 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 each R1 is independently H or acetyl; R2 is NR42, or NR4OR4; R3 is OH, OAcyl, N3, or NH2; and each R4 is independently selected from the group consisting of: H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, and cycloalkyl, each excepting hydrogen optionally substituted from one up to the maximum number of substituents with F, OH, or OC(O)CH3, with the proviso that when each R1 is H and R3 is OH, R2 excludes N(CH3)2; and with the proviso that when each R1 is COCH3 and R3 is OC(O)CH3, R2 excludes N(CH3)2, NHCH3, NH(CH2)2CH3, NHCH(CH3)2, NH(CH2)3CH3, and NH(cyclohexyl).