GLYCOSIDASE INHIBITORS AND USES THEREOF

摘要

The invention provides compounds for 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 R1 is H and R2 is C(O)NR112, or R1 is C(O)NR112 and R2 is H, or R1 is H and R2 is selected from the group consisting of: H, CH3, CH2F, CHF2, and CH2OH, where each R11 is independently H or C1-6 alkyl; R3 is H and R4 is OH, or R3 is H and R4 is H, or R3 is H and R4 is F, or R3 is F and R4 is H, or R3 is F and R4 is F, or R3 is OH and R4 is H; R5 is H and R6 is OH, or R5 is H and R6 is H, or R5 is H and R6 is F, or R5 is F and R6 is H, or R5 is F and R6 is F, or R5 is OH and R6 is H; R7 is H and R8 is OH, or R7 is H and R8 is H, or R7 is H and R8 is F, or R7 is F and R8 is H, or R7 is F and R8 is F, or R7 is OH and R8 is H; R9 is selected from the group consisting of: H, CH3, CH2F, CHF2, and CH2OH; and R10 is selected from the group consisting of: H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, acyl, C8-20 arylalkylacyl, C3-20 heteroarylalkylacyl, C7-20 arylalkyl, C8-20 arylalkenyl, C8-20 arylalkynyl, C2-20 heteroarylalkyl, C3-20 heteroarylalkenyl, and C3-20 heteroarylalkynyl, each excluding H optionally substituted from one to four substituents with one of more of halo, OH, OCF3, CN, SO2NH2, SO2Me, C(O)NH2, CH2F, CHF2, CF3, CH2CH2F, CH2CF3, CH2CH2CH2F, C1-6 alkyl, C1-6 alkoxy, or C3-7 cycloalkyl.