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US 9,809,537 B2Granted
Glycosidase inhibitors and uses thereof
AssigneesAlectos Therapeutics Inc., Merck Sharp & Dohme Corp.
InventorsErnest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
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Abstract
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.
Claims6
A compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein
- R1 is selected from the group consisting of:
- CH2NR8R9, wherein R8 is H and R9 is C1-6 acyl, and (CH2)nC(O)NR102, wherein n is 1, and one R10 is H and the other R10 is C1-6 alkyl;
- R2 is H and R3 is OH, or R2 is H and R3 is H, or R2 is H and R3 is F, or R2 is F and R3 is H, or R2 is F and R3 is F, or R2 is OH and R3 is H;
- R4 is H and R5 is OH, or R4 is H and R5 is H, or R4 is H and R5 is F, or R4 is F and R5 is H, or R4 is F and R5 is F, or R4 is OH and R5 is H;
- R6 is selected from the group consisting of:
- CH3, CH2F, and CHF2;
- and
- R7 is selected from the group consisting of:
- C1-18 alkyl, C2-10 alkenyl, C2-10 alkynyl, C7-20 arylalkyl, C8-20 arylalkenyl, and C8-20 arylalkynyl, each 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,
- with the proviso that the compound excludes N-(((2R,3R,4R,5R)-3,4-dihydroxy-5-methylpyrrolidin-2-yl)methyl)acetamide.
8 more elements
Dependencies are inferred from the claim text.