发明名称 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.
申请公布号 US8927507(B2) 申请公布日期 2015.01.06
申请号 US201214006888 申请日期 2012.03.16
申请人 发明人 McEachern Ernest J.;Vocadlo David J.;Zhou Yuanxi;Coburn Craig A.;Liu Kun;Selnick Harold G.
分类号 C08B37/00;C07D487/02;A61K31/70;A61K31/425;C12Q1/34;C07H13/04;C07H9/06 主分类号 C08B37/00
代理机构 Clark & Elbing LLP 代理人 Clark & Elbing LLP
主权项 1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein each R1 is independently H or C1-6 acyl; R2 is H, CH3, or CH2CH3; and when R2 is H, R3 is selected from the group consisting of: C1-6 acyl, arylacyl, CH2C≡CH, (CH2)3F, (CH2)3OH, (CH2)2CF3, (CH2)CH(CH3)2, CH(CH3)(CH2CH3), CH(CH3)(CH2OCH3), CH2(cyclopropyl), (CH2)2(cyclopropyl), cyclobutyl, cyclopentyl, tetrahydrothiophen-3-yl, 1-methyl-1H-pyrazol-3-yl, C(O)OCH3, C(O)O(phenyl), C(O)O(benzyl), and C(O)NH(CH2CH3), said C1-6 acyl optionally substituted with 1 substituent selected from CH3 and phenyl; and when R2 is CH3, R3 is selected from the group consisting of: (CH2)2CH3, CH2CH═CH2, and OCH3; and when R2 is CH2CH3, R3 is CH2CH3.
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