发明名称 Selective glycosidase inhibitors and uses thereof
摘要 The invention provides compounds with enhanced permeability 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 US9409924(B2) 申请公布日期 2016.08.09
申请号 US201214129177 申请日期 2012.06.27
申请人 Alectos Therapeutics Inc.;Merck Sharp & Dohme Corp. 发明人 Li Tong-Shuang;McEachern Ernest;Vocadlo David;Zhou Yuanxi;Zhu Yongbao;Selnick Harold
分类号 C07D513/04;C07H9/06;C07H13/04;C07H13/12;C07H15/18;C12Q1/34;C12Q1/48;C12Q1/37;G01N33/50 主分类号 C07D513/04
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 R1 and R2 are independently H or F; R3 is OR5 and R4 is H, or R3 is H and R4 is OR5; each R5 is independently H or C1-6 acyl; R6 is H, F, or OR5; R7 is selected from the group consisting of: H, F, C1-8 alkyl, C2-8 alkenyl, and C2-8 alkynyl, wherein the C1-8 alkyl, C2-8 alkenyl, or C2-8 alkynyl are optionally substituted from one up to the maximum number of substituents with one or both of fluoro or OH; R8 is selected from the group consisting of: C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-6 cycloalkyl, aryl and heteroaryl, optionally substituted from one up to the maximum number of substituents with fluoro or OH; each R9 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 R9 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, with the proviso that when R6 is OR5, R7 is other than F.
地址 Burnaby CA