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公开(公告)号：US09938299B2
公开(公告)日：2018-04-10
申请号：US14655222
申请日：2013-12-20
发明人： Harold G. Selnick , Kun Liu , Ernest J. McEachern , Ramesh Kaul , Zhongyong Wei , Yaode Wang , Jiang Chang
IPC分类号： C07D513/04 , B65D71/14 , B65D71/16 , B65D5/00 , B65D5/20
CPC分类号： C07D513/04 , B65D5/005 , B65D5/2057 , B65D71/14 , B65D71/16 , B65D2571/0016 , B65D2571/0029 , B65D2571/0066 , B65D2571/00716
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.
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公开(公告)号：US09815861B2
公开(公告)日：2017-11-14
申请号：US14966221
申请日：2015-12-11
发明人： Ramesh Kaul , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC分类号： C07H9/06 , C07H9/00 , C07D513/04 , C12Q1/34 , C07H17/00
CPC分类号： C07H9/06 , C07D513/04 , C07H9/00 , C07H17/00 , C12Q1/34 , G01N2333/924 , G01N2500/04 , G01N2500/20
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.
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公开(公告)号：US09611275B2
公开(公告)日：2017-04-04
申请号：US14399146
申请日：2013-05-03
发明人： Harold G. Selnick , Wenping Li , Eric Hostetler , Kun Liu , Ernest J. McEachern , Yuanxi Zhou , Zhongyong Wei , Changwei Mu , Yaode Wang , Jiang Chang
IPC分类号： C07D513/04 , C07B59/00 , C07H9/06
CPC分类号： C07D513/04 , C07B59/005 , C07B2200/05 , C07H9/06
摘要： The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
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公开(公告)号：US20150152127A1
公开(公告)日：2015-06-04
申请号：US14399146
申请日：2013-05-03
发明人： Harold G. Selnick , Wenping Li , Eric Hostetler , Kun Liu , Ernest J. McEachern , Yuanxi Zhou , Zhongyong Wei , Changwei Mu , Yaode Wang , Jiang Chang
CPC分类号： C07D513/04 , C07B59/005 , C07B2200/05 , C07H9/06
摘要： The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
摘要翻译： 本发明涉及包含这些化合物的化合物和药物制剂，其可用作O-连接的N-乙酰氨基葡糖苷酶（O-GlcNAcase）抑制剂，因此可用于治疗某些疾病，例如阿尔茨海默病，包括减少NFTs和/ 或超磷酸化tau。 本发明还涉及将化合物用作O-GlcNAcase显像剂。
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公开(公告)号：US20140243309A1
公开(公告)日：2014-08-28
申请号：US14345976
申请日：2012-09-21
发明人： Jason Brubaker , Christopher Dinsmore , Dawn Marie Hoffman , Joon Jung , Duan Liu , Scott Peterson , Tony Siu , Luis E. Torres , Hongjun Zhang , Zhongyong Wei , Feng Shi
IPC分类号： C07D231/38 , C07D403/08 , C07D403/12 , C07D405/08 , C07D401/12
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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