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公开(公告)号：US09695197B2
公开(公告)日：2017-07-04
申请号：US14439790
申请日：2013-10-30
发明人： Ramesh Kaul , Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Qun Dang , Harold G. Selnick
IPC分类号： C07D498/04 , C07D513/04 , C07H9/06
CPC分类号： C07D513/04 , C07D498/04 , C07H9/06
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：US20150218147A1
公开(公告)日：2015-08-06
申请号：US14424615
申请日：2013-08-29
IPC分类号： C07D417/06 , C07D401/08 , C07D207/14
CPC分类号： C07D417/06 , C07D207/14 , C07D401/06 , C07D401/08
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.
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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：US09522883B2
公开(公告)日：2016-12-20
申请号：US14424602
申请日：2013-08-29
IPC分类号： C07D211/56 , A61K31/445 , A61K31/4523 , C07D401/06 , C07D417/06
CPC分类号： C07D211/56 , A61K31/445 , A61K31/4523 , C07D401/06 , C07D417/06
摘要： The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D-glucopyranoside (O-GlcNAc).
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公开(公告)号：US09809537B2
公开(公告)日：2017-11-07
申请号：US14424873
申请日：2013-08-29
发明人： Ernest J. McEachern , Jianyu Sun , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
IPC分类号： C07D207/12 , A61K31/40 , A61K31/428 , A61K31/4439 , C07D401/06 , C07D417/06 , C12N9/99 , C07D207/16
CPC分类号： C07D207/12 , A61K31/40 , A61K31/428 , A61K31/4439 , C07D207/16 , C07D401/06 , C07D417/06 , C12N9/99 , C12Y302/01169
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.
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公开(公告)号：US09670195B2
公开(公告)日：2017-06-06
申请号：US14424615
申请日：2013-08-29
IPC分类号： C07D207/14 , C07D417/06 , C07D401/06 , C07D401/08
CPC分类号： C07D417/06 , C07D207/14 , C07D401/06 , C07D401/08
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.
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公开(公告)号：US20150291620A1
公开(公告)日：2015-10-15
申请号：US14439790
申请日：2013-10-30
发明人： Ramesh Kaul , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Qun Dang , Harold G. Selnick
IPC分类号： C07D513/04 , C07D498/04
CPC分类号： C07D513/04 , C07D498/04 , C07H9/06
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.
摘要翻译： 本发明提供了具有增强的选择性抑制糖苷酶的通透性的化合物，化合物的前药以及包含化合物的化合物或前药的药物组合物。 本发明还提供了治疗与O-GlcNAcase的缺乏或过度表达相关的疾病和障碍的方法，O-GlcNAc的积累或缺乏。
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公开(公告)号：US20150274656A1
公开(公告)日：2015-10-01
申请号：US14424873
申请日：2013-08-29
发明人： Ernest J. McEachern , Jianyu Sun , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
IPC分类号： C07D207/12 , C07D207/16 , C07D417/06 , C07D401/06
CPC分类号： C07D207/12 , A61K31/40 , A61K31/428 , A61K31/4439 , C07D207/16 , C07D401/06 , C07D417/06 , C12N9/99 , C12Y302/01169
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.
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公开(公告)号：US20150218097A1
公开(公告)日：2015-08-06
申请号：US14424602
申请日：2013-08-29
IPC分类号： C07D211/56 , C07D417/06 , C07D401/06
CPC分类号： C07D211/56 , A61K31/445 , A61K31/4523 , C07D401/06 , C07D417/06
摘要： The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D-glucopyranoside (O-GlcNAc).
摘要翻译： 本发明提供式（I）化合物，其用于抑制gh辅酶，化合物的前药和包含化合物的化合物或前药的药物组合物。 本发明还提供了治疗与O-gh蛋白2-乙酰氨基-2-脱氧-α-D-葡萄糖吡喃糖苷酶（O-GlcNAcase）的缺乏或过度表达相关的疾病和病症的方法，2-乙酰氨基 - 2-脱氧-β-D-吡喃葡萄糖苷（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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