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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：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：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：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：US10913733B2
公开(公告)日：2021-02-09
申请号：US16061988
申请日：2016-12-14
IPC分类号： A61K31/454 , C07D417/06 , C07D417/14 , C07D409/06
摘要： The present invention is directed to thiazolyl piperidine compounds of the general structural formula I: which are inhibitors of O-GlcNAcase. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which O-GlcNAcase is involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which O-GlcNAcase is involved.
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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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