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公开(公告)号：EP2655388B1
公开(公告)日：2016-06-08
申请号：EP11850773.0
申请日：2011-12-21
发明人： KAUL, Ramesh , MCEACHERN, Ernest J. , MU, Changwei , SELNICK, Harold G. , VOCADLO, David J. , WANG, Yaode , WEI, Zhongyong , ZHOU, Yuanxi , ZHU, Yongbao
IPC分类号： C07H9/06 , A61K31/7056 , C07D513/04 , C12Q1/34
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：EP2691407A1
公开(公告)日：2014-02-05
申请号：EP12765063.8
申请日：2012-03-20
发明人： KAUL, Ramesh , MCEACHERN, Ernest J. , VOCADLO, David J. , ZHOU, Yuanxi , LIU, Kun , SELNICK, Harold G. , WEI, Zhongyong , MU, Changwei , WANG, Yaode , WANG, Xiaona
IPC分类号： C07H15/12 , A61K31/7056 , C07H11/00 , C07H13/00 , C07H13/12 , C07H15/18 , C07H17/07 , C07H19/04 , C07H9/06 , C12N9/24 , C12Q1/34
CPC分类号： C07H19/24 , A61K31/7056 , C07D513/04 , C07H9/06 , C07H11/00 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/203 , C07H15/207 , C07H17/02 , C07H17/04 , C12N9/99 , C12Q1/34 , C12Y302/01169
摘要： The invention provides compounds of formula (I) with substituents as specified in Claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
摘要翻译： 本发明提供了具有权利要求1中指定的取代基的式（I）化合物用于选择性抑制糖苷酶，所述化合物的前药和包含所述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的过度表达或O-GlcNac的积累有关的疾病和病症的方法。
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公开(公告)号：EP2655388A1
公开(公告)日：2013-10-30
申请号：EP11850773.0
申请日：2011-12-21
发明人： KAUL, Ramesh , McEACHERN, Ernest J. , MU, Changwei , SELNICK, Harold G. , VOCADLO, David J. , WANG, Yaode , WEI, Zhongyong , ZHOU, Yuanxi , ZHU, Yongbao
IPC分类号： C07H9/06 , A61K31/7056 , C07D513/04 , C12Q1/34
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：EP2935283A1
公开(公告)日：2015-10-28
申请号：EP13868947.6
申请日：2013-12-20
发明人： SELNICK, Harold, G. , LIU, Kun , MCEACHERN, Ernest, J. , KAUL, Ramesh , WEI, Zhongyong , WANG, Yaode , CHANG, Jiang
IPC分类号： C07D513/04 , A61P11/02
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.
摘要翻译： 本发明提供了用于选择性抑制糖苷酶的通透性增强的化合物，所述化合物的前药和包含所述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的缺乏或过表达，O-GlcNAc的积累或缺乏有关的疾病和病症的方法。
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公开(公告)号：EP2847199A1
公开(公告)日：2015-03-18
申请号：EP13787989.6
申请日：2013-05-03
发明人： SELNICK, Harold, G. , LI, Wenping , HOSTETLER, Eric , LIU, Kun , MCEACHERN, Ernest, J. , ZHOU, Yuanxi , WEI, Zhongyong , MU, Changwei , WANG, Yaode , CHANG, Jiang
IPC分类号： C07D513/04
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-联N-乙酰氨基葡糖苷酶（O-GlcNAcase）抑制剂，并因此可用于治疗某些病症如阿尔茨海默氏病，包括减少NFT和/ 或超磷酸化的tau。 本发明还涉及这些化合物作为O-GlcNAcase成像剂的用途。
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公开(公告)号：EP2935283B1
公开(公告)日：2019-02-27
申请号：EP13868947.6
申请日：2013-12-20
发明人： SELNICK, Harold, G. , LIU, Kun , MCEACHERN, Ernest, J. , KAUL, Ramesh , WEI, Zhongyong , WANG, Yaode , CHANG, Jiang
IPC分类号： C07D513/04 , A61P11/02 , A61K31/429
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公开(公告)号：EP2847199B1
公开(公告)日：2017-10-25
申请号：EP13787989.6
申请日：2013-05-03
发明人： SELNICK, Harold, G. , LI, Wenping , HOSTETLER, Eric , LIU, Kun , MCEACHERN, Ernest, J. , ZHOU, Yuanxi , WEI, Zhongyong , MU, Changwei , WANG, Yaode , CHANG, Jiang
IPC分类号： C07D513/04 , C07H9/06 , A61K31/429 , A61P25/00
CPC分类号： C07D513/04 , C07B59/005 , C07B2200/05 , C07H9/06
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公开(公告)号：EP2691407B1
公开(公告)日：2017-02-22
申请号：EP12765063.8
申请日：2012-03-20
发明人： KAUL, Ramesh , MCEACHERN, Ernest J. , VOCADLO, David J. , ZHOU, Yuanxi , LIU, Kun , SELNICK, Harold G. , WEI, Zhongyong , MU, Changwei , WANG, Yaode , WANG, Xiaona
IPC分类号： C07H15/12 , A61K31/7056 , C07H11/00 , C07H13/00 , C07H13/12 , C07H15/18 , C07H17/07 , C07H19/04 , C07H9/06 , C12N9/24 , C12Q1/34
CPC分类号： C07H19/24 , A61K31/7056 , C07D513/04 , C07H9/06 , C07H11/00 , C07H13/12 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/203 , C07H15/207 , C07H17/02 , C07H17/04 , C12N9/99 , C12Q1/34 , C12Y302/01169
摘要： The invention provides compounds of formula (I) with substituents as specified in Claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
摘要翻译： 本发明提供了具有权利要求1所述取代基的式（I）化合物用于选择性抑制糖苷酶，所述化合物的前药和包含所述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的过度表达或O-GlcNac的积累有关的疾病和病症的方法。
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公开(公告)号：EP2637503B1
公开(公告)日：2016-09-14
申请号：EP11840448.2
申请日：2011-11-08
发明人： CHANG, Jiang , MCEACHERN, Ernest, J. , MU, Changwei , SHI, Feng , VOCADLO, David, J. , WANG, Yaode , WEI, Zhongyong , ZHOU, Yuanxi , ZHU, Yongbao
IPC分类号： C07H9/06 , C07D513/04 , A61K31/7056
CPC分类号： C07D513/04 , C07H9/06
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公开(公告)号：EP2637503A1
公开(公告)日：2013-09-18
申请号：EP11840448.2
申请日：2011-11-08
发明人： CHANG, Jiang , MCEACHERN, Ernest, J. , MU, Changwei , SHI, Feng , VOCADLO, David, J. , WANG, Yaode , WEI, Zhongyong , ZHOU, Yuanxi , ZHU, Yongbao
IPC分类号： A01N43/78 , A61K31/425
CPC分类号： C07D513/04 , C07H9/06
摘要： The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
摘要翻译： 本发明涉及用于选择性抑制糖苷酶的化合物，所述化合物和包含所述化合物的药物组合物的用途，以及治疗与O-GlcNAcase的缺陷或过表达和/或O-GlcNAc的积累或缺乏有关的疾病和病症的方法。
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