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公开(公告)号：EP2847199A4
公开(公告)日：2015-11-11
申请号：EP13787989
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
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公开(公告)号：EP2637503A4
公开(公告)日：2014-04-09
申请号：EP11840448
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 , A61K31/7056 , C07D513/04
CPC分类号： C07D513/04 , C07H9/06
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3.发明公开SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF 有权SEREKTIVE GLYCOSIDASEHEMMER UND IHRE VERWENDUNG
公开(公告)号：EP2638052A4
公开(公告)日：2014-04-02
申请号：EP11839469
申请日：2011-11-08
发明人： COBURN CRAIG A , LIU KUN , MCEACHERN ERNEST J , MU CHANGWEI , SELNICK HAROLD G , VOCADLO DAVID J , WANG YAODE , WEI ZHONGYONG , ZHOU YUANXI
IPC分类号： C07H9/06 , A61K31/7052 , C07D513/04 , C07D513/14 , C07H13/02 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N33/50
CPC分类号： C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
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公开(公告)号：EP2935283A4
公开(公告)日：2016-10-05
申请号：EP13868947
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 , A61K31/429 , A61P11/02
CPC分类号： C07D513/04
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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5.发明公开SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF 有权SEREKTIVE GLYCOSIDASEHEMMER UND IHRE VERWENDUNG
公开(公告)号：EP2691407A4
公开(公告)日：2014-08-27
申请号：EP12765063
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 , C07H9/06 , C07H11/00 , C07H13/00 , C07H13/12 , C07H15/18 , C07H17/07 , C07H19/04 , 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： 本发明提供了具有如权利要求1中所定义的取代基的式（I）化合物，其用于选择性抑制糖苷酶，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：EP2655388A4
公开(公告)日：2014-06-18
申请号：EP11850773
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：EP3154970A4
公开(公告)日：2017-11-15
申请号：EP15806980
申请日：2015-06-09
申请人： MERCK SHARP & DOHME
发明人： WALJI ABBAS M , HOSTETLER ERIC , GRESHOCK THOMAS , LI JING , MOORE KEITH P , BENNACEF IDRISS , MULHEARN JAMES , SELNICK HAROLD , WANG YAODE , YANG KUN , FU JIANMIN
IPC分类号： C07D471/04
CPC分类号： A61K51/0455 , A61K51/0459 , C07B2200/05 , C07D471/04 , C07D519/00
摘要： or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
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