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公开(公告)号：US20140018309A1
公开(公告)日：2014-01-16
申请号：US13997484
申请日：2011-12-21
申请人： Ramesh Kaul , Ernest J. Mceachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
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： 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.
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：US09701693B2
公开(公告)日：2017-07-11
申请号：US14129169
申请日：2012-06-27
申请人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
发明人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
IPC分类号： C07D513/00 , C07D513/04 , C07H9/06 , C12Q1/37 , C12Q1/34
CPC分类号： C07D513/04 , C07H9/06 , C12Q1/34 , C12Q1/37 , G01N2333/924 , G01N2500/04
摘要： The invention provides compounds 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：US20140296205A1
公开(公告)日：2014-10-02
申请号：US14129177
申请日：2012-06-27
申请人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
发明人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
IPC分类号： C07D513/04 , G01N33/50 , C12Q1/34
CPC分类号： C07D513/04 , C07H9/06 , C12Q1/34 , C12Q1/37 , G01N33/5038 , G01N2333/924 , G01N2500/04
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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公开(公告)号：US09120781B2
公开(公告)日：2015-09-01
申请号：US13697179
申请日：2011-05-10
申请人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Kun Liu , Harold G. Selnick
发明人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Kun Liu , Harold G. Selnick
IPC分类号： C07D263/56 , C07D263/58 , C07D277/82 , C07D413/04 , C07D417/04 , C07D277/64 , C07D263/52 , C07D277/60
CPC分类号： C07D417/04 , C07D263/52 , C07D263/56 , C07D263/58 , C07D277/60 , C07D277/64 , C07D277/82 , C07D413/04
摘要： The invention provides compounds of Formula (I) 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化合物（I）的化合物，以及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：US20140275022A1
公开(公告)日：2014-09-18
申请号：US14129169
申请日：2012-06-27
申请人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
发明人： Tong-Shuang Li , Ernest J. Mceachern , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold G. Selnick
IPC分类号： C07D513/04 , C12Q1/34
CPC分类号： C07D513/04 , C07H9/06 , C12Q1/34 , C12Q1/37 , G01N2333/924 , G01N2500/04
摘要： The invention provides compounds 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：US20130131044A1
公开(公告)日：2013-05-23
申请号：US13697179
申请日：2011-05-10
IPC分类号： C07D417/04 , C07D277/60 , C07D413/04 , C07D263/52
CPC分类号： C07D417/04 , C07D263/52 , C07D263/56 , C07D263/58 , C07D277/60 , C07D277/64 , C07D277/82 , C07D413/04
摘要： The invention provides compounds of Formula (I) 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化合物（I）的化合物，以及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：US20100298366A1
公开(公告)日：2010-11-25
申请号：US12851495
申请日：2010-08-05
申请人： Yuanxi ZHOU , Elyse Bourque , Yongbao Zhu , Jonathan Langille , Markus Metz , Wen Yang , Ernest J. Mceachern , Curtis Harwig , Ian R. Baird , Tong-Shuang Li , Renato T. Skerlj
发明人： Yuanxi ZHOU , Elyse Bourque , Yongbao Zhu , Jonathan Langille , Markus Metz , Wen Yang , Ernest J. Mceachern , Curtis Harwig , Ian R. Baird , Tong-Shuang Li , Renato T. Skerlj
IPC分类号： A61K31/4545 , C07D413/14 , C07D413/04 , C07D401/14 , A61K31/454 , A61K31/506 , A61P31/18
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
摘要翻译： 本发明涉及趋化因子受体结合化合物，药物组合物及其用途。 更具体地，本发明涉及趋化因子受体活性的调节剂，优选CCR5的调节剂。 这些化合物表现出对人体免疫缺陷病毒（HIV）感染靶细胞的保护作用。
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公开(公告)号：US06864265B2
公开(公告)日：2005-03-08
申请号：US09957682
申请日：2001-09-17
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis , Rosaria Maria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis , Rosaria Maria Di Fluri
IPC分类号： C07D491/052 , A61K31/44 , A61K31/4402 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , A61P31/18 , A61P43/00 , C07D213/38 , C07D213/65 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04 , A61K31/4436 , C07D471/00
CPC分类号： C07D401/14 , C07D213/38 , C07D213/65 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04
摘要： Compounds that bind to chemokine receptors such as CXCR4 and CCR5 demonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an aromatic or heteroaromatic moiety.
摘要翻译： 结合趋化因子受体如CXCR4和CCR5的化合物显示出针对人免疫缺陷病毒感染细胞的保护作用。 这些化合物含有通过芳族或杂芳族部分与核心氮连接的叔胺[[s]]。
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公开(公告)号：US20100105915A1
公开(公告)日：2010-04-29
申请号：US12612488
申请日：2009-11-04
申请人： Gary J. BRIDGER , Renato Skerlj , Ai Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
发明人： Gary J. BRIDGER , Renato Skerlj , Ai Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
IPC分类号： C07D401/02
CPC分类号： C07D239/42 , A61K45/06 , C07D213/38 , C07D215/40 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D487/04
摘要： Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.
摘要翻译： 公开了结合趋化因子受体并抑制其天然配体结合的杂环化合物。 本发明化合物可防止HIV感染并发挥拮抗剂对CXCR4受体特征的作用。
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10.发明申请公开(公告)号：US20080167341A1
公开(公告)日：2008-07-10
申请号：US12036187
申请日：2008-02-22
申请人： Gary BRIDGER , Renato T. Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason B. Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria R. Di Fluri
发明人： Gary BRIDGER , Renato T. Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason B. Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria R. Di Fluri
IPC分类号： A61K31/4709 , A61P7/00
CPC分类号： A61K31/4184 , A61K31/415 , A61K31/436 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/497 , A61K31/4985 , A61K31/50 , A61K31/502 , A61K31/506 , A61K31/5377 , C07D235/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D471/06 , C07D491/04 , C07D491/052 , Y02A50/411
摘要： The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
摘要翻译： 本发明涉及由三个侧基包围的核心氮原子组成的杂环化合物，其中三个侧基中的两个优选为苯并咪唑基甲基和四氢喹啉基，第三侧基含有N并且任选地含有另外的环。 这些化合物与趋化因子受体结合，包括CXCR4和CCR5，并表现出针对人类免疫缺陷病毒（HIV）感染靶细胞的保护作用。
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