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1.发明申请BISARYLSULFONE AND DIALKYLARYLSULFONE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS 审中-公开作为钙通道阻滞剂的双联砜和二烷基磺酸盐化合物公开(公告)号：US20140113898A1
公开(公告)日：2014-04-24
申请号：US13883956
申请日：2011-11-04
申请人： Hassan A. Pajouhesh , Richard Holland , Yuanxi Zhou , Yongbao Zhu , Michael Edward Grimwood , Navjot Chahal
发明人： Hassan A. Pajouhesh , Richard Holland , Yuanxi Zhou , Yongbao Zhu , Michael Edward Grimwood , Navjot Chahal
IPC分类号： C07D487/04 , C07D213/82 , C07D295/26 , C07D239/28 , C07D471/04 , C07C317/32 , C07D231/14
CPC分类号： C07D487/04 , C07C317/28 , C07C317/32 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07D207/16 , C07D209/30 , C07D211/60 , C07D213/62 , C07D213/71 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/14 , C07D239/28 , C07D239/36 , C07D295/073 , C07D295/195 , C07D295/26 , C07D309/08 , C07D317/60 , C07D335/02 , C07D471/04
摘要： The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
摘要翻译： 本发明涉及可用于治疗与钙通道功能相关的病症的二芳基砜和二烷基芳基砜化合物（例如，表4和5的式（I） - （IX）或化合物（1） - （227）中任一项的化合物） 特别是与N型钙通道活性相关的病症。 本发明还涉及包含这些二芳基砜化合物的药物组合物，以及用于治疗诸如心血管疾病，癫痫，癌症和疼痛的病症的方法。
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2.发明申请公开(公告)号：US20120245137A1
公开(公告)日：2012-09-27
申请号：US13496729
申请日：2010-09-17
申请人： Hassan A. Pajouhesh , Robert Galemmo, JR. , Richard Holland , Yuanxi Zhou , Yongbao Zhu , Eric Simonson , Navjot Chahal , Mike Grimwood
发明人： Hassan A. Pajouhesh , Robert Galemmo, JR. , Richard Holland , Yuanxi Zhou , Yongbao Zhu , Eric Simonson , Navjot Chahal , Mike Grimwood
IPC分类号： A61K31/44 , C07D239/26 , A61K31/505 , C07C317/48 , A61K31/166 , C07D295/13 , A61K31/5375 , C07D205/04 , A61K31/397 , C07D265/36 , A61K31/538 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/18 , A61P25/06 , C07D213/82
CPC分类号： C07C317/44 , A61K31/095 , C07C317/14 , C07C317/22 , C07C317/28 , C07C317/30 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I).
摘要翻译： 公开了有效改善由不希望的钙通道活性，特别是不需要的N型和/或T型钙通道活性表征的病症的方法和化合物。 具体而言，是一系列含有芳基砜衍生物的化合物，如式（I）所例举。
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公开(公告)号：US20140011996A1
公开(公告)日：2014-01-09
申请号：US14013934
申请日：2013-08-29
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , MIchael Edward Grimwood , Jason Tan , Yuanxi Zhou
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , MIchael Edward Grimwood , Jason Tan , Yuanxi Zhou
IPC分类号： C07D211/28 , C07D401/06 , C07D211/62 , C07D409/12 , C07D405/06 , C07D413/12 , C07D211/26 , C07D401/12 , C07D211/66 , C07D405/14 , C07D211/46 , C07D211/38 , C07D405/12 , C07D417/12
CPC分类号： A61K31/5377 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , C07D211/26 , C07D211/28 , C07D211/38 , C07D211/46 , C07D211/62 , C07D211/66 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
摘要翻译： 公开了有助于改善由不希望的钙通道活性，特别是不希望的T型钙通道活性表征的病症的方法和化合物。 具体而言，是一系列含有式（1）所示的N-哌啶基乙酰胺衍生物的化合物。
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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：US07790747B2
公开(公告)日：2010-09-07
申请号：US11453221
申请日：2006-06-14
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 , C07D409/14
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：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：US09126957B2
公开(公告)日：2015-09-08
申请号：US14238481
申请日：2012-08-10
申请人： Harold G. Selnick , Kun Liu , Ernest J. McEachern , Yuanxi Zhou , Yongbao Zhu
发明人： Harold G. Selnick , Kun Liu , Ernest J. McEachern , Yuanxi Zhou , Yongbao Zhu
IPC分类号： A61K31/423 , A61K31/428 , C07D263/58 , C07D413/04 , C07D417/04 , C07D277/60 , C07D277/82
CPC分类号： C07D263/58 , A61K31/423 , A61K31/428 , C07D277/60 , C07D277/82 , C07D413/04 , C07D417/04
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，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。
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公开(公告)号：US08901087B2
公开(公告)日：2014-12-02
申请号：US13883811
申请日：2011-11-08
申请人： Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
发明人： Jiang Chang , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , Feng Shi , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou , Yongbao Zhu
IPC分类号： C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C07D513/04
CPC分类号： C07D513/04
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，化合物的用途和包含该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过度表达有关的疾病和障碍和/或O-GlcNAc的积累或缺陷的方法。
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公开(公告)号：US09409924B2
公开(公告)日：2016-08-09
申请号：US14129177
申请日：2012-06-27
申请人： Tong-Shuang Li , Ernest McEachern , David Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold Selnick
发明人： Tong-Shuang Li , Ernest McEachern , David Vocadlo , Yuanxi Zhou , Yongbao Zhu , Harold Selnick
IPC分类号： C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/34 , C12Q1/48 , C12Q1/37 , G01N33/50
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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