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公开(公告)号：US09243020B2
公开(公告)日：2016-01-26
申请号：US13997484
申请日：2011-12-21
申请人： Ramesh Kaul , Ernest J. McEachern , Harold G. Selnick , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu
发明人： Ramesh Kaul , Ernest J. McEachern , Harold G. Selnick , David J. Vocadlo , Yuanxi Zhou , Yongbao Zhu
IPC分类号： C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C07H17/00 , C07D513/04 , C07H9/06 , 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.
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：US20090298883A1
公开(公告)日：2009-12-03
申请号：US12420793
申请日：2009-04-08
申请人： Hassan PAJOUHESH , Ramesh KAUL , Yanbing DING , Yongbao ZHU , Lingyun ZHANG , Nagasree CHAKKA , Mike GRIMWOOD , Jason TAN , Yuanxi ZHOU
发明人： Hassan PAJOUHESH , Ramesh KAUL , Yanbing DING , Yongbao ZHU , Lingyun ZHANG , Nagasree CHAKKA , Mike GRIMWOOD , Jason TAN , Yuanxi ZHOU
IPC分类号： A61K31/454 , A61K31/445 , A61P9/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/30 , A61P25/00 , A61P3/10 , A61P29/00 , A61P35/00 , A61P13/10 , A61P13/12 , A61P15/16
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：US20080280900A1
公开(公告)日：2008-11-13
申请号：US12118492
申请日：2008-05-09
申请人： Hassan PAJOUHESH , Hossein PAJOUHESH , Yanbing DING , Jason TAN , Mike GRIMWOOD , Francesco BELARDETTI , Ramesh KAUL
发明人： Hassan PAJOUHESH , Hossein PAJOUHESH , Yanbing DING , Jason TAN , Mike GRIMWOOD , Francesco BELARDETTI , Ramesh KAUL
IPC分类号： A61K31/5377 , A61K31/496 , A61P35/00
CPC分类号： A61K31/496 , A61K31/5377
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 thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
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。 具体地说，通式（1）或式（2）公开了一系列含有噻吩并嘧啶或氧代喹唑啉衍生物的化合物，其中X为连接基，Y为芳族部分或N（R5）（R6）。
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公开(公告)号：US08377968B2
公开(公告)日：2013-02-19
申请号：US12420793
申请日：2009-04-08
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
IPC分类号： A61K31/454 , A61K31/445 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/30 , A61P25/00 , A61P3/10 , A61P29/00 , A61P35/00 , A61P13/10 , A61P13/12 , A61P15/16
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).
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公开(公告)号：US08133998B2
公开(公告)日：2012-03-13
申请号：US12118492
申请日：2008-05-09
申请人： Hassan Pajouhesh , Hossein Pajouhesh , Yanbing Ding , Jason Tan , Mike Grimwood , Francesco Belardetti , Ramesh Kaul , Richard Holland , Navjot Chahal
发明人： Hassan Pajouhesh , Hossein Pajouhesh , Yanbing Ding , Jason Tan , Mike Grimwood , Francesco Belardetti , Ramesh Kaul , Richard Holland , Navjot Chahal
IPC分类号： C07D491/00 , C07D333/00 , C07D333/52 , C07D333/38
CPC分类号： A61K31/496 , A61K31/5377
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 thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
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。 具体地说，通式（1）或式（2）公开了一系列含有噻吩并嘧啶或氧代喹唑啉衍生物的化合物，其中X为连接基，Y为芳族部分或N（R5）（R6）。
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公开(公告)号：US20100105682A1
公开(公告)日：2010-04-29
申请号：US12445256
申请日：2007-10-12
申请人： Hassan Pajouhesh , Hossein Pajouhesh , Ramesh Kaul
发明人： Hassan Pajouhesh , Hossein Pajouhesh , Ramesh Kaul
IPC分类号： A61K31/496 , A61P43/00 , A61K31/5377 , A61K31/4965 , A61P25/00 , A61P1/00 , A61P3/00 , A61P9/00 , A61P3/10 , A61P35/00 , A61P25/16 , C07D413/14 , C07D295/155 , C07D413/06 , C07D401/12
CPC分类号： A61K31/495 , A61K31/496 , A61K31/5377 , C07D207/09 , C07D211/16 , C07D211/58 , C07D213/75 , C07D241/04 , C07D295/185
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X1 and X2 are linkers.
摘要翻译： 公开了有效改善由不需要的钙通道活性，特别是不需要的N型钙通道活性表征的病症的方法和化合物。 具体地，公开了一系列含有哌嗪环和环丙基环的化合物，通式（I）其中X1和X2是连接基。
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公开(公告)号：US20090221603A1
公开(公告)日：2009-09-03
申请号：US12097035
申请日：2006-12-19
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Gabriel Hum , Hossein Pajouhesh
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Gabriel Hum , Hossein Pajouhesh
IPC分类号： A61K31/496 , A61K31/495 , C07D241/04 , C07D401/06 , A61P25/00
CPC分类号： C07D211/26 , A61K31/495 , A61K31/496 , C07D211/62 , C07D211/64 , C07D213/74 , C07D241/04 , C07D295/185 , C07D309/04
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of heterocyclic amides are disclosed of the general formula (1) where Z is N or ═CHNR2 and X is NR2, O, S, S═O or SO2. Among other definitions for R, R1, W and Y, the compounds of formula (1) are further characterized by at least one of W or Y being CR3Ar2 where Ar is an aromatic or heteroaromatic ring (for example, where W or Y is a benzhydryl moiety).
摘要翻译： 公开了有效改善由不需要的钙通道活性，特别是不想要的N型或T型钙通道活性表征的病症的方法和化合物。 具体地，公开了通式（1）的一系列杂环酰胺，其中Z是N或-CHNR 2，X是NR 2，O，S，S-O或SO 2。 对于R，R 1，W和Y的其它定义，式（1）化合物的进一步特征在于W或Y中的至少一个是CR 3 Ar 2，其中Ar是芳族或杂芳族环（例如，其中W或Y是 二苯甲基部分）。
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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：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：US08569344B2
公开(公告)日：2013-10-29
申请号：US13601357
申请日：2012-08-31
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
IPC分类号： A61K31/445 , A61P29/00
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).
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