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公开(公告)号：US09199949B2
公开(公告)日：2015-12-01
申请号：US14129163
申请日：2012-06-27
IPC分类号： C07D263/58 , C07D413/04 , C07D417/04 , C07D277/60 , A61K31/423 , A61K31/428 , C07D277/82 , C12Q1/37 , C07D263/52
CPC分类号： C07D277/60 , C07D263/52 , C07D263/58 , C07D277/82 , 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：US20150045346A1
公开(公告)日：2015-02-12
申请号：US14129163
申请日：2012-06-27
IPC分类号： C07D277/60 , C07D263/52
CPC分类号： C07D277/60 , C07D263/52 , C07D263/58 , C07D277/82 , 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.
摘要翻译： 本发明提供了用于选择性抑制糖苷酶，化合物前药和包含化合物的化合物或前药的药物组合物的化合物。 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：US20140206665A1
公开(公告)日：2014-07-24
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： C07D263/58 , C07D413/04 , C07D417/04 , C07D277/60
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，化合物的用途和包括该化合物的药物组合物，以及治疗与O-GlcNAC的缺乏或过量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：US20140107044A1
公开(公告)日：2014-04-17
申请号：US14006888
申请日：2012-03-16
申请人： Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Craig A. Coburn , Kun Liu , Harold G. Selnick
发明人： Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Craig A. Coburn , Kun Liu , Harold G. Selnick
CPC分类号： C07H9/06 , C07H13/04 , C12Q1/34 , 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.
摘要翻译： 本发明提供了用于选择性抑制糖苷酶，化合物前药和包含化合物的化合物或前药的药物组合物的化合物。 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：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：US20120121508A1
公开(公告)日：2012-05-17
申请号：US13386955
申请日：2010-07-20
申请人： Ian M. Bell , Eric Hostetler , Harold G. Selnick , Craig A. Stump
发明人： Ian M. Bell , Eric Hostetler , Harold G. Selnick , Craig A. Stump
IPC分类号： A61K51/04 , A61P25/00 , C07D471/10
CPC分类号： C07D471/10 , C07B59/002 , C07D471/20
摘要： The present invention is directed to radiolabeled CGRP receptor antagonists which are useful for the quantitative imaging of CGRP receptors in mammals.
摘要翻译： 本发明涉及放射性标记的CGRP受体拮抗剂，其可用于哺乳动物中CGRP受体的定量成像。
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8.发明申请3- AND 6-QUINOLINES WITH N-ATTACHED HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS 有权具有N-连接的杂环CGRP受体拮抗剂的3-和6-喹啉公开(公告)号：US20110306604A1
公开(公告)日：2011-12-15
申请号：US13059164
申请日：2009-08-14
申请人： Michael R. Wood , Ian M. Bell , June J. Kim , Harold G. Selnick , Craig A. Stump
发明人： Michael R. Wood , Ian M. Bell , June J. Kim , Harold G. Selnick , Craig A. Stump
IPC分类号： A61K31/551 , A61K31/4545 , A61P25/00 , A61K31/437 , A61K31/496 , A61P25/06 , C07D471/20 , A61K31/499
CPC分类号： C07D471/20
摘要： Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
摘要翻译： 式（I）的化合物（其中变量R1A，R1B，R2，R3，R4，A和Z如本文所定义），其可用作CGRP受体的拮抗剂，并且可用于治疗或预防CGRP 涉及受体，例如头痛，特别是偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP受体的疾病中的用途。
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公开(公告)号：US20110021516A1
公开(公告)日：2011-01-27
申请号：US12934208
申请日：2009-03-24
申请人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
发明人： Harold G. Selnick , Ian M. Bell , Melody McWherter , Donnette D. Staas , Shawn J. Stachel , Thomas Steele , Craig Stump , Michael R. Wood , C. Blair Zartman
IPC分类号： A61K31/5365 , C07D471/04 , A61K31/496 , A61P25/06
CPC分类号： C07D471/10 , C07D403/06 , C07D471/20 , C07D519/00
摘要： The present invention is directed to compounds of the formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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10.发明授权Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease 有权苄醚和苄氨基β-分泌酶抑制剂用于治疗阿尔茨海默病公开(公告)号：US07829597B2
公开(公告)日：2010-11-09
申请号：US10573232
申请日：2004-09-29
IPC分类号： C07C15/12 , C07C13/48 , A61K31/135
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂的式（I）化合物，其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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