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公开(公告)号：US08518975B2
公开(公告)日：2013-08-27
申请号：US12673858
申请日：2008-09-04
申请人： Robert G. Aslanian , Xianhai Huang , Anandan Palani , Jun Qin , Wei Zhou , Xiaohong Zhu , Robert D. Mazzola, Jr. , Pawan Dhondi , William J. Greenlee
发明人： Robert G. Aslanian , Xianhai Huang , Anandan Palani , Jun Qin , Wei Zhou , Xiaohong Zhu , Robert D. Mazzola, Jr. , Pawan Dhondi , William J. Greenlee
IPC分类号： C07D403/12 , C07D401/12 , C07D237/14 , A61K31/501 , A61K31/50 , A61K31/4439
CPC分类号： C07D403/12 , C07D237/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/14
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式还公开了使用式（I）化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。
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公开(公告)号：US20110082153A1
公开(公告)日：2011-04-07
申请号：US12673858
申请日：2008-09-04
申请人： Robert G. Aslanian , Xianhai Huang , Anandan Palani , JUn Qin , Wei Zhou , Xiaohong Zhu , Robert Mazzola , Pawan Dhondi , William J. Greenlee
发明人： Robert G. Aslanian , Xianhai Huang , Anandan Palani , JUn Qin , Wei Zhou , Xiaohong Zhu , Robert Mazzola , Pawan Dhondi , William J. Greenlee
IPC分类号： A61K31/501 , C07D403/12 , C07D237/14 , A61K31/50 , C07D401/12 , A61K31/4439 , C07D403/14 , A61P25/28 , A61P27/06 , A61P9/00 , A61P29/00
CPC分类号： C07D403/12 , C07D237/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/14
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式（I）。 还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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3.发明申请公开(公告)号：US20110027264A1
公开(公告)日：2011-02-03
申请号：US12919574
申请日：2009-02-26
申请人： Xianhai Huang , Xianghai Huang , Anandan Palani , Robert G. Aslanian , Zhaoning Zhu , Dmitri A. Pissarnitski , Hongmei Li , William J. Greenlee , Zhiqiang Zhao , Robert D. Mazzola, JR. , Jun Qin , Pawan Dhondi
发明人： Xianhai Huang , Xianghai Huang , Anandan Palani , Robert G. Aslanian , Zhaoning Zhu , Dmitri A. Pissarnitski , Hongmei Li , William J. Greenlee , Zhiqiang Zhao , Robert D. Mazzola, JR. , Jun Qin , Pawan Dhondi
IPC分类号： A61K39/395 , C07D401/12 , C07D221/20 , A61K38/16 , A61K31/454 , A61K31/438 , A61P25/28
CPC分类号： C07D401/12 , C07D498/20
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有下式：还公开了使用式（I）化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。
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公开(公告)号：US08450343B2
公开(公告)日：2013-05-28
申请号：US12746041
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert G. Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhu , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
发明人： Xianhai Huang , Anandan Palani , Jun Qin , Robert G. Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhu , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , C07D403/10 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号：US08357682B2
公开(公告)日：2013-01-22
申请号：US12598704
申请日：2008-05-05
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, Jr. , John Clader , Hubert Josien , Jun Qin
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, Jr. , John Clader , Hubert Josien , Jun Qin
IPC分类号： C07D413/10 , C07D413/14 , C07D498/10 , A61K31/395 , A61K31/4245 , A61K31/4439
CPC分类号： C07D413/10 , C07D413/14 , C07D498/04 , C07D498/10 , C07D498/20
摘要： The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 本发明提供了一类新颖的式（I）杂环化合物作为γ-分泌酶的调节剂，其中式（I）变量的定义在本文中定义，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物 制备包含一种或多种此类化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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公开(公告)号：US20100247514A1
公开(公告)日：2010-09-30
申请号：US12598704
申请日：2008-05-05
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, JR. , John Clader , Hubert Josien , Jun Qin
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, JR. , John Clader , Hubert Josien , Jun Qin
IPC分类号： A61K39/395 , C07D413/10 , A61K31/4245 , C07D413/14 , A61K31/4439 , C07D498/10 , A61K31/438 , C07D498/04 , A61K31/437 , A61K31/5365 , A61P25/28 , A61P25/00 , A61K31/397 , A61P9/00
CPC分类号： C07D413/10 , C07D413/14 , C07D498/04 , C07D498/10 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法和方法 使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病。
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公开(公告)号：US08927559B2
公开(公告)日：2015-01-06
申请号：US13878654
申请日：2011-10-06
申请人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
发明人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要翻译： 本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态 受体。
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公开(公告)号：US08673900B2
公开(公告)日：2014-03-18
申请号：US13128493
申请日：2009-11-12
申请人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Jun Qin , Xiaoxiang Liu , Hongmei Li , Wei Zhou , Anandan Palani , Xiaohong Zhu , Monica L. Vicarel , Mihirbaran Mandal , Zhong-Yue Sun , Chad E. Bennett , Troy Michael McCracken , Gioconda V. Gallo
发明人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Jun Qin , Xiaoxiang Liu , Hongmei Li , Wei Zhou , Anandan Palani , Xiaohong Zhu , Monica L. Vicarel , Mihirbaran Mandal , Zhong-Yue Sun , Chad E. Bennett , Troy Michael McCracken , Gioconda V. Gallo
IPC分类号： C07D471/04 , C07D498/04 , A61K31/5395
CPC分类号： C07D471/04 , C07D498/04
摘要： In many embodiments, the present invention provides novel heterocyclic compounds which are modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在许多实施方案中，本发明提供了新的杂环化合物，其为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗方法， 使用这些化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。
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公开(公告)号：US20110053918A1
公开(公告)日：2011-03-03
申请号：US12665551
申请日：2008-06-27
申请人： Zhaoning Zhu , William J. Greenlee , Robert D. Mazzola, JR. , Jun Qin , Xianhai Huang , Anandan Palani
发明人： Zhaoning Zhu , William J. Greenlee , Robert D. Mazzola, JR. , Jun Qin , Xianhai Huang , Anandan Palani
IPC分类号： A61K31/541 , C07D239/70 , C07D239/24 , C07D233/56 , C07D403/12 , C07D401/10 , C07D279/02 , C07D413/10 , C07D265/36 , C07D241/36 , A61K31/4353 , A61K31/519 , A61K31/505 , A61K31/4166 , A61K31/4439 , A61K31/5355 , A61K31/538 , A61K31/497 , A61P25/28 , A61P9/10 , A61P25/00
CPC分类号： C07D487/04 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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公开(公告)号：US20130210805A1
公开(公告)日：2013-08-15
申请号：US13878654
申请日：2011-10-06
申请人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, JR. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Johny Biju , Li Dong , Xian Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi
发明人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, JR. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Johny Biju , Li Dong , Xian Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi
IPC分类号： C07D239/91 , A61K31/517 , A61K45/06 , C07D403/10 , C07D417/10 , C07D413/10 , C07D405/10 , C07D413/14 , C07D498/10 , C07D403/14 , A61K31/55 , C07D401/14 , A61K31/5395 , C07D471/04 , C07D401/10
CPC分类号： C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要翻译： 本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态 受体。
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