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公开(公告)号：US08580956B2
公开(公告)日：2013-11-12
申请号：US12600910
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
IPC分类号： C07D498/04 , C07D498/14 , A61K31/4245 , A61K31/5365 , A61K31/5383
CPC分类号： C07D498/04 , C07D413/10
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：US20120238546A1
公开(公告)日：2012-09-20
申请号：US13378080
申请日：2010-06-15
IPC分类号： A61K31/553 , A61P25/28 , A61K31/551 , C07D498/04 , C07D471/04
CPC分类号： C07D498/04 , C07D471/04 , C07D513/04
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）的化合物调节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：US20100256128A1
公开(公告)日：2010-10-07
申请号：US12601322
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
发明人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
IPC分类号： A61K31/5365 , C07D498/04 , A61K31/5395 , A61P25/28
CPC分类号： C07D498/04 , C07D403/10 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: 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下式杂环化合物：作为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这样的化合物的药物制剂的方法 化合物，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：US20120245158A1
公开(公告)日：2012-09-27
申请号：US13377885
申请日：2010-06-15
IPC分类号： A61K31/519 , A61K31/53 , A61P25/28 , C07D487/04 , C07D498/04 , A61K31/5395
CPC分类号： C07D471/04 , C07D498/04
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-分泌酶活性的方法和治疗阿尔茨海默病的方法。
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公开(公告)号：US20130303517A1
公开(公告)日：2013-11-14
申请号：US13996361
申请日：2011-12-19
申请人： Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, JR. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
发明人： Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, JR. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
IPC分类号： C07D241/42 , C07D401/12 , C07D403/06 , C07D471/04 , A61K31/4985 , C07D471/10 , C07D405/12 , C07D401/14 , A61K31/506 , A61K31/55 , C07D417/12 , C07D498/04 , C07D491/107 , A61K45/06 , A61K31/498
CPC分类号： C07D241/42 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/55 , A61K45/06 , C07D241/38 , C07D241/44 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/048 , C07D491/107 , C07D498/04 , C07D498/10
摘要： The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译： 本发明提供了式（I）的某些喹喔啉和氮杂 - 喹喔啉及其药学上可接受的盐，其中J1，J2，R1，R2，R3，R22，Ra，Rb，Rc，Rd，X，Y，b，n ，和q如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。
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公开(公告)号：US09469615B2
公开(公告)日：2016-10-18
申请号：US13996361
申请日：2011-12-19
申请人： Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, Jr. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
发明人： Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, Jr. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
IPC分类号： C07D241/38 , C07D241/42 , A61K31/498 , A61K31/506 , A61K31/4985 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D403/06 , C07D471/04 , C07D471/10 , C07D491/107 , C07D498/04 , C07D403/12 , C07D401/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D241/44 , C07D417/14 , C07D491/048 , C07D498/10
CPC分类号： C07D241/42 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/55 , A61K45/06 , C07D241/38 , C07D241/44 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/048 , C07D491/107 , C07D498/04 , C07D498/10
摘要： The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
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公开(公告)号：US20100298359A1
公开(公告)日：2010-11-25
申请号：US12746313
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee
发明人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee
IPC分类号： A61K31/517 , C07D401/10 , A61K31/4725 , A61P29/00 , A61K39/395 , A61P25/28 , C07D403/10
CPC分类号： C07D471/04 , C07D401/10 , C07D403/10 , C07D491/04 , C07D498/04
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：US20110294784A1
公开(公告)日：2011-12-01
申请号：US13140987
申请日：2009-12-18
申请人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John Clader , Dmitri Pissarnitski , Hubert Josien , Hongmei Li
发明人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John Clader , Dmitri Pissarnitski , Hubert Josien , Hongmei Li
IPC分类号： A61K31/553 , A61P27/00 , A61P25/28 , A61P9/10 , C07D498/04 , A61P25/00
CPC分类号： C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). 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。 这些化合物具有式（化学式应该插在这里，如纸上所示）。 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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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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公开(公告)号：US20080019978A1
公开(公告)日：2008-01-24
申请号：US11771538
申请日：2007-06-29
申请人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
发明人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
IPC分类号： A61K31/519 , A61K31/397 , A61K31/56 , A61K31/60 , A61K38/16 , A61K39/395 , A61P1/00 , A61P11/00 , A61P3/00 , A61P3/10 , A61P35/00 , A61P9/00 , C07D239/70
CPC分类号： C07D491/04 , C07D471/04
摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
摘要翻译： 本发明提供式（I）的化合物及其药学上可接受的盐，溶剂合物，酯和互变异构体，其中：Q选自：和L选自：药物组合物，其包含一种或多种 更多的式（I）化合物和使用式（I）化合物的方法。
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