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公开(公告)号：US20100137320A1
公开(公告)日：2010-06-03
申请号：US12393630
申请日：2009-02-26
申请人： Xianhai Huang , Anandan Palani , Robert G. Aslanian , Wei Zhou
发明人： Xianhai Huang , Anandan Palani , Robert G. Aslanian , Wei Zhou
IPC分类号： A61K31/5025 , C07D487/04 , A61P25/28 , A61P25/00
CPC分类号： C07D487/04
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：US08426403B2
公开(公告)日：2013-04-23
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 , A61K31/5395 , C07D498/04 , 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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53.发明申请公开(公告)号：US20120329743A1
公开(公告)日：2012-12-27
申请号：US13523354
申请日：2012-06-14
申请人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号： C07D221/16 , C07D413/10 , A61K31/5377 , C07D401/10 , A61P11/00 , A61K31/501 , C07H15/26 , A61K31/706 , A61P11/06 , A61P37/08 , A61K31/473 , A61K31/506
CPC分类号： C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t 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： 本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8，R8a，E，Y，Z，n，u和t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：US20120232108A1
公开(公告)日：2012-09-13
申请号：US13377598
申请日：2010-06-15
IPC分类号： A61K31/437 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04
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.
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公开(公告)号：US20100297128A1
公开(公告)日：2010-11-25
申请号：US12747011
申请日：2008-12-09
IPC分类号： A61K39/395 , C07D487/04 , C07D471/04 , C07D473/32 , A61K31/5025 , A61K31/437 , A61K31/52 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04 , C07D471/04
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 electronic 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。 化合物具有式[化学式应该插入在此，其以电子形式的摘要出现。]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：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：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：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：US20110257156A1
公开(公告)日：2011-10-20
申请号：US13126056
申请日：2009-11-05
申请人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
发明人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
IPC分类号： A61K31/55 , A61K31/5383 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/438 , A61K31/437 , C07D413/10 , C07D498/20 , C07D498/04 , A61P25/00 , A61P25/28 , A61K31/4245 , A61K31/5386
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides novel 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此类化合物的药物制剂的方法，以及治疗方法， 使用这种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：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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