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1. 发明申请

US20110294784A1 GAMMA SECRETASE MODULATORS 有权
标题翻译： GAMMA秘密调节器
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。

2. 发明授权

US08357682B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
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。

3. 发明申请

US20100247514A1 GAMMA SECRETASE MODULATORS 有权
标题翻译： GAMMA秘密调节器
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。

4. 发明申请

US20070197581A1 Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权
标题翻译：苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂
公开(公告)号：US20070197581A1
公开(公告)日：2007-08-23
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas Bara , Chad Bennett , Duane Burnett , Mary Ann Caplen , John Clader , David Cole , Martin Domalski , Hubert Josien , Chad Knutson , Hongmei Li , Mark McBriar , Dmitri Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas Bara , Chad Bennett , Duane Burnett , Mary Ann Caplen , John Clader , David Cole , Martin Domalski , Hubert Josien , Chad Knutson , Hongmei Li , Mark McBriar , Dmitri Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： A61K31/4741 , A61K31/473 , A61K31/353 , A61K31/19
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。环烷基环或杂环烷基环可任选被一个或多个取代基取代。一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如，治疗阿尔茨海默病。

5. 发明申请

US20060004004A1 Novel gamma secretase inhibitors 审中-公开
标题翻译：新型γ分泌酶抑制剂
公开(公告)号：US20060004004A1
公开(公告)日：2006-01-05
申请号：US11098745
申请日：2005-04-04
申请人： Theodros Asberom , John Clader , Hubert Josien , Mark McBriar , Dmitri Pissarnitski , Zhiqiang Zhao
发明人： Theodros Asberom , John Clader , Hubert Josien , Mark McBriar , Dmitri Pissarnitski , Zhiqiang Zhao
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4545 , C07D413/14 , C07D41/14
CPC分类号： C07D451/04 , C07D211/96 , C07D401/06 , C07D401/12 , C07D413/06 , C07D413/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Gamma-secretase inhibitors of the formula: are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes —C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-C(O)—Y, —S(O)—Y, -alkylene-S(O)—Y, -alkylene-cycloalkylene-S(O)—Y, -cycloalkylene-alkylene-S(O)—Y, -alkylene-cycloalkylene-alkylene-S(O)—Y, -cycloalkylene-S(O)—Y, —S(O2)—Y, -alkylene-S(O2)—Y, -alkylene-cycloalkylene-S(O2)—Y, -cycloalkylene-alkylene-S(O2)—Y, -alkylene-cycloalkylene-alkylene-S(O2)—Y, and -cycloalkylene-S(O2)—Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, —O-alkyl, —OH, —N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, —C(O)—; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.
摘要翻译：下式的γ-分泌酶抑制剂：可用于治疗各种神经变性疾病，其中例如：R 1包括未取代或取代的芳基或杂芳基; R 2包括-C（O）-Y， - 亚烷基-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-C（O） - Y， - 亚烷基 - 亚环烷基 - 亚烷基-C（O）-Y-环亚烷基-C（O）-Y，-S（O）-Y-亚烷基-S（O）-Y-亚烷基 - 亚环烷基-S （O）-Y-亚烷基 - 亚烷基-S（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-S（O）-Y-亚烷基-S（O）-Y，-S（O） - 亚烷基-S（O）2 - 亚烷基 - 亚环烷基-S（O）2 - 亚烷基-S（O 2） -S（O）2 - 亚烷基 - 亚环烷基 - 亚烷基-S（O）2 - 和 - 亚环烷基-S（O 2） / Y，其中Y如本文所定义，并且所述亚烷基或亚环烷基中的每一个可以是未经取代的或如本文所提供的取代的; 每个R 3独立地包括H，烷基，-O-烷基，-OH，-N（R 9）2，酰基和芳酰基或其部分（R 3）2和连接在式I中的环碳原子一起定义为羰基，-C（O） - ; 每个R 3A和R 3B独立地包括H或烷基; R 11包括芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。一种或多种式I化合物或其药学上可接受的盐，溶剂化物和/或酯或其组合物可用于治疗，例如阿尔茨海默氏病。

6. 发明申请

US20060009467A1 Novel gamma secretase inhibitors 审中-公开
标题翻译：新型γ分泌酶抑制剂
公开(公告)号：US20060009467A1
公开(公告)日：2006-01-12
申请号：US11223545
申请日：2005-09-09
申请人： Hubert Josien , John Clader , Theodros Asberom , Dmitri Pissarnitski
发明人： Hubert Josien , John Clader , Theodros Asberom , Dmitri Pissarnitski
IPC分类号： A61K31/496 , A61K31/4545 , C07D403/02 , C07D401/02
CPC分类号： C07D401/06 , C07D211/56 , C07D211/58 , C07D211/62 , C07D401/12 , C07D403/06
摘要： Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.
摘要翻译：公开了新的芳基和杂芳基磺酰胺。作为γ分泌酶抑制剂的磺酰胺由下式表示：其中Ar 1和Ar 2独立地表示芳基或杂芳基，Y表示键或 - （C （R 3）2个）1-3个1-3个基团。还公开了抑制γ分泌酶的方法，以及使用式I化合物治疗阿尔茨海默病的方法。

7. 发明申请

US20060100427A1 Novel Gamma Secretase inhibitors 审中-公开
标题翻译：新型Gamma分泌酶抑制剂
公开(公告)号：US20060100427A1
公开(公告)日：2006-05-11
申请号：US11242337
申请日：2005-10-03
申请人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
发明人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
IPC分类号： A61K31/5377 , C07D413/02 , C07D401/14
CPC分类号： C07D401/12 , C07D211/96 , C07D401/14 , C07D409/12 , C07D471/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-X（CO）Y或亚烷基-X（CO）Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

8. 发明申请

US20050085506A1 Novel gamma secretase inhibitors 失效
标题翻译：新型γ分泌酶抑制剂
公开(公告)号：US20050085506A1
公开(公告)日：2005-04-21
申请号：US10941440
申请日：2004-09-15
申请人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
发明人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
IPC分类号： A61K31/445 , C07D211/60 , C07D43/02
CPC分类号： C07D401/14 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D491/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-XC（O）Y，亚烷基-XC（O）Y，亚环烷基-XC（O）-Y，-CH -XC（O）-NR 3 -Y或-CH-XC（O）-Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

9. 发明授权

US08759337B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08759337B2
公开(公告)日：2014-06-24
申请号：US13140987
申请日：2009-12-18
申请人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
发明人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
IPC分类号： A61K31/553 , C07D498/04
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。

10. 发明申请

US20110257156A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
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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