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21. 发明申请

US20060040936A1 Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors 失效
标题翻译：取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂
公开(公告)号：US20060040936A1
公开(公告)日：2006-02-23
申请号：US11168797
申请日：2005-06-28
申请人： Hubert Josien , John Clader , Thomas Bara , Ruo Xu , Hongmei Li , Dmitri Pissarnitski , Zhiqiang Zhao
发明人： Hubert Josien , John Clader , Thomas Bara , Ruo Xu , Hongmei Li , Dmitri Pissarnitski , Zhiqiang Zhao
IPC分类号： A61K31/5377 , A61K31/498 , A61K31/496 , A61K31/46 , C07D43/02 , C07D413/02 , C07D487/04
CPC分类号： C07D265/30 , C07D413/12 , C07D451/02 , C07D487/08
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of: 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：其中：L是-O-，-N（R 6） - ， - S - ， - S（O） - 或-S（O - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-XC（O）-Y， - 亚烷基-XC（O）-Y， - 亚烷基-C（O ）-Y-亚烷基 - 亚环烷基-OC（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-OC（O）-Y-亚烷基 - 亚烷基-C（O） Y（ - ）亚环烷基-C（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基亚烷基-XC（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O）-Y，芳基和杂芳基; R 3选自芳基，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，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9，-N（R 6） - （CH 2）芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基 ; 或Y选自：一种或多种式I化合物或包含该化合物的制剂可用于，例如，治疗阿尔茨海默病。

22. 发明申请

US20050171129A1 Polycyclic guanine derivative phosphodiesterase V inhibitors 审中-公开
标题翻译：多环鸟嘌呤衍生物磷酸二酯酶V抑制剂
公开(公告)号：US20050171129A1
公开(公告)日：2005-08-04
申请号：US11020625
申请日：2004-12-23
申请人： Theodros Asberom , John Clader , Yueqing Hu , Dmitri Pissarnitski , Andrew Stamford , Ruo Xu
发明人： Theodros Asberom , John Clader , Yueqing Hu , Dmitri Pissarnitski , Andrew Stamford , Ruo Xu
IPC分类号： A61K31/519 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P11/00 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/10 , A61P27/06 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/14 , C07D487/20
CPC分类号： C07D487/14
摘要： A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
摘要翻译：具有式（Ia）或（b）的化合物，其盐或溶剂化物，具有本文定义的变量，其可以选择性抑制磷酸二酯酶V并且可用于治疗性功能障碍和其它生理障碍，症状和疾病：

23. 发明申请

US20110263529A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：US20110263529A1
公开(公告)日：2011-10-27
申请号：US13125995
申请日：2009-11-05
申请人： Ruo Xu , John W. Clader
发明人： Ruo Xu , John W. Clader
IPC分类号： A61K31/695 , A61P25/28 , A61K31/437 , C07F7/10 , C07D498/04
CPC分类号： C07D498/04 , C07F7/0812
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。

24. 发明授权

US08580956B2 Gamma secretase modulators 失效
标题翻译：伽玛分泌酶调节剂
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。

25. 发明申请

US20100255005A1 GAMMA SECRETASE MODULATORS 失效
公开(公告)号：US20100255005A1
公开(公告)日：2010-10-07
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： A61K39/395 , C07D498/04 , A61K31/437 , A61P25/28 , A61P29/00 , A61K39/00 , A61P27/06 , A61P9/10 , A61P27/00 , A61K31/5383 , C07D413/10 , A61K31/423 , A61K31/5025 , A61K31/4245 , A61K31/4439 , C07D498/14 , A61K31/445 , A61K31/473 , A61K38/17
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.

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