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1. 发明授权

US08450343B2 Gamma secretase modulators 失效
标题翻译：伽玛分泌酶调节剂
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。

2. 发明申请

US20110015190A1 GAMMA SECRETASE MODULATORS 失效
标题翻译： GAMMA秘密调节器
公开(公告)号：US20110015190A1
公开(公告)日：2011-01-20
申请号：US12746041
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhou , 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 Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhou , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
IPC分类号： A61K31/5383 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61K31/5377 , C07D498/04 , C07D403/02 , A61K31/4178 , A61P25/28
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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US09096582B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US09096582B2
公开(公告)日：2015-08-04
申请号：US14354992
申请日：2012-10-26
申请人： William Greenlee , Dmitri Pissarnitski , Zhiqiang Zhao , Zhaoning Zhu
发明人： William Greenlee , Dmitri Pissarnitski , Zhiqiang Zhao , Zhaoning Zhu
IPC分类号： C07D413/10
CPC分类号： C07D413/10 , C07D413/14
摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
摘要翻译：本文公开了式（I）的化合物及其药学上可接受的盐，其中每个取代基被给出如说明书和权利要求书中所阐述的定义。还公开了含有式（I）化合物的药物组合物和该化合物在治疗神经变性疾病或病症如阿尔茨海默病中的用途。

8. 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。

9. 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。

10. 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。

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