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1. 发明授权

US08569521B2 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：US08569521B2
公开(公告)日：2013-10-29
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00
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 substituents. 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：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4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。

2. 发明授权

US08067621B2 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：US08067621B2
公开(公告)日：2011-11-29
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00 , A61K31/35
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：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4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。

3. 发明申请

US20120264736A1 BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 有权
标题翻译：苯并呋喃酮，噻吗啉，四氢萘酮和相关的游离氨基酸酶抑制剂
公开(公告)号：US20120264736A1
公开(公告)日：2012-10-18
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： A61K31/352 , C07D409/12 , A61K31/381 , C07D405/12 , A61K31/4433 , A61K31/496 , C07D487/08 , A61K31/4995 , C07D405/14 , A61K31/4545 , C07D413/08 , A61K31/5377 , C07D493/04 , C07D491/052 , A61P25/28 , C07D311/80
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 substituents. 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：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4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

US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 有权
标题翻译：四氢吡喃葡萄糖消炎酶抑制剂
公开(公告)号：US20110236400A1
公开(公告)日：2011-09-29
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
IPC分类号： A61K39/395 , C07D493/04 , C07D311/80 , C07D407/12 , A61K31/35 , A61K31/352 , A61K31/381 , A61P25/28 , A61P29/00 , A61P31/00 , C07C201/12 , C07C67/343
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - （O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-O-C（O ） - 杂芳基和碱性叔胺。

5. 发明授权

US08664411B2 Tetrahydropyranochromene gamma secretase inhibitors 有权
标题翻译：四氢吡喃色烯γ分泌酶抑制剂
公开(公告)号：US08664411B2
公开(公告)日：2014-03-04
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
IPC分类号： C07D311/80 , C07D493/04 , A61K31/352
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和碱性叔胺。

6. 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。

7. 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。

8. 发明申请

US20110110948A1 BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 有权
标题翻译：苯并呋喃酮，噻吗啉，四氢萘酮和相关的游离氨基酸酶抑制剂
公开(公告)号：US20110110948A1
公开(公告)日：2011-05-12
申请号：US12668550
申请日：2008-07-15
申请人： Thavalakulamgara K. Sasikumar , Duane A. Burnett , Theodros Asberom , Wen-Lian Wu , Hongmei Li , Ruo Xu , Hubert B. Josien
发明人： Thavalakulamgara K. Sasikumar , Duane A. Burnett , Theodros Asberom , Wen-Lian Wu , Hongmei Li , Ruo Xu , Hubert B. Josien
IPC分类号： A61K39/395 , C07D513/04 , C07D493/04 , C07D491/052 , C07D491/147 , C07D513/14 , A61K31/542 , A61K31/352 , A61K31/407 , A61K31/436 , A61K31/4162 , A61K31/519 , A61K31/549 , A61P25/28 , A61P29/00 , A61P31/00
CPC分类号： C07D493/04 , C07D491/04 , C07D513/04 , C07D513/14
摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.
摘要翻译：公开了式（I）的新型γ-分泌酶抑制剂：或其药学上可接受的盐，溶剂化物或酯，其中L 1，n，X，Ar，Y，Z，Q和Q 1如本文所定义。还公开了抑制γ分泌酶的方法，治疗阿尔茨海默氏病的方法，治疗一种或多种神经变性疾病的方法，以及抑制淀粉样蛋白（例如，淀粉样β蛋白）沉积在神经组织内或周围的方法（例如，大脑）使用式1.0化合物。

9. 发明授权

US08618123B2 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：US08618123B2
公开(公告)日：2013-12-31
申请号：US12668550
申请日：2008-07-15
申请人： Thavalakulamgara K. Sasikumar , Duane A. Burnett , Theodros Asberom , Wen-Lian Wu , Hongmei Li , Ruo Xu , Hubert B. Josien
发明人： Thavalakulamgara K. Sasikumar , Duane A. Burnett , Theodros Asberom , Wen-Lian Wu , Hongmei Li , Ruo Xu , Hubert B. Josien
IPC分类号： A01N43/42 , A01N43/18 , A01N43/16 , A01N41/10 , A61K31/44 , A61K31/38 , A61K31/35 , A61K31/10 , C07D221/18 , C07D221/22 , C07D409/00 , C07D335/04 , C07D495/00 , C07D311/78 , C07D311/94 , C07C315/00 , C07C317/00
CPC分类号： C07D493/04 , C07D491/04 , C07D513/04 , C07D513/14
摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.
摘要翻译：公开了式（I）的新型γ-分泌酶抑制剂：或其药学上可接受的盐，溶剂化物或酯，其中L 1，n，X，Ar，Y，Z，Q和Q 1如本文所定义。还公开了抑制γ分泌酶的方法，治疗阿尔茨海默氏病的方法，治疗一种或多种神经变性疾病的方法，以及抑制淀粉样蛋白（例如，淀粉样β蛋白）沉积在神经组织内或周围的方法（例如，大脑）使用式1.0化合物。

10. 发明申请

US20100093695A1 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：US20100093695A1
公开(公告)日：2010-04-15
申请号：US12633311
申请日：2009-12-08
申请人： Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitski , Zhiqiang Zhao
发明人： Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitski , Zhiqiang Zhao
IPC分类号： A61K31/438 , C07D413/14 , A61K31/5377 , C07D413/12 , C07D487/04 , A61K31/55 , A61K31/551
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（R6） - ， - S - ， - S（O） - 或-S（O 2） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-X-C（O）-Y， - 亚烷基-X-C（O）-Y， - 亚烷基-C（O）-Y， - 亚烷基 - 亚环烷基-X-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚烷基-C（O）（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-X-C（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）b -NR 8 R 9，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。

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