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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。

3. 发明申请

US20050171098A1 MCH antagonists and their use in the treatment of obesity 失效
公开(公告)号：US20050171098A1
公开(公告)日：2005-08-04
申请号：US11045713
申请日：2005-01-28
申请人： John Clader , Hubert Josien , Anandan Palani , Tin Chan
发明人： John Clader , Hubert Josien , Anandan Palani , Tin Chan
IPC分类号： C07D295/12 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K45/00 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/12 , A61P25/00 , A61P43/00 , C07D211/26 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/96 , C07D211/98 , C07D241/04 , C07D295/155 , C07D295/215 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , A61K31/541 , A61K31/496 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D295/215 , A61K45/06 , C07D211/26 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/96 , C07D211/98 , C07D295/155 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14
摘要： The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

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

US20070155675A1 Substituted azetidinone compunds, processes for preparing the same, formulations and uses thereof 有权
标题翻译：取代的氮杂环丁酮化合物，其制备方法，制剂和用途
公开(公告)号：US20070155675A1
公开(公告)日：2007-07-05
申请号：US11705978
申请日：2007-02-13
申请人： Duane Burnett , John Clader , Wayne Vaccaro
发明人： Duane Burnett , John Clader , Wayne Vaccaro
IPC分类号： A61K31/7052 , A61K31/506 , A61K31/4025 , A61K31/397
CPC分类号： C07D403/12 , C07D205/08 , Y10S930/28
摘要： The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.
摘要翻译：本发明提供取代的氮杂环丁酮化合物，其制备方法及其制备方法，其可用于治疗受试者血管病变如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低血浆中甾醇和/或甾烷醇的水平。

6. 发明授权

US5326762A Inhibitors of acyl-coenzyme A: cholesterol acyl transferase 失效
标题翻译：酰基辅酶A抑制剂：胆固醇酰基转移酶
公开(公告)号：US5326762A
公开(公告)日：1994-07-05
申请号：US885420
申请日：1992-05-19
申请人： John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
发明人： John Clader , Sundeep Dugar , Timothy Kogan , Bradley Tait , Wayne Vaccaro
IPC分类号： C07C233/18 , C07C233/20 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08 , H01N43/40 , C07D211/70
CPC分类号： C07C233/20 , C07C233/18 , C07C233/22 , C07C233/36 , C07C233/38 , C07C233/40 , C07C233/49 , C07C233/51 , C07C235/50 , C07C237/22 , C07C271/22 , C07C311/08 , Y10S514/824
摘要： Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.
摘要翻译：其中R 1和R 2独立地是杂芳基，X取代的杂芳基，X取代的苯基，N-取代的三嗪基或N-取代的咪唑基; 此外，R 1和R 2中的一个可以如上所定义，另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH - ， - N（低级烷基） - ， - C ） - ，亚苯基，X取代亚苯基，亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的中断的烷基链; R4是氢，低级烷基，苯基，X取代的苯基，杂芳基或X取代的杂芳基; 或其药学上可接受的盐，其可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

7. 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。

8. 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。

9. 发明申请

US20070155676A1 Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof 有权
标题翻译：取代的氮杂环丁酮化合物，其制备方法，制剂及其用途
公开(公告)号：US20070155676A1
公开(公告)日：2007-07-05
申请号：US11708449
申请日：2007-02-20
申请人： Duane Burnett , John Clader
发明人： Duane Burnett , John Clader
IPC分类号： A61K31/7052 , A61K31/506 , A61K31/4709 , A61K31/4025 , A61K31/4439 , A61K31/397 , C07D405/14 , C07D405/02
CPC分类号： C07D405/12 , C07D405/14 , Y10S930/28
摘要： The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.
摘要翻译：本发明提供取代的氮杂环丁酮化合物，其制备方法及其制备方法，其可用于治疗受试者的血管病症如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低血浆中甾醇和/或甾醇的水平。

10. 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。

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