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1. 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。

2. 发明申请

US20050004121A1 MCH antagonists for the treatment of obesity 失效
标题翻译： MCH拮抗剂用于治疗肥胖
公开(公告)号：US20050004121A1
公开(公告)日：2005-01-06
申请号：US10878788
申请日：2004-06-28
申请人： Anandan Palani , Sherry Shapiro , Hubert Josien , Thomas Bara , John Clader , Pradeep Pushpavanam , Shengjian Li , Mark McBriar
发明人： Anandan Palani , Sherry Shapiro , Hubert Josien , Thomas Bara , John Clader , Pradeep Pushpavanam , Shengjian Li , Mark McBriar
IPC分类号： C07D409/14 , A61K31/5377 , A61K31/496
CPC分类号： C07D409/14
摘要： The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentrating hormone (MCH). In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of the invention generally have the structure: where the substituents are as defined herein.
摘要翻译：本发明公开了使用拮抗剂用于黑色素浓缩激素（MCH），治疗肥胖症，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法，以及作为黑色素浓缩激素（MCH）拮抗剂的新化合物。在其它方面，本发明涉及包含这种MCH拮抗剂的药物组合物以及制备这些化合物的方法。本发明的化合物通常具有以下结构：其中取代基如本文所定义。

3. 发明申请

US20140057836A1 HCV NS3 PROTEASE INHIBITORS 有权
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：US20140057836A1
公开(公告)日：2014-02-27
申请号：US13960343
申请日：2013-08-06
申请人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
发明人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
IPC分类号： C07K5/08 , A61K45/06 , A61K38/06
CPC分类号： C07K5/08 , A61K38/06 , A61K45/06 , C07D419/00 , C07D491/22
摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
摘要翻译：本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

4. 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。

5. 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。

6. 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。

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