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11. 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。

12. 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：

13. 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。

14. 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.

15. 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。

16. 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。

17. 发明授权

US5149709A 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：US5149709A
公开(公告)日：1992-09-22
申请号：US547644
申请日：1990-07-03
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
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 from 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间断的烷基链; 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。

18. 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。

19. 发明申请

US20070155674A1 Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof 有权
公开(公告)号：US20070155674A1
公开(公告)日：2007-07-05
申请号：US11705977
申请日：2007-02-13
申请人： Duane Burnett , John Clader
发明人： Duane Burnett , John Clader
IPC分类号： A61K31/7052 , A61K31/397 , A61K31/695 , C07H17/02 , C07D205/02
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.

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