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11. 发明授权

US08501797B2 (2-aryl-1H-imidazol-4-yl)-linked heterocycle derivatives 有权
标题翻译：（2-芳基-1H-咪唑-4-基） - 连接的杂环衍生物
公开(公告)号：US08501797B2
公开(公告)日：2013-08-06
申请号：US13515325
申请日：2010-12-15
申请人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
发明人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC分类号： A61K31/415
CPC分类号： C07D487/04 , C07D471/04
摘要： This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及具有PDE10A酶抑制剂结构的式I化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经退行性疾病的受试者的方法，包括给予受试者治疗有效量的式I化合物本发明还提供了治疗患有药物成瘾的受试者的方法，包括向受试者施用治疗有效量的式I化合物。本发明还提供治疗患有精神障碍的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。

12. 发明申请

US20120129836A1 Imidazole derivatives as PDE10A enzyme inhibitors 有权
标题翻译：咪唑衍生物作为PDE10A酶抑制剂
公开(公告)号：US20120129836A1
公开(公告)日：2012-05-24
申请号：US13299368
申请日：2011-11-18
申请人： Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
发明人： Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
IPC分类号： A61K31/4985 , C07D471/04 , A61K31/437 , A61P25/14 , A61P25/18 , A61K31/5513 , A61K31/519 , A61K31/554 , C07D487/04 , A61P25/28
CPC分类号： C07D487/04 , A61K31/437 , A61K31/4985 , A61K45/06 , C07D471/04 , C07D519/00
摘要： This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及PDE10A酶抑制剂的化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予治疗有效量的式I化合物。

13. 发明授权

US08501795B2 (3-aryl-1H-1,2,4-triazol-5-yl)-linked heterocycle derivatives 有权
标题翻译：（3-芳基-1H-1,2,4-三唑-5-基） - 连接的杂环衍生物
公开(公告)号：US08501795B2
公开(公告)日：2013-08-06
申请号：US13515351
申请日：2010-12-15
申请人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
发明人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC分类号： A61K31/41
CPC分类号： C07D487/04 , C07D471/04
摘要： This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及具有PDE10A酶抑制剂结构的式I化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予治疗有效量的式I化合物。

14. 发明申请

US20120309714A1 Heteroaromatic Phenylimidazole derivatives as PDE10A enzyme inhibitors 有权
标题翻译：杂芳基苯基咪唑衍生物作为PDE10A酶抑制剂
公开(公告)号：US20120309714A1
公开(公告)日：2012-12-06
申请号：US13513867
申请日：2010-12-15
申请人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
发明人： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC分类号： A61K31/519 , C07D471/04 , A61K31/437 , A61K31/4985 , C07F7/10 , A61K31/496 , A61P25/28 , A61P25/18 , A61P25/00 , A61P25/22 , A61K31/551 , A61K31/554 , C07D487/04 , A61K31/695
CPC分类号： A61K31/4985 , A61K45/06 , C07D471/04 , C07D487/04
摘要： This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及PDE10A酶抑制剂的化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予治疗有效量的式I化合物。

15. 发明授权

US07858620B2 Cyanoisoquinoline 失效
标题翻译：氰基异喹啉
公开(公告)号：US07858620B2
公开(公告)日：2010-12-28
申请号：US12208799
申请日：2008-09-11
申请人： Jan Kehler , Jacob Nielsen , Morten Langgaard
发明人： Jan Kehler , Jacob Nielsen , Morten Langgaard
IPC分类号： A61K31/496 , A61K31/5377 , C07D217/22
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D417/04
摘要： This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及PDE10A酶抑制剂的化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明进一步提供了治疗患有精神障碍的受试者的方法，包括向受试者施用治疗有效量的式I化合物。

16. 发明申请

US20090075988A1 CYANOISOQUINOLINE 失效
标题翻译：氰基喹啉
公开(公告)号：US20090075988A1
公开(公告)日：2009-03-19
申请号：US12208799
申请日：2008-09-11
申请人： Jan Kehler , Jacob Nielsen , Morten Langgaard
发明人： Jan Kehler , Jacob Nielsen , Morten Langgaard
IPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D401/14 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P25/00 , A61P25/28 , A61P25/30
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D417/04
摘要： This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
摘要翻译：本发明涉及PDE10A酶抑制剂的化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明进一步提供了治疗患有精神障碍的受试者的方法，包括向受试者施用治疗有效量的式I化合物。

17. 发明授权

US08173639B2 Isoquinolinone derivatives as NK3 antagonists 失效
标题翻译：异喹啉酮衍生物作为NK3拮抗剂
公开(公告)号：US08173639B2
公开(公告)日：2012-05-08
申请号：US12101592
申请日：2008-04-11
申请人： Klaus Baek Simonsen , Jan Kehler , Karsten Juhl , Nikolay Khanzhin , Soren Moller Nielsen
发明人： Klaus Baek Simonsen , Jan Kehler , Karsten Juhl , Nikolay Khanzhin , Soren Moller Nielsen
IPC分类号： C07D217/26 , C07D401/02 , A61K31/47
CPC分类号： C07D217/24 , C07D401/06 , C07D413/06 , C07D487/08
摘要： Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.
摘要翻译：提供了通式的异喹诺酮衍生物。化合物是NK3拮抗剂，可用于治疗例如精神病和精神分裂症。

18. 发明授权

US07223765B2 4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives 失效
标题翻译： 4-苯基-1-哌嗪基，哌啶基和四氢吡啶基衍生物
公开(公告)号：US07223765B2
公开(公告)日：2007-05-29
申请号：US11377772
申请日：2006-03-15
申请人： Benny Bang-Andersen , Jan Kehler , Jakob Felding
发明人： Benny Bang-Andersen , Jan Kehler , Jakob Felding
IPC分类号： A61K31/496 , C07D403/06 , C07D403/12
CPC分类号： C07D215/227 , C07D209/08 , C07D209/30 , C07D217/06 , C07D295/073
摘要： The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.
摘要翻译：本发明涉及具有式I的取代的4-苯基-1-哌嗪基衍生物，其中W是C，CH或N，当W是C时，由W发出的虚线表示键，当W是N或CH时，没有键 ; X是CH 2，O，S，CO，CS，SO或SO 2; Q为下式的基团，其中Z为3至4个链成员的链; 其中链成员选自C，CH，CH 2，CO，N和NH，条件是链中只有一个可以是N或NH，并且所述链任选地含有一个或两个双债券条件是当基团Q经由N原子连接时，X不为O或S; 及其任何对映异构体及其酸加成盐。这些化合物对D 4 S受体具有高亲和力。

19. 发明申请

US20060287386A1 Benzo[b]furane and benzo[b]thiophene derivatives 失效
公开(公告)号：US20060287386A1
公开(公告)日：2006-12-21
申请号：US11452823
申请日：2006-06-14
申请人： Jan Kehler , Karsten Juhl , Morten Norgaard
发明人： Jan Kehler , Karsten Juhl , Morten Norgaard
IPC分类号： A61K31/381 , A61K31/343 , C07D333/56
CPC分类号： C07D307/82 , C07D333/62
摘要： The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.

20. 发明申请

US20060148815A1 4-Phenyl-1-piperazinyl, -piperidinyl and-tetrahydropyridyl derivatives 失效
标题翻译： 4-苯基-1-哌嗪基，哌啶基和四氢吡啶基衍生物
公开(公告)号：US20060148815A1
公开(公告)日：2006-07-06
申请号：US11377772
申请日：2006-03-15
申请人： Benny Bang-Andersen , Jan Kehler , Jakob Felding
发明人： Benny Bang-Andersen , Jan Kehler , Jakob Felding
IPC分类号： A61K31/496 , A61K31/454 , C07D403/02 , C07D401/02
CPC分类号： C07D215/227 , C07D209/08 , C07D209/30 , C07D217/06 , C07D295/073
摘要： The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.
摘要翻译：本发明涉及具有式I的取代的4-苯基-1-哌嗪基衍生物，其中W是C，CH或N，当W是C时，由W发出的虚线表示键，当W是N或CH时，没有键 ; X是CH 2，O，S，CO，CS，SO或SO 2; Q为下式的基团，其中Z为3至4个链成员的链; 其中链成员选自C，CH，CH 2，CO，N和NH，条件是链中只有一个可以是N或NH，并且所述链任选地含有一个或两个双债券条件是当基团Q经由N原子连接时，X不为O或S; 及其任何对映异构体及其酸加成盐。这些化合物对D 4 S受体具有高亲和力。

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