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1. 发明申请

US20100087496A1 NOVEL CINNAMIC AMIDE DERIVATIVES USEFUL AS ION CHANNEL MODULATORS 审中-公开
标题翻译：作为离子通道调制器有用的新型的CINNAMIC AMIDE衍生物
公开(公告)号：US20100087496A1
公开(公告)日：2010-04-08
申请号：US12519683
申请日：2007-12-17
申请人： Antonio Nardi , Morten Grunnet , Joachim Demnitz , Thomas Diness Jensen , Palle Christophersen , David Spencer Jones , Elsebet Ostergaard Nielsen , Dorte Strobaek , Lars Siim Madsen
发明人： Antonio Nardi , Morten Grunnet , Joachim Demnitz , Thomas Diness Jensen , Palle Christophersen , David Spencer Jones , Elsebet Ostergaard Nielsen , Dorte Strobaek , Lars Siim Madsen
IPC分类号： A61K31/165 , C07C233/01 , C07D257/04 , A61K31/41 , A61P15/00
CPC分类号： C07C309/15 , C07C1/26 , C07C17/10 , C07C311/08 , C07C311/09 , C07C311/21 , C07C311/46 , C07C311/51 , C07C2529/40 , C07C9/00 , C07C19/075
摘要： This invention relates to novel cinnamic amide derivatives that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of ion channels.
摘要翻译：本发明涉及被认为是离子通道的有效调节剂的新型肉桂酰胺衍生物，因此，它们是用于治疗与对离子通道调节有反应的疾病或病症多种多样的有价值的候选物。

2. 发明申请

US20080214820A1 Enantiomers of 3-Heteroaryl-8H-8-Azabicyclo (3.2.1) Oct-2-Ene and their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors 失效
标题翻译： 3-杂芳基-8,8-8-氮杂双环（3.2.1）十二-2-烯的对映异构体及其作为单胺神经递质重吸收抑制剂的用途
公开(公告)号：US20080214820A1
公开(公告)日：2008-09-04
申请号：US11793137
申请日：2005-12-15
申请人： Dan Peters , David Tristram Brown , Borje Egestad , Eva Dam , David Spencer Jones , Brian Frostrup , Elsebet Ostergaard Nielsen , Gunnar M. Olsen , John Paul Redrobe
发明人： Dan Peters , David Tristram Brown , Borje Egestad , Eva Dam , David Spencer Jones , Brian Frostrup , Elsebet Ostergaard Nielsen , Gunnar M. Olsen , John Paul Redrobe
IPC分类号： A61K31/46 , C07D221/22 , A61P25/26
CPC分类号： C07D451/02
摘要： This invention relates to novel enantiomers useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型对映异构体。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

3. 发明授权

US08110586B2 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 失效
标题翻译： 8-氮杂 - 双环[3.2.1]辛烷衍生物及其作为单胺神经递质再摄取抑制剂的用途
公开(公告)号：US08110586B2
公开(公告)日：2012-02-07
申请号：US11992836
申请日：2006-11-09
申请人： Dan Peters , Birgitte L. Eriksen , Elsebet Ostergaard Nielsen , John Paul Redrobe , Gunnar M. Olsen
发明人： Dan Peters , Birgitte L. Eriksen , Elsebet Ostergaard Nielsen , John Paul Redrobe , Gunnar M. Olsen
IPC分类号： A61K31/439 , C07D451/10 , C07D451/12 , C07D451/06 , A61P25/00 , A61P25/24 , A61P15/12 , A61P15/10 , A61P13/00
CPC分类号： C07D451/06
摘要： This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型8-氮杂 - 双环[3.2.1]辛烷衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

4. 发明申请

US20090233929A1 Imidazole Derivatives for the Treatment of Anxiety and Related Diseases 失效
标题翻译：用于治疗焦虑和相关疾病的咪唑衍生物
公开(公告)号：US20090233929A1
公开(公告)日：2009-09-17
申请号：US12083375
申请日：2006-10-12
申请人： William Dalby Brown , Janus S. Larsen , Lene Teuber , David Tristram Brown , Philip K. Ahring , Naheed Mirza , Elsebet Ostergaard Nielsen
发明人： William Dalby Brown , Janus S. Larsen , Lene Teuber , David Tristram Brown , Philip K. Ahring , Naheed Mirza , Elsebet Ostergaard Nielsen
IPC分类号： A61K31/5377 , A61K31/44 , A61K31/415 , C07D413/02 , C07D401/00 , C07D233/02
CPC分类号： C07D233/64 , C07D233/90 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D417/06
摘要： This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
摘要翻译：本发明涉及新颖的咪唑衍生物，含有这些化合物的药物组合物及其处理方法。本发明的化合物可用于治疗中枢神经系统疾病和病症，其对GABA A受体复合物的调节有反应，特别是用于对抗焦虑和相关疾病。

5. 发明申请

US20090111841A1 Novel 3,9-Diaza-Spiro[5,5]Undecane Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors 失效
标题翻译：新型3,9-二氮杂螺[5,5]十一烷衍生物及其用作单胺神经递质重吸收抑制剂
公开(公告)号：US20090111841A1
公开(公告)日：2009-04-30
申请号：US11922931
申请日：2006-06-28
申请人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , John Paul Redrobe
发明人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , John Paul Redrobe
IPC分类号： A61K31/438 , C07D221/20 , A61P25/28 , A61P25/16 , A61P31/12 , A61P25/22 , A61P25/24
CPC分类号： C07D471/10
摘要： This invention relates to novel 3,9-diaza-spiro[5.5]undecane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型3,9-二氮杂螺[5.5]十一烷衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

6. 发明申请

US20090075983A1 Novel Diazabicycloalkane Derivatives and Their Medical Use 审中-公开
标题翻译：新型二氮杂双环烷烃衍生物及其医疗用途
公开(公告)号：US20090075983A1
公开(公告)日：2009-03-19
申请号：US12087598
申请日：2007-02-13
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Jeppe Kejser Christensen , Tino Dyhring
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Jeppe Kejser Christensen , Tino Dyhring
IPC分类号： A61K31/4995 , C07D487/08 , A61K31/551 , A61P25/00 , A61P29/00
CPC分类号： C07D471/08
摘要： This invention relates to novel diaza-bicyclo-alkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新的二氮杂双环烷烃衍生物，其被发现是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

7. 发明申请

US20090036477A1 Novel 3-Aza-Spiro[5,5]Undec-8-Ene Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors 失效
标题翻译：新型3-氮杂螺[5,5] Undec-8-Ene衍生物及其用作单胺神经递质重吸收抑制剂
公开(公告)号：US20090036477A1
公开(公告)日：2009-02-05
申请号：US11922929
申请日：2006-06-28
申请人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , John Paul Redrobe
发明人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , John Paul Redrobe
IPC分类号： A61K31/438 , C07D221/20 , A61P25/24
CPC分类号： C07D221/20
摘要： This invention relates to novel 3-aza-spiro[5.5]undec-8-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型3-氮杂 - 螺[5.5]十一碳-8-烯衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

8. 发明申请

US20090023772A1 Novel substituted heteroaryloxy alkylamines and their use as monoamine neurotransmitter re-uptake inhibitors 审中-公开
标题翻译：新型取代的杂芳氧基烷基胺及其作为单胺神经递质再摄取抑制剂的用途
公开(公告)号：US20090023772A1
公开(公告)日：2009-01-22
申请号：US11658892
申请日：2005-08-24
申请人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , Jorgen Scheel-Kruger , Gunnar M. Olsen
发明人： Birgitte L. Eriksen , Dan Peters , Elsebet Ostergaard Nielsen , Jorgen Scheel-Kruger , Gunnar M. Olsen
IPC分类号： A61K31/47 , C07D215/20 , A61P25/00
CPC分类号： C07D217/02 , C07D213/64 , C07D215/227 , C07D215/233
摘要： This invention relates to novel substituted heteroaryloxy alkylamines useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及可用作单胺神经递质再摄取抑制剂的新型取代的杂芳氧基烷基胺。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

9. 发明申请

US20080188519A1 Novel azacyclic ethynyl derivatives 失效
标题翻译：新型氮杂环乙炔衍生物
公开(公告)号：US20080188519A1
公开(公告)日：2008-08-07
申请号：US12076929
申请日：2008-03-25
申请人： Dan Peters , Gurmar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Philip K. Ahring
发明人： Dan Peters , Gurmar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Philip K. Ahring
IPC分类号： C07D453/02 , A61K31/439 , A61P3/00 , A61P25/00
CPC分类号： C07D451/02 , C07D211/70 , C07D453/02
摘要： Azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中发现其是胆碱能配体的偶氮环乙炔衍生物。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

10. 发明授权

US06392045B1 9-azobicyclo[3.3.1] non-2-ene derivatives as cholinergic ligands at nicotinic ACH receptors 失效
标题翻译： 9-偶氮双环[3.3.1]壬-2-烯衍生物作为烟碱型ACH受体上的胆碱能配体
公开(公告)号：US06392045B1
公开(公告)日：2002-05-21
申请号：US09450635
申请日：1999-11-29
申请人： Dan Peters , Gunnar M. Olsen , Simon Feldbaek Nielsen , Elsebet Ostergaard Nielsen
发明人： Dan Peters , Gunnar M. Olsen , Simon Feldbaek Nielsen , Elsebet Ostergaard Nielsen
IPC分类号： C07D40304
CPC分类号： C07D451/14
摘要： The present invention discloses compounds of formula (1), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof, wherein ---- is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; or a bicyclic heteroaryl group composed of a monocyclic 5 to 6 membered heteroaryl group fused to a benzene ring or fused to another monocyclic 5 to 6 membered heteroaryl, all of which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group. The compounds of the invention are useful as nicotinic ACh receptor ligands.
摘要翻译：本发明公开了式（1）的化合物，其任何对映体或其任何混合物或其药学上可接受的盐，其中----是单键或双键; R是氢，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基; 并且R 1是（a），其中R 2是氢，烷基，烯基，炔基，环烷基，环烷基烷基，氨基; 可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，氨基酰基等的取代基取代一次或多次的芳基，硝基，芳基和单环5至6元杂芳基; 可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3， OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基; 或由与苯环稠合或与另一个单环5至6元杂芳基稠合的单环5至6元杂芳基组成的双环杂芳基，所有这些可以与选自以下的取代基取代一次或多次：烷基烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基。本发明的化合物可用作烟碱ACh受体配体。

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