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31. 发明授权

US08173658B2 Diazabicycylic aryl derivatives and their medical use 失效
标题翻译：二氮杂双环芳基衍生物及其医疗用途
公开(公告)号：US08173658B2
公开(公告)日：2012-05-08
申请号：US12093655
申请日：2006-12-05
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
IPC分类号： C07D403/04 , A61K31/501 , A61P25/28 , A61P29/00 , A61P25/04
CPC分类号： C07D471/08
摘要： This invention relates to novel diazabicyclic aryl 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芳基衍生物，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。

32. 发明申请

US20100227869A1 ENANTIOPURE QUINUCLIDINYLOXY PYRIDAZINES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
标题翻译：纯化喹啉吡啶吡啶并使用它作为NICOTINIC乙酰胆碱受体配体
公开(公告)号：US20100227869A1
公开(公告)日：2010-09-09
申请号：US12160402
申请日：2007-02-13
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
IPC分类号： A61K31/501 , C07D403/12 , A61P25/00 , A61P29/00 , A61P1/00 , A61P9/12 , A61P15/00 , A61P17/00
CPC分类号： C07D453/02
摘要： This invention relates to novel enantiopure azabicyclo pyridazinyloxy 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：本发明涉及新型对映纯氮氮杂双环哒嗪氧基衍生物，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。

33. 发明申请

US20100210625A1 NOVEL1,4-DIAZA-BICYCLO[3.2.2]NONYL HETEROARYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 失效
标题翻译：新的1,4-二氮杂双环[3.2.2]有用的非线性乙酰胆碱受体配体有用的非对映异构体衍生物
公开(公告)号：US20100210625A1
公开(公告)日：2010-08-19
申请号：US12733168
申请日：2008-08-14
申请人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser
发明人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser
IPC分类号： A61K31/551 , C07D487/08 , A61P29/00 , A61P25/30 , A61P17/00 , A61P1/00 , A61P15/00 , A61P25/06 , A61P25/18 , A61P25/28 , A61P25/16 , A61P25/08
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl heteroaryl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.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1,4-二氮杂 - 双环[3.2.2]壬基杂芳基衍生物及其在制备药物组合物中的用途。发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。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。

34. 发明授权

US07750011B2 Diazabicyclic aryl derivatives and their medical use 失效
标题翻译：二氮杂双环芳基衍生物及其医疗用途
公开(公告)号：US07750011B2
公开(公告)日：2010-07-06
申请号：US11884345
申请日：2006-02-13
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring
IPC分类号： C07D403/04 , C07D401/04 , C07D409/04 , C07D405/14 , A61K31/501 , A61K31/497 , A61P21/00 , A61P5/00 , A61P25/00 , A61P29/00
CPC分类号： C07D487/08
摘要： This invention relates to novel diazabicyclic aryl 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：本发明涉及在尼古丁乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体的新的二氮杂双环芳基衍生物。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。

35. 发明授权

US07652010B2 Azabicyclic aryl derivatives and their medical use 失效
标题翻译：氮杂芳基衍生物及其医疗用途
公开(公告)号：US07652010B2
公开(公告)日：2010-01-26
申请号：US11663152
申请日：2005-10-14
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen
IPC分类号： A61K31/35 , A61K31/501 , A61K31/53 , A61K31/497 , A61K31/506 , C07D401/04 , C07D498/08 , C07D513/08 , C07D515/08 , C07D401/12 , C07D403/12 , C07D405/12 , A61K43/66 , A61P29/00 , C07D453/02
CPC分类号： C07D453/02
摘要： Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, 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 may be used for the treatment of various diseases or disorders, including 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：包括氮杂双环辛基 - 哒嗪基 - 氧化合物的氮杂二吖啶基化合物，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，该化合物可用于治疗各种疾病或病症，包括与中枢神经系统（CNS）胆碱能系统，周围神经系统（PNS），与平滑相关的疾病或病症肌肉收缩，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，疼痛和戒断症状有关的疾病或病症。

36. 发明授权

US07612074B2 Diazabicyclic aryl derivatives as cholinergy ligands 失效
标题翻译：二氮杂双环芳基衍生物作为胆碱能配体
公开(公告)号：US07612074B2
公开(公告)日：2009-11-03
申请号：US11663967
申请日：2005-11-29
申请人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen
发明人： Dan Peters , Daniel B. Timmermann , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen
IPC分类号： A61K31/497
CPC分类号： C07D487/08
摘要： This invention relates to novel diazabicyclic aryl compounds of the formula wherein: R′ represents hydrogen or alkyl; A represents an aromatic monocyclic or bicyclic carbocyclic or heterocyclic; and is hydrogen or a subsituent as defined in the specification. The compounds are cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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：本发明涉及下式的新的二氮杂双环芳基化合物：其中：R'表示氢或烷基; A表示芳族单环或双环碳环或杂环; 并且是如本说明书中定义的氢或取代基。这些化合物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。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）的胆碱能系统，与平滑肌收缩有关的疾病或病症的疾病或病症多种化的疾病或病症，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，疼痛和戒断症状有关的疾病或病症。

37. 发明授权

US08101598B2 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their medical use 有权
标题翻译： 1,4-二氮杂双环[3.2.2]壬基恶二唑基衍生物及其医疗用途
公开(公告)号：US08101598B2
公开(公告)日：2012-01-24
申请号：US12861420
申请日：2010-08-23
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel
IPC分类号： A61P25/00 , A61K31/551 , C07D471/08
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。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。

38. 发明授权

US07514450B2 Azabicyclic aryl derivatives 失效
标题翻译：偶氮二芳基衍生物
公开(公告)号：US07514450B2
公开(公告)日：2009-04-07
申请号：US10591871
申请日：2005-05-10
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B. Timmermann
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B. Timmermann
IPC分类号： A01N43/90 , A61K31/44 , C07D453/02
CPC分类号： C07D453/02
摘要： This invention relates to novel azabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. 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：本发明涉及在尼古丁乙酰胆碱受体中被发现是胆碱能配体的新的氮杂双环芳基衍生物。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。

39. 发明申请

US20110257161A1 NOVEL DIAZA-BICYCLONONYL-PHENYL DERIVATIVES AND THEIR MEDICAL USE 审中-公开
标题翻译：新型二氮杂双环苯基衍生物及其医药用途
公开(公告)号：US20110257161A1
公开(公告)日：2011-10-20
申请号：US13132366
申请日：2009-12-03
申请人： Dan Peters , Daniel B. Timmermann , Elsebet ?stergaard Nielsen , Jeppe Kejser Christensen , Tino Dyhring
发明人： Dan Peters , Daniel B. Timmermann , Elsebet ?stergaard Nielsen , Jeppe Kejser Christensen , Tino Dyhring
IPC分类号： A61K31/551 , A61P25/28 , A61P25/18 , A61P25/24 , A61P25/00 , A61P3/04 , A61P25/16 , A61P25/14 , A61P25/22 , A61P25/08 , A61P25/02 , A61P9/10 , A61P15/06 , A61P1/12 , A61P11/06 , A61P15/10 , A61P29/00 , A61P17/10 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , C07D487/04
CPC分类号： C07D471/08
摘要： This invention relates to novel diazabicyclononyl-phenyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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壬基苯基衍生物及其在制备药物组合物中的用途。发现本发明的化合物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。

40. 发明授权

US08946412B2 Diazabicyclononyl oxadiazole compounds and their use as nicotinic acetylcholine receptor modulators 有权
标题翻译：二氮杂双环壬基恶二唑化合物及其作为烟碱乙酰胆碱受体调节剂的用途
公开(公告)号：US08946412B2
公开(公告)日：2015-02-03
申请号：US13516350
申请日：2010-12-16
申请人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Tino Dyhring , Philip K. Ahring
发明人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Tino Dyhring , Philip K. Ahring
IPC分类号： A61K31/551 , A61K51/04 , C07D471/08
CPC分类号： C07D471/08 , A61K51/0468
摘要： This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. 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. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.
摘要翻译：本发明涉及二氮杂双环壬基恶二唑基衍生物，其被发现是烟碱乙酰胆碱受体的调节剂。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。 Ar1表示吡咯基，任选被烷基或卤代烷基取代。

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