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11. 发明申请

US20110201656A1 NOVEL DIPHENYL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：新型二苯基-1,2,3-三唑衍生物作为非线性乙酰胆碱受体的调节剂有用
公开(公告)号：US20110201656A1
公开(公告)日：2011-08-18
申请号：US13057957
申请日：2009-08-03
申请人： Antonio Nardi , Jeppe Kejser Christensen , Dan Peters
发明人： Antonio Nardi , Jeppe Kejser Christensen , Dan Peters
IPC分类号： A61K31/4192 , C07D249/06 , A61P25/00 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/24 , A61P25/18 , A61P3/04 , A61P25/20 , A61P25/02 , A61P25/08 , A61P9/12 , A61P9/06 , A61P21/00 , A61P1/12 , A61P11/06 , A61P15/00 , A61P5/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P17/00 , A61P17/10 , A61P25/36 , A61P25/30
CPC分类号： C07D249/06
摘要： This invention relates to novel diphenyl 1,2,3-triazole 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.
摘要翻译：本发明涉及新的二苯基1,2,3-三唑衍生物，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。

12. 发明授权

US07989470B2 3,8-substituted 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 失效
标题翻译： 3,8-取代的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：US07989470B2
公开(公告)日：2011-08-02
申请号：US12727972
申请日：2010-03-19
申请人： Dan Peters , Bjarne H. Dahl , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Jorgen Scheel-Kruger , John Paul Redrobe
发明人： Dan Peters , Bjarne H. Dahl , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Jorgen Scheel-Kruger , John Paul Redrobe
IPC分类号： A61K31/46 , C07D451/02
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。

13. 发明申请

US20110183995A1 ELTOPRAZINE FOR SUPPRESSION OF L-DOPA INDUCED DYSKINESIAS 审中-公开
标题翻译：用于抑制L-多巴诱导的DYSKINESIAS的ELTOPRAZZA
公开(公告)号：US20110183995A1
公开(公告)日：2011-07-28
申请号：US13001058
申请日：2009-06-23
申请人： Anders Björklund , Munolo Carta , Jørgen Buus Lassen
发明人： Anders Björklund , Munolo Carta , Jørgen Buus Lassen
IPC分类号： A61K31/496 , C07D403/10 , A61P25/16
CPC分类号： A61K31/496 , A61K31/198 , A61K2300/00
摘要： This invention relates to the use of the drug Eltoprazine for combating dyskinesias arising from chronic Levodopa (L-DOPA) therapy in patients suffering from Parkinson's disease.
摘要翻译：本发明涉及药物Eltoprazine在患有帕金森病的患者中对抗慢性左旋多巴（L-DOPA）治疗引起的运动障碍的用途。

14. 发明授权

US07985761B2 Diphenylurea derivatives and their use as chloride channel blockers or BKCa channel modulators 失效
标题翻译：二苯基脲衍生物及其作为氯化物通道阻断剂或BKCa通道调节剂的用途
公开(公告)号：US07985761B2
公开(公告)日：2011-07-26
申请号：US12280490
申请日：2007-03-09
申请人： Bjarne H. Dahl , Palle Christophersen , Lars Siim Madsen
发明人： Bjarne H. Dahl , Palle Christophersen , Lars Siim Madsen
IPC分类号： A61K31/4245 , C07D271/07
CPC分类号： C07D271/07
摘要： The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers or BKCa channel modulators.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：本发明涉及可用作氯化物通道阻断剂或BKCa通道调节剂的新型二苯基脲衍生物。在其他方面，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。

15. 发明授权

US07960561B2 2-(phenylamino) benzimidazole derivatives and their use as modulators of small-conductance calcium-activated potassium channels 有权
标题翻译： 2-（苯基氨基）苯并咪唑衍生物及其作为小电导钙激活钾通道的调节剂的用途
公开(公告)号：US07960561B2
公开(公告)日：2011-06-14
申请号：US11919708
申请日：2006-06-21
申请人： Ulrik Svane Sørensen , Lene Teuber , Dan Peters , Dorte Strøbæk , Tina Holm Johansen , Karin Sandager Nielsen , Palle Christophersen
发明人： Ulrik Svane Sørensen , Lene Teuber , Dan Peters , Dorte Strøbæk , Tina Holm Johansen , Karin Sandager Nielsen , Palle Christophersen
IPC分类号： A61K31/4184 , C07D235/30
CPC分类号： C07D235/30
摘要： This invention relates to novel 2-(phenylamino)benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels).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：本发明涉及可用作小电导钙激活钾通道（SK通道）的调节剂的新型2-（苯基氨基）苯并咪唑衍生物。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。

16. 发明授权

US07943630B2 3,9-diaza-spiro[5.5]undecane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 失效
标题翻译： 3,9-二氮杂螺[5.5]十一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：US07943630B2
公开(公告)日：2011-05-17
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： A01N43/42 , A61K31/44 , C07D211/00 , C07D213/00 , C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00
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。

17. 发明授权

US07939556B2 Imidazole derivatives and their use for modulating the GABAA receptor complex 失效
标题翻译：咪唑衍生物及其用于调节GABA A受体复合物的用途
公开(公告)号：US07939556B2
公开(公告)日：2011-05-10
申请号：US12089883
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 Østergaard Nielsen
发明人： William Dalby Brown , Janus S. Larsen , Lene Teuber , David Tristram Brown , Philip K. Ahring , Naheed Mirza , Elsebet Østergaard Nielsen
IPC分类号： A61K31/415
CPC分类号： C07D233/90 , C07D401/10 , C07D401/12 , C07D403/12
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。

18. 发明申请

US20110105478A1 NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES USEFUL AS MODULATOR OF NICOTINIC ACETYLCHOLINE RECEPTORS 失效
标题翻译：新的1,4-二氮杂双环[3.2.2]有用的作为非线性乙酰胆碱受体的调节剂的NONYL OXADIAZOLYL衍生物
公开(公告)号：US20110105478A1
公开(公告)日：2011-05-05
申请号：US12921922
申请日：2009-03-09
申请人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Eva Dam Christoffersen
发明人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Eva Dam Christoffersen
IPC分类号： A61K31/551 , C07D487/08 , A61P25/00 , A61P25/28 , A61P25/24 , A61P25/18 , A61P3/04 , A61P25/16 , A61P29/00 , A61P1/00 , A61P11/06 , A61P17/10
CPC分类号： C07D471/08
摘要： This invention relates to novel N-oxides of a 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivative 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1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物的新型N-氧化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。

19. 发明申请

US20110085978A1 NOVEL QUINOLINYLAMIDE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE AND SEROTONIN RECEPTORS 审中-公开
标题翻译：新戊酰胺衍生物作为多巴胺和丝氨酸受体的调节剂有用
公开(公告)号：US20110085978A1
公开(公告)日：2011-04-14
申请号：US12922368
申请日：2009-03-13
申请人： Dan Peters , Lars Christian Rønn , Karin Sandager Nielsen , Jørgen Scheel-Krüger
发明人： Dan Peters , Lars Christian Rønn , Karin Sandager Nielsen , Jørgen Scheel-Krüger
IPC分类号： A61K49/00 , C07D401/12 , A61K31/496 , C07D401/14 , A61K31/4709 , A61K31/5513 , A61P25/18 , A61P25/00
CPC分类号： C07D215/38 , C07D401/12
摘要： This invention provides novel quinolinylamide derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.
摘要翻译：本发明提供具有医疗效用的新型喹啉基酰胺衍生物，特别是作为多巴胺和5-羟色胺受体的调节剂，优选为D3,5HT1A和5-HT2A受体亚型，特别可用于治疗神经精神障碍。精神分裂症

20. 发明申请

US20110053984A1 NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译：新型4-苄氧基 - 四氢吡啶衍生物及其作为单胺神经递质抑制剂的用途
公开(公告)号：US20110053984A1
公开(公告)日：2011-03-03
申请号：US12921030
申请日：2009-02-27
申请人： Dan Peters , John Paul Redrobe , Elsebet Østergaard Nielsen
发明人： Dan Peters , John Paul Redrobe , Elsebet Østergaard Nielsen
IPC分类号： A61K31/445 , C07D211/46 , A61P25/00 , A61P29/00 , A61P13/00 , A61P15/00
CPC分类号： C07D211/46
摘要： This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rb and Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo; R′, R″, R′″ and R″″ independent of each other represent C1-6-alkyl; and with the proviso that the compound is not 4-benzhydryloxy-1,2,2,6,6-pentamethyl-piperidine, 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：本发明涉及式（I）的新型4-二苯甲氧基 - 四烷基 - 哌啶衍生物，其任何立体异构体或其立体异构体的任何混合物或其N-氧化物或其药学上可接受的盐，其中R a表示氢或C 1 -6-烷基; Rb和Rc彼此独立地表示苯基，该苯基任选被一个或多个独立地选自卤素，三氟甲基，三氟甲氧基，氰基，C 1-6 - 烷氧基和亚甲基二氧基的取代基取代; R'，R“，R”“和R”“彼此独立地表示C 1-6 - 烷基; 并且条件是该化合物不是4-二苯甲基氧基-1,2,2,6,6-五甲基哌啶，其可用作单胺神经递质再摄取抑制剂。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。

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