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1.发明申请NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开新型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
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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![NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE](/abs-image/US/2010/12/02/US20100305108A1/abs.jpg.150x150.jpg)
2.发明申请NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE 审中-公开新的1,4-二氮杂双环[3.2.2]壬基吡啶衍生物及其医疗用途公开(公告)号：US20100305108A1
公开(公告)日：2010-12-02
申请号：US12742595
申请日：2008-11-13
申请人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser Christensen , John Paul Redrobe , Jens Damsgaard Mikkelsen
发明人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser Christensen , John Paul Redrobe , Jens Damsgaard Mikkelsen
IPC分类号： A61K31/551 , C07D471/08 , A61P25/00 , A61P25/18 , A61P25/24 , A61P3/04 , A61P25/28 , A61P25/22 , A61P25/30 , A61P29/00
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine 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1,4-二氮杂 - 双环[3.2.2]壬基嘧啶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。
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3.发明申请N-ARYL-N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THIER USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开N-ARYL-N-哌啶-4-甲酰胺衍生物，并用作单胺神经递质抑制剂公开(公告)号：US20100298380A1
公开(公告)日：2010-11-25
申请号：US12671592
申请日：2008-07-31
IPC分类号： A61K31/454 , C07D401/06 , A61P29/00 , A61P25/28 , A61P25/22 , A61P25/00 , A61P25/24 , A61P25/30 , A61P19/02 , A61P1/00 , A61P15/00 , A61P43/00 , A61P25/32 , A61P25/34
CPC分类号： C07D401/06
摘要： This invention relates to novel N-aryl-N-piperidin-4-ylmethyl amide 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N-芳基-N-哌啶-4-基甲基酰胺衍生物。 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。
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4.发明申请NOVEL CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 失效新颖的2-酮衍生物及其作为单胺神经递质抑制剂的用途公开(公告)号：US20100227883A1
公开(公告)日：2010-09-09
申请号：US12160403
申请日：2007-02-13
IPC分类号： A61K31/46 , C07D451/12 , C07D451/06 , A61P25/00 , A61P29/00 , A61P15/10 , A61P13/00
CPC分类号： C07D451/06
摘要： This invention relates to novel chromen-2-one 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色烯-2-酮衍生物。 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。
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5.发明授权Chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 失效色烯-2-酮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：US08263617B2
公开(公告)日：2012-09-11
申请号：US12520236
申请日：2007-12-18
IPC分类号： A61K31/439 , C07D451/00
CPC分类号： C07D451/06
摘要： This invention relates to novel chromen-2-one derivatives of Formula (I) 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： 本发明涉及用作单胺神经递质再摄取抑制剂的式（I）的新型色烯-2-酮衍生物。 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。
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6.发明申请AZABICYCLOOCTYL-QUINAZOLONE DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS 审中-公开适用于亚胺基胆碱受体调节剂的AZABICYCLOOCTYL-QUINAZOLONE衍生物公开(公告)号：US20110112119A1
公开(公告)日：2011-05-12
申请号：US12994243
申请日：2009-06-09
申请人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser Christensen , Philip K. Ahring , John Paul Redrobe , Jens Damsgaard Mikkelsen
发明人： Dan Peters , Daniel B. Timmermann , Elsebet Østergaard Nielsen , Gunnar M. Olsen , Tino Dyhring , Jeppe Kejser Christensen , Philip K. Ahring , John Paul Redrobe , Jens Damsgaard Mikkelsen
IPC分类号： C07D453/02 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/08 , A61P25/24 , A61P9/00 , A61P15/06 , A61P9/06 , A61P11/06 , A61P15/10 , A61P29/00 , A61P1/00 , A61P17/10 , A61P17/00 , A61P25/34 , A61P25/36 , A61P25/32 , A61P25/16
CPC分类号： C07D453/02
摘要： This invention relates to novel azabicyclooctyl-quinazolinone 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： 本发明涉及新的氮杂双环辛基 - 喹唑啉酮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。
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7.发明申请NOVEL PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开新型哌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：US20110046179A1
公开(公告)日：2011-02-24
申请号：US12377830
申请日：2007-08-29
申请人： Birgitte L. Eriksen , Dan Peters , Bjarne H. Dahl , Elsebet Østergaard Nielsen , John Paul Redrobe
发明人： Birgitte L. Eriksen , Dan Peters , Bjarne H. Dahl , Elsebet Østergaard Nielsen , John Paul Redrobe
IPC分类号： A61K31/445 , C07D211/62 , C07D211/22 , A61K31/4465 , A61P25/00 , A61P25/24 , A61P25/28 , A61P25/22 , A61P25/30 , A61P29/00 , A61P19/02 , A61P15/00 , A61P13/00
CPC分类号： C07D211/22
摘要： This invention relates to novel piperidine 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： 本发明涉及用作单胺神经递质再摄取抑制剂的新型哌啶衍生物。 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。
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8.发明申请4-PHENYL-PIPERAZIN-1-YL-ALKYL-BENZOIMIDAZOL-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE IN-HIBITORS 审中-公开4-苯基 - 哌嗪-1-基-L-烷基苯并咪唑-2-酮衍生物及其作为单胺神经递质重新获得抑制剂的用途公开(公告)号：US20110028490A1
公开(公告)日：2011-02-03
申请号：US12812272
申请日：2009-01-21
IPC分类号： A61K31/496 , C07D403/06 , C07D403/08 , A61P25/00 , A61P25/28 , A61P25/16 , A61P29/00 , A61P25/30 , A61P13/00 , A61P15/12 , A61P15/10
CPC分类号： C07D235/26
摘要： This invention relates to novel 4-phenyl-piperazin-1-yl-alkyl-benzoimidazol-2-one derivatives of structure (I) 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结构（I）的新型4-苯基 - 哌嗪-1-基 - 烷基 - 苯并咪唑-2-酮衍生物。 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。
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9.发明申请NOVEL CARBOXYLIC ACID 4-PHENYLAZO-PHENYL ESTER DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 失效新型羧酸4-苯甲酰苯酯衍生物及其作为单胺神经递质抑制剂的用途公开(公告)号：US20100311699A1
公开(公告)日：2010-12-09
申请号：US12745530
申请日：2008-11-27
IPC分类号： A61K31/655 , C07D471/08 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28 , A61P25/06
CPC分类号： C07D487/08 , C07D243/08 , C07D295/205 , C07D471/08
摘要： This invention relates to novel carboxylic acid 4-phenylazo-phenyl ester 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羧酸4-苯基偶氮苯基酯衍生物。 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。
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10.发明申请NOVEL BENZOOXAZOL-AND BENZOOXATHIOL-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开新型苯并恶唑和苯并恶唑-2-酮衍生物及其作为单胺神经递质抑制剂的用途公开(公告)号：US20100286195A1
公开(公告)日：2010-11-11
申请号：US12677077
申请日：2008-09-08
IPC分类号： A61K31/439 , C07D453/02 , A61P25/24 , A61P25/16 , A61P25/28 , A61P25/36 , A61P25/32 , A61P35/00 , A61P1/00 , A61P19/02 , A61P3/04 , A61P25/14
CPC分类号： C07D411/12 , C07D413/12
摘要： This invention relates to novel benzooxazol- and benzooxathiol-2-one 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苯并恶唑和苯甲酰硫醇-2-酮衍生物。 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。
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