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1. 发明授权

EP2121677B1 NOVEL CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 有权
公开(公告)号：EP2121677B1
公开(公告)日：2010-11-03
申请号：EP07857757.4
申请日：2007-12-18
申请人： NeuroSearch A/S
发明人： PETERS, Dan , REDROBE, John, Paul , OLSEN, Gunnar, M. , NIELSEN, Elsebet Østergaard
IPC分类号： C07D451/06 , A61K31/46 , A61P25/00
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.

2. 发明申请

WO2009098209A1 NOVEL 9-AZA-BICYCLO[3.3.1]NON-3-YLOXY CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译：新型9-氮杂双环[3.3.1]非3-氯乙烯-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：WO2009098209A1
公开(公告)日：2009-08-13
申请号：PCT/EP2009/051217
申请日：2009-02-04
申请人： NeuroSearch A/S , PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D451/14 , A61K31/439 , A61P25/24
CPC分类号： C07D451/14
摘要： This invention relates to novel 9-aza-bicyclo[3.3.1]non-3-yloxy 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9-氮杂 - 双环[3.3.1]壬-3-基氧基色烯-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。

3. 发明申请

WO2009109519A1 NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTATKE INHIBITORS 审中-公开
标题翻译：新型4-苄氧基 - 四氢吡啶并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：WO2009109519A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052333
申请日：2009-02-27
申请人： NeuroSearch A/S , PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D211/46 , A61K31/495
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 R a represents hydrogen or C 1-6 -alkyl; R b and R c 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, C 1-6 -alkoxy and methylenedioxo; R', R", R'" and R"" independent of each other represent C 1-6 -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，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。

4. 发明申请

WO2009109518A1 NOVEL 4-BENZHYDRYL-TETRAHYDRO-PYRIDINE 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：WO2009109518A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052331
申请日：2009-02-27
申请人： NeuroSearch A/S , PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D211/70 , A61K31/4409
CPC分类号： C07D211/70
摘要： This invention relates to novel 4-benzhydryl-tetrahydro-pyridine 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 R a represents hydrogen or C 1-6 -alkyl; R b and R c 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, C 1-6 -alkoxy and methylenedioxo 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4-二苯甲基 - 四氢 - 吡啶衍生物，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; Rband 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，可用作单胺神经递质，吸收抑制剂。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。

5. 发明申请

WO2009098208A1 NOVEL PHENYLETHYNYL DERIVATIVES OF 8-AZA-BICYCLO[3.2.1]OCTANE AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译： 8-AZA-BICYCLO [3.2.1] OCTAN的新型苯乙烯衍生物及其作为单胺神经递质抑制剂的用途
公开(公告)号：WO2009098208A1
公开(公告)日：2009-08-13
申请号：PCT/EP2009/051216
申请日：2009-02-04
申请人： NeuroSearch A/S , PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D451/06 , A61K31/46 , A61P25/00
CPC分类号： C07D451/06
摘要： This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1 ]octane 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8-氮杂 - 双环[3.2.1]辛烷的新型苯乙炔衍生物。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. 发明公开

EP2240476A1 NOVEL PHENYLETHYNYL DERIVATIVES OF 8-AZA-BICYCLO[3.2.1]OCTANE AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译： 8-氮杂二环[3.2.1]辛烷NEW PHENYLETHINYLDERIVATE及其作为单胺神经递质再摄取抑制剂
公开(公告)号：EP2240476A1
公开(公告)日：2010-10-20
申请号：EP09708474.3
申请日：2009-02-04
申请人： NeuroSearch A/S
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D451/06 , A61K31/46 , A61P25/00
CPC分类号： C07D451/06
摘要： This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1 ]octane 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.

7. 发明公开

EP2094655A1 NOVEL BIPHENYL THIO-UREA DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS 审中-公开
标题翻译：作为钾通道调节剂适合...新的联苯基硫脲
公开(公告)号：EP2094655A1
公开(公告)日：2009-09-02
申请号：EP07857650.1
申请日：2007-12-17
申请人： NeuroSearch A/S
发明人： NARDI, Antonio , DEMNITZ, Joachim , GRUNNET, Morten , CHRISTOPHERSEN, Palle , JONES, David Spencer , NIELSEN, Elsebet Østergaard , STRØBÆK, Dorte , MADSEN, Lars Siim
IPC分类号： C07C335/18 , C07D257/04 , A61K31/17 , A61P15/12
CPC分类号： C07D257/04 , A61K31/17 , A61K31/41 , A61K31/496 , A61K31/5025 , A61K31/53 , C07C335/18
摘要： The invention relates to novel biphenyl thio-urea derivatives of Formula (I), wherein A represents hydroxy or tetrazolyl; R1 represents halo, hydroxy or phenyl, which phenyl may optionally be substituted with halo; and R2 and R3, independent of each other, represent halo, trifluoromethyl, nitro and/or phenyl, that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of disease or disorders as diverse as those which are responsive to modulation of ion channels.

8. 发明授权

EP1877052B1 BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX 有权
标题翻译：苯并咪唑和它们用于调制GABAA受体复合物
公开(公告)号：EP1877052B1
公开(公告)日：2009-07-22
申请号：EP06725630.5
申请日：2006-04-07
申请人： NeuroSearch A/S
发明人： LARSEN, Janus S. , TEUBER, Lene , AHRING, Philip K. , NIELSEN, Elsebet Østergaard , MIRZA, Naheed
IPC分类号： A61K31/4184 , C07D401/10 , C07D403/10 , C07D417/10 , C07D417/14 , A61P25/00
CPC分类号： C07D403/10 , C07D401/10 , C07D417/10
摘要： This invention relates to novel benzimidazole derivatives of formula (I), 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 GABA receptor complex, and in particular for combating anxiety and related diseases.

9. 发明公开

EP2027122A1 NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONANE DERIVATIVES AND THEIR MEDICAL USE 有权
公开(公告)号：EP2027122A1
公开(公告)日：2009-02-25
申请号：EP07729315.7
申请日：2007-05-21
申请人： NeuroSearch A/S
发明人： PETERS, Dan , OLSEN, Gunnar M. , NIELSEN, Elsebet Østergaard , TIMMERMANN, Daniel, B. , LOECHEL, Steven, Charles , CHRISTENSEN, Jeppe, Kejser , DYHRING, Tino
IPC分类号： C07D471/08 , A61K31/551 , A61P25/00 , A61P25/28
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonane 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.

10. 发明公开

EP1984365A1 3,9-DIAZABICYCLO[3.3.1]NONANE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS 审中-公开
标题翻译： 3,9-二氮杂双环 - [3.3.1]壬烷衍生物及其作为单胺神经递质再摄取抑制剂
公开(公告)号：EP1984365A1
公开(公告)日：2008-10-29
申请号：EP07704485.7
申请日：2007-02-09
申请人： NeuroSearch A/S
发明人： PETERS, Dan , REDROBE, John Paul , NIELSEN, Elsebet Østergaard
IPC分类号： C07D471/08 , A61K31/4995 , A61P25/00
CPC分类号： C07D471/08
摘要： This invention relates to novel 3,9-diazabicyclo[3.3.1 ]nonane 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.

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