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1.发明申请公开(公告)号：US20110275684A1
公开(公告)日：2011-11-10
申请号：US13144884
申请日：2010-01-18
IPC分类号： A61K31/4192 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/16 , A61P25/14 , A61P25/24 , A61P25/18 , A61P3/00 , A61P3/04 , A61P25/02 , A61P9/12 , A61P9/06 , A61P9/10 , A61P15/06 , A61P1/12 , A61P11/06 , A61P15/00 , A61P15/10 , A61P5/14 , A61P5/00 , A61P25/06 , A61P29/00 , A61P17/00 , A61P17/10 , A61P1/00 , A61P1/04 , A61P25/30 , A61P25/36 , A61P25/32 , C07D249/18
CPC分类号： C07D249/18 , C07D403/06
摘要： The present invention relates to novel benzotriazole derivatives, efficacious in animal models of CNS disorders and, as such, valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders. In other aspects the invention relates to pharmaceutical compositions comprising the benzotriazole derivatives of the invention and to the use of these compounds for therapeutic applications.
摘要翻译： 本发明涉及新的苯并三唑衍生物，其在中枢神经系统疾病的动物模型中是有效的，因此是预防或治疗CNS（中枢神经系统）疾病或病症的有价值的候选物。 在其他方面，本发明涉及包含本发明的苯并三唑衍生物的药物组合物以及这些化合物在治疗应用中的用途。
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2.发明申请NOVEL DIPHENYL PURINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开新型二苯基衍生物有用作为非丁基乙酰胆碱受体的调节剂公开(公告)号：US20110269778A1
公开(公告)日：2011-11-03
申请号：US13123259
申请日：2009-10-08
IPC分类号： A61K31/52 , C07D487/04 , A61K31/522 , A61K31/519 , A61P25/22 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/24 , A61P25/18 , A61P3/04 , A61P25/14 , A61P25/08 , A61P11/06 , A61P17/00 , A61P25/06 , A61P25/30 , A61P1/00 , C07D473/00
CPC分类号： C07D487/04
摘要： This invention relates to novel (6-phenyl-5-amino/nitro-pyrimidin-4-yl)-phenyl-amines, 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： 本发明涉及被发现是烟碱乙酰胆碱受体调节剂的新的（6-苯基-5-氨基/硝基 - 嘧啶-4-基） - 苯基胺。 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NOVEL DIPHENYL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开新型二苯基-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
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。
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4.发明申请N-ACYLHYDRAZONE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 有权N-乙酰胆碱衍生物有用作为非线性乙酰胆碱受体的调节剂公开(公告)号：US20100280092A1
公开(公告)日：2010-11-04
申请号：US12743836
申请日：2008-11-19
IPC分类号： A61K31/405 , C07D209/20 , A61P25/00 , A61P25/28 , A61P25/24 , A61P25/22 , A61P9/12 , A61P9/06 , A61P29/00 , A61P25/30
CPC分类号： C07D209/18 , C07D209/30 , C07D409/12
摘要： This invention relates to N-acylhydrazone derivatives, which are found to be useful as 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N-酰腙衍生物，其被发现可用作烟碱型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病症多种多样 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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5.发明申请NOVEL PHENYL-QUINOLINE-CARBOXYLIC ACID PYRIDINE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开新型苯基喹啉 - 羧酸吡啶衍生物有用作为非线性乙酰胆碱受体的调节剂公开(公告)号：US20110207773A1
公开(公告)日：2011-08-25
申请号：US13059799
申请日：2009-08-20
IPC分类号： A61K31/4709 , C07D401/12 , C07D405/14 , A61P25/00 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/24 , A61P25/18 , A61P3/04 , A61P25/20 , A61P25/02 , A61P25/14 , A61P25/08 , A61P15/00 , A61P9/12 , A61P9/06 , A61P21/00 , A61P1/12 , A61P11/06 , A61P5/00 , A61P25/04 , A61P29/00 , A61P17/00 , A61P17/10 , A61P25/30 , A61P25/36
CPC分类号： C07D401/12
摘要： This invention relates to novel phenyl-quinoline-carboxylic acid pyridine 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： 本发明涉及新的苯基 - 喹啉羧酸吡啶衍生物，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病症多种多样 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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6.发明申请NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开新型三肽衍生物有用作为非线性乙酰胆碱受体的调节剂公开(公告)号：US20110105543A1
公开(公告)日：2011-05-05
申请号：US12922007
申请日：2009-03-09
IPC分类号： A61K31/505 , C07D239/42 , C07C217/80 , C07C215/74 , C07D403/10 , C07D239/30 , C07D405/10 , C07D239/48 , C07D237/20 , C07D213/73 , C07D401/10 , C07D209/08 , C07C309/01 , A61K31/136 , A61K31/506 , A61K31/50 , A61K31/44 , A61K31/4439 , A61K31/404 , A61K31/185 , A61P25/22 , A61P25/28 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P3/00 , A61P3/04 , A61P25/20 , A61P25/08 , A61P15/00 , A61P9/12 , A61P9/06 , A61P43/00 , A61P1/12 , A61P5/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P17/00 , A61P25/30 , A61P25/36 , A61P25/34
CPC分类号： C07D209/08 , C07C215/74 , C07C217/80 , C07C309/48 , C07D213/72 , C07D237/20 , C07D239/30 , C07D239/42 , C07D239/48
摘要： This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R1, R2, R3, R4 and R5. independently of each other, represent hydrogen, halo, tri-fluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkoxy, alkyl, amino or sulfamoyl; or R1 and R2, together with the phenyl ring to which they are attached form an indolyl ring or a benzo-dioxolyl ring; and R3, R4 and R5 are as defined above; and R6 represents amino or nitro, 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： 本发明涉及新的三芳基衍生物，式（I），其立体异构体或其立体异构体的混合物或其药学上可接受的盐，其中X，Y和Z全部代表CH; 或X，Y和Z中的一个或二个表示N; X，Y和Z的其他基团表示CH; 和R1，R2，R3，R4和R5。 代表氢，卤素，三氟甲基，三氟甲氧基，氰基，羟基，烷氧基，烷基，氨基或氨磺酰基; 或R 1和R 2与它们所连接的苯环一起形成吲哚基环或苯并二氧杂环基; R3，R4和R5如上定义; 并且R6表示氨基或硝基，其被发现是烟碱型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。
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7.发明申请6-PHENYL-PYRIMIDIN-4-YL-(PHENYLAMINE OR PHENOXY) DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开6-苯基 - 吡啶基-4-YL-（苯胺或苯氧基）衍生物作为非丁基乙酰胆碱受体的调节剂有用公开(公告)号：US20110230485A1
公开(公告)日：2011-09-22
申请号：US13122983
申请日：2009-10-09
IPC分类号： A61K31/5377 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D239/47 , C07D413/12 , A61K31/505 , A61K31/506 , A61P25/22 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/24 , A61P25/18 , A61P3/04 , A61P25/20 , A61P25/14 , A61P25/08 , A61P43/00 , A61P9/12 , A61P9/06 , A61P21/00 , A61P1/12 , A61P11/06 , A61P15/00 , A61P5/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P17/00 , A61P17/10 , A61P25/30 , A61P25/36
CPC分类号： C07D239/34 , C07D239/42 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention relates to novel 6-phenyl-phymidin-4-yl-(phenylannine or phenoxy) 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： 本发明涉及被发现是烟碱型乙酰胆碱受体的调节剂的新的6-苯基 - 吩啶-4-基 - （苯基苯胺或苯氧基）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。
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8.发明申请NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 审中-公开新的1,2,3-三唑衍生物有用作为非线性乙酰胆碱受体的调节剂公开(公告)号：US20110060017A1
公开(公告)日：2011-03-10
申请号：US12921995
申请日：2009-03-09
IPC分类号： A61K31/4192 , C07D249/04 , A61P25/00 , A61P25/20 , A61P25/16 , A61P25/28 , A61P25/24 , A61P25/18 , A61P21/00 , A61P25/30 , A61P29/00 , A61P15/00 , A61P3/10 , A61P1/00
CPC分类号： C07D249/06
摘要： This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetyl-choline 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1,2,3-三唑衍生物，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），疾病或病症的胆碱能系统有关的疾病或病症多种多样 与平滑肌收缩，内分泌疾病或病症有关的疾病或疾病，与由于终止化学物质的滥用而引起的炎症，疼痛和戒断症状相关的神经变性疾病或病症。
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9.发明申请NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS 失效新的1,2,3-三唑衍生物有用作为非线性乙酰胆碱受体的调节剂公开(公告)号：US20100222398A1
公开(公告)日：2010-09-02
申请号：US12672252
申请日：2008-08-06
IPC分类号： A61K31/4245 , C07D249/06 , A61K31/4192 , A61P25/22 , A61P25/16 , A61P25/28 , A61P25/18 , A61P25/24 , A61P3/04 , A61P25/14 , A61P9/12 , A61P9/06 , A61P25/08 , A61P11/06 , A61P1/12 , A61P15/10 , A61P15/12 , A61P25/06 , A61P25/02 , A61P25/34 , A61P25/36 , A61P25/32 , C07D413/04 , A61K31/422 , C07D413/10
CPC分类号： C07D249/06 , C07D413/04
摘要： This invention relates to novel 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。
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10.发明授权1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors 失效1,2,3-三唑衍生物可用作烟碱乙酰胆碱受体的调节剂公开(公告)号：US08110588B2
公开(公告)日：2012-02-07
申请号：US12672252
申请日：2008-08-06
IPC分类号： C07D413/10 , C07D249/06 , A61K31/4192 , A61K31/4245
CPC分类号： C07D249/06 , C07D413/04
摘要： This invention relates to novel 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。
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