首页> 外国专利> New azabicycloalkyl pyridine derivatives useful as nicotinic receptor ligands, e.g. for treating cognitive dysfunction, attention deficit disorders and functional disorders associated with Alzheimer's disease

New azabicycloalkyl pyridine derivatives useful as nicotinic receptor ligands, e.g. for treating cognitive dysfunction, attention deficit disorders and functional disorders associated with Alzheimer's disease

机译:可用作烟碱样受体配体的新的氮杂双环烷基吡啶衍生物,例如用于治疗认知功能障碍,注意力缺陷障碍和与阿尔茨海默氏病相关的功能障碍

摘要

Azabicycloalkyl pyridine derivatives (I) are new. Azabicycloalkyl pyridine derivatives of formula (I) are new, except for 4-(6-X-3-pyridyl)-1-azabicyclo[2.2.1]heptanes. R : H, halo, OH, 1-6C alkoxy, 3-7C cycloalkoxy or (3-7C)cycloalkyl(1-3C)alkoxy, or heterocycloalkyl, aryl or heteroaryl optionally substituted with 1-6C alkyl, 3-7C cycloalkyl, (3-7C)cycloalkyl(1-3C)alkyl, 1-6C alkoxy, 3-7C cycloalkoxy or (3-7C)cycloalkyl(1-3C)alkoxy, 1-6C fluoroalkyl, 1-6C fluoroalkoxy, NO 2, CN, OH, NH 2, mono- or di(1-6C alkyl)amino, heterocycloalkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryloxy or 1-6C alkylcarbonyl; m, n, o= 1 or 2; X : H, F, Cl or Br. [Image] ACTIVITY : Nootropic; Tranquilizer; Neuroprotective; Antiparkinsonian; Neuroleptic; Antialcoholic; Vasotropic; Cerebroprotective; Antismoking; Antiaddictive; Analgesic; Cardiant; Vulnerary; Antiinflammatory. MECHANISM OF ACTION : Nicotinic receptor ligand. 4-(6-(3-(1-Pyrazolyl)phenyl)-3-pyridyl)-1-axabicyclo[2.2.1]heptane had an IC50 of 4.7 nM in a nicotinic receptor subunit alpha 7 binding assay.
机译:氮杂双环烷基吡啶衍生物(I)是新的。式(I)的氮杂双环烷基吡啶衍生物是新的,除了4-(6-X-3-吡啶基)-1-氮杂双环[2.2.1]庚烷。 R:H,卤素,OH,1-6C烷氧基,3-7C环烷氧基或(3-7C)环烷基(1-3C)烷氧基,或杂环烷基,芳基或杂芳基,可选地被1-6C烷基,3-7C环烷基取代, (3-7C)环烷基(1-3C)烷基,1-6C烷氧基,3-7C环烷氧基或(3-7C)环烷基(1-3C)烷氧基,1-6C氟烷基,1-6C氟烷氧基,NO 2,CN ,OH,NH 2,单或二(1-6C烷基)氨基,杂环烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳氧基或1-6C烷基羰基; m,n,o = 1或2; X:H,F,Cl或Br。活动:促智;镇静剂;具有神经保护作用;反帕金森病;抗精神病药;抗酒;变压性脑保护禁止吸烟;反吸毒止痛药卡迪恩伤药;消炎(药。作用机理:烟碱受体配体。在烟碱样受体亚基α7结合试验中,4-(6-(3-(1-(吡唑基)苯基)-3-吡啶基)-1-氮杂双环[2.2.1]庚烷的IC50为4.7 nM。

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