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

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.