Azabicycloalkane derivatives, preparation thereof and use thereof in therapy

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.