New N-azabicyclooctyl bicyclic heteroaryl carboxamides, are alpha 7-nicotinic acetylcholine receptor ligands useful for improving attention, concentration, learning and/or memory performance

摘要

N-Azabicyclo-(2.2.2)-octyl benzo- or pyrido-furan- or -thiophene-2-carboxamides (I) are new. Azabicyclooctyl-amides of formula (I) and their salts, solvates and solvated salts are new. R1 = 1-aza-bicyclo-(2.2.2)-octyl (optionally substituted (os) at the N by 1-4C alkyl, benzyl or oxy); R2 = H or T; R3 = H, halo or T; R4 = H, halo, CN, NH2, CF3, OCF3, T, COT, NHT, CHO, COOH, OT, COOT, ST, NHCOT, CONHT, 1-4C alkylsulfonylamino, 3-8C cycloalkylcarbonylamino, 3-6C cycloalkylaminocarbonyl, pyrrolyl, NHCONHT, heterocyclylcarbonyl, heterocyclylcarbonylamino, heteroarylcarbonylamino, OH, phenyl or heterocyclyl (where T is os by OH, CN, NH2, NHCONHT, CONHT, heterocyclyl or aryl; CONHT is os by OT or NHT; NHCOT is os by OT; and heterocyclyl is os by =O); A = O or S; ring B = benzo or pyrido (both os by one or more of halo, CN, CHO, CF3, OCF3, NO2, NH2, T or OT); E = -CC-; or arylene or heteroarylene (both os by one or more of halo, CN, CF3, OCF3, NO2, NH2, OT or T); T = 1-6C alkyl. An Independent claim is included for the preparation of (I).