DERIVATIVES OF AZAINDOL WITH A COMBINATION OF PARTIAL AGONISM OF THE NICOTINE RECEIVER OF ACETILCOLINE AND INHIBITION OF DOPAMINE REABSORTION.

摘要

Compounds derived from azaindole, characterized by the general formula (I): or a tautomer, stereoisomer, N-oxide, or a pharmacologically acceptable salt, hydrate or solvate, of any of the foregoing, wherein - X, Y and Z independently represent N or C, with the proviso that the ring contains at least one atom of N, and not more than 2, - m and n are independently or 0 (zero) or 1, with the proviso that when Y and Z represent carbon and X represents nitrogen, m is 0 (zero), - R2 and R3 independently represent hydrogen, halogen, (C1-3) alkyl, alkynyl (C1-3), NH-alkyl (C1-3), CF3, hydroxyl, alkyl (C1 -3) oxy or a piperidinyl, pyrrolidinyl, tetrahydropyridinyl, morpholinyl, azepanyl, 1-azabicyclo [2.2.2] octanyl or 1-aza-bicyclo [2.2.2] oct-2-enyl group, group that is unsubstituted or substituted with one or more substituents selected from halogen, (C1-3) alkyl, phenyl or benzyl, - R4, R5 and R6 independently represent hydrogen, halogen or, (C1-3) alkyl, (C2-3) alkynyl, CF3, NH (C1-3) alkyl, hydroxyl or (C1-3) alkyl oxy, with the proviso that R4 exists only when Y = C, and R5 only when Z = C, with the proviso that when X and Z are N, Y is C, R4 is Cl, R5 and R6 are H, myn are zero (0), and R2 is H, R3 is not iodine or 1 , 2,3,6-tetrahydropyridin-4-yl; with the proviso that when X is N, Y and Z are C, R4 is Cl, R5 is Br, R6 is H, m and n are zero (0), and R3 is H, R2 is not iodine or H; with the proviso that when X and Z are C, Y is N, R5 is hydroxy, R2, R4 and R6 are H, m and n are zero (0), R3 is not 1,2,3,6-tetrahydropyridin-4- With the condition that when X is N, Y and Z are C, myn are zero (0), R2, R3, R4 and R5 are H, R6 is not chlorine or fluorine, with the proviso that when X is N , Y and Z are C, myn are zero (0), R2, R3, R4 and R6 are H, R5 is not bromine, chlorine or fluorine, with the proviso that when X is N, Y and Z are C, m is 1, n is zero (0), R2, R4, R5 and R6 are H, R3 is not ethyl or morpholin-4-yl, with the proviso that when X is N, Y and Z are C, m and n are zero (0), R2, R4, R5 and R6 are H, R3 is not bromine, with the proviso that when X is N, Y and Z are C, m and n are zero (0), R2, R3, R5 and R6 are H, R4 is not chlorine, with the proviso that when X is N, Y and Z are C, m is zero (0), n is 1, R3, R4, R5 and R6 are H, R2 is not hydrogen or pyridine -4-yl, with the proviso that when X is N, Y and Z are C, m is zero (0), n is 1, R4, R5 and R6 are H, R3 is bromine, R2 it is not pyridin-4-yl, 2-methylpyridinyl-4-yl, -ethyl-pyridinyl-4-yl or morpholin-4-yl.