Triazoles as Farnesyl Transferase Inhibitors

摘要

a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L¹ and L² are R¹-Y- wherein each (R¹-Y)- substituent is defined independently of the other; Y is C_1-4alkanediyl, C_2-4alkenediyl, C_2-4alkynediyl, C(-O), or a direct bond; R¹ is hydrogen, cyano, aryl or a substituted or unsubstituted C_1-14heterocycle; =Z¹-Z²=Z³- represents a radical of formula -N-N-CH- (a-1), -N-CH-N- (a-2), -CH-N-N- (a-3); X is SO₂, (CH₂), wherein n is 1 to 4, C(-O), C(-S), or a direct bond; R² is aryl, C_3-7cycloalkyl, C_3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C_1-14heterocycle, C_3-7cycloalkyl, hydroxycarbonyl, C_1-6alkyloxycarbonyl, hydroxyC_1-6alkyl, hydroxyC_1-6alkyloxy, hydroxyC_1-6alkylthio and arylC_1-6alkylthio, C_1-12alkyl or C_1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C_1-14heterocycle, C_3-7cycloalkyl, hydroxycarbonyl, C_1-6alkyloxycarbonyl, hydroxyC_1-6alkyl, hydroxyC_1-6alkyloxy, hydroxyC_1-6alkylthio and arylC_1-6alkylthio; R³ is aryl, -NR⁵R⁶, a substituted or unsubstituted C_1-14heterocycle, or C_2-4alkenediyl substituted with a substituted or unsubstituted C_1-14heterocycle or aryl; R⁴ is hydrogen, aryl, C_3-7cycloalkyl, C_1-6alkyl or C_1-6alkyl substituted with C_3-7cycloalkyl, hydroxycarbonyl, C_1-4alkyloxycarbonyl or aryl; R⁵ and R⁶ are each independently selected from hydrogen, a substituted or unsubstituted C_1-14heterocycle, aryl, C_1-12alkyl and C_1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C_1-14heterocycle.