| 摘要 |
N-(Hetero)aryl-2-(N-(aminobenzyl)-amino)-benzamide and 2-amino-nicotinamide derivatives (I), including their enantiomers, diastereomers, tautomers and salts, are new. N-(Hetero)aryl-2-(N-(aminobenzyl)-amino)-benzamide and 2-amino-nicotinamide derivatives of formula (I), including their enantiomers, diastereomers, tautomers and salts, are new. X = CH or N; W = H or F; A1-A5 = CH or N, provided that not more than two are N; R1 = aryl or heteroaryl (both optionally substituted (os) by one or more of halo, OH, T, 3-6C cycloalkyl, 3-6C alkenyl, 2-6C alkynyl, aralkoxy, OT, haloalkyl, cyanoalkyl, =O, OR5 or SO2R6, where 1-6C alkyl groups are os by OR5 or NR9R10); T = 1-12C alkyl; Y, Y' = a bond, CO, CS or SO2; R2, R3 = H, CONR9R10, SO2R6, COR11, CO-alkyl, CO-alkyl-R11 or NR9R10, or alkyl, 3-10C cycloalkyl, 3-6C cycloalkenyl, aryl or heteroaryl (all os by one or more of halo, CN, T, OT, hydroxyalkyl, haloalkyl, NR7R8, OR5, alkyl-OR6, SR4, SOR4 or SO2R6); or N(YR2)Y'R3 = 3-8 membered (un)saturated ring, optionally containing further heteroatoms and os by one or more of halo, T, OT', haloalkyl, hydroxyalkyl, =O, OR5, SR4, SOR4 or SO2R6; T' = T or 1-12C haloalkyl; R4 = T, aryl or heteroaryl; R5 = H, T', 3-10C cycloalkyl or 3-6C halocycloalkyl; R6 = H, T' or NR9R10, or aryl or heteroaryl (both os by one or more of T, alkoxy, halo or haloalkoxy); R7, R8 = H or T; R9, R10 = H, alkyl, 2-6C alkenyl, aryl, 3-8C cycloalkyl or CONR7R8, or T (os by one or more of aryl (os by one or more of alkoxy or haloalkyl), morpholino, OH, halo, OT or NR7R8); or NR9R10 = 5-8 membered ring, optionally containing additional heteroatoms; and R11 = alkyl, alkoxy, hydroxyalkyl, hydroxyalkoxy, 3-6C cycloalkyl or phenyl (os by one or more of alkyl or haloalkyl), pyridyl, biphenylyl or naphthyl. Alkyl moieties have 1-6C unless specified otherwise. An Independent claim is also included for anthranilic and aminonicotinic acid derivatives of formulae (II) and (III) as intermediates in the preparation of (I). M = halo; Q = a leaving group (e.g. halo, O-triflate, O-mesylate, O-tosylate or sulfone) or N(YR2)Y'R3; and Ry = H or 1-6C alkyl. |
