Preparation of novel aminopyridines having Aurora A selective inhibitory action.

Abstract

The title compds. I [R1, R2 = H, lower alkyl, or alternatively R1 and R2 are combined together to form CH2; R3 = halo; R4 = halo or Me substituted with 1-3 halogen atoms; X = CH, N; W = (un)substituted thiazolyl, pyrazolyl, thiadiazolyl; with the proviso] which are Aurora A selective inhibitors useful in combination therapy of cancer, were prepd. E.g., a multi-step synthesis of I [R1, R2 = H; R3 = F; R4 = Cl; X = CH; W = 2-thiazolyl], starting from (6-bromopyridin-2-yl)methanol, was given (no characterization data provided for intermediates). The compds. I exhibit excellent Aurora A selective activity (biol. data were provided for exemplified compds. I). Pharmaceutical compns. comprising the compd. I alone or in combination with other antitumor agent(s) were disclosed. [on SciFinder(R)]