ANTIMITOTIC AMIDES FOR TREATING CANCER AND PROLIFERATIVE DISEASES Russian patent published in 2020 - IPC C07D401/14 C07D401/12 C07D405/14 C07D409/14 A61K31/444 A61K31/506 A61P35/00 

FIELD: chemistry.

SUBSTANCE: disclosed is a compound of formula II

where: X¹ - CR⁷; X² is selected from a group comprising N and CR¹⁰; each of R¹, R³ and R⁴ is independently selected from a group comprising -H, halogens, substituted or unsubstituted alkyls with 1–8 carbon atoms, unsubstituted cycloalkyls with 3–6 carbon atoms, -C(O)NR^AR^B, -OR^A, -NR^AR^B, -S(O)₂R^A, unsubstituted phenyl and substituted or unsubstituted oxetane or piperazine; R2 is independently selected from a group comprising -H, halogens, substituted or unsubstituted alkyls with 1–8 carbon atoms, unsubstituted cycloalkyls with 3–6 carbon atoms, -C(O)NR^AR^B, -OR^A, -NR^AR^B, -S(O)₂R^A, substituted or unsubstituted phenyl and unsubstituted oxetane or piperazine; each of R⁷, R¹⁰ and R¹¹ is independently selected from a group comprising -H and unsubstituted alkyls with 1–8 carbon atoms; each of R⁵ and R⁶ is independently selected from a group comprising -H, halogens and unsubstituted alkyls with 1–8 carbon atoms; each of R⁸ and R⁹ is independently selected from a group comprising -H and halogens; each of R^A and R^B in the presence of independently selected from a group comprising -H, halogens, substituted or unsubstituted alkyls with 1–8 carbon atoms, substituted or unsubstituted cycloalkyls with 3–6 carbon atoms; in those cases, when for X¹ N is selected, as X² CH is selected, and as each of radicals R¹, R², R³, R⁴, R⁸, R⁹ and R¹¹ selected is hydrogen, substitutes for substituted alkyl are independently selected from amino, alkylamino, alkoxy, alkylsulfanyl, oxo (= O), halo, acyl, nitro, hydroxyl, cyano, thione (= S) and imino; substitutes for substituted cycloalkyl are independently selected from halogen and unsubstituted alkyl with 1–8 carbon atoms, or pharmaceutically acceptable salt for inhibition of tubulin activity.

EFFECT: disclosed are antimitotic amides for treating cancer and proliferative diseases.

40 cl, 4 tbl