PIPERAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of piperazine of the general formula (I) where R₁ and R₂ - hydrogen or C_1-8-alkyl or they are condensed to chain -(CH₂)_k where k = 3 or 4; R₃ - hydrogen, halogen, hydroxy-group, C_1-4-alkyl, phenyl lower alkoxy- or phenoxy-group or NR^xR^y where R^x and R^y - hydrogen, lower alkyl, C_2-4-unsaturated lower alkyl or benzyl; R₄ - hydrogen, halogen, hydroxy-group, trifluoromethyl, lower alkyl, lower alkoxy-, phenoxy- or lower alkoxy-group; R₅ - hydrogen, halogen, hydroxy-, nitro-group, lower alkyl, lower alkoxy-group, phenyl, acyl- or acyloxy-group; R₆ - H, halogen, lower alkyl, alkoxy-group or phenyl; R₇ - H, halogen or lower alkyl; or R₆ and R₇ together with carbon atoms to which they are bound form benzo- or naphtho-group; l = 0-7; m and n = 0 or 1; W - carbon or nitrogen; X - oxygen or sulfur; Y is NH or oxygen; Z - hydrogen, alkoxy-, phenoxy-, alkylamino-group, piperazinyl, boc-piperazinyl or oxo-group; or their pharmaceutically acceptable acid salts. Compounds of the formula (I) show high antitumor activity and very low toxicity. EFFECT: improved method of synthesis, enhanced properties. 3 cl, 6 tbl, 181 ex