POLYMERIC CONJUGATE, A METHOD OF ITS SYNTHESIS AND A PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, polymers, peptides, medicine, pharmacy. SUBSTANCE: invention relates to a polymeric conjugate synthesized by interaction of compounds of the formula (II): where one of A₂ and A₃ means chemical bond and other means A; R means phenyl or t-butoxy-group; R₃ means hydrogen atom or acetyl-group; A means a simple chemical bond, an amino acid residue or peptide spacer taken from: β--Ala, Gly, Phe-Gly, Phe-Phe, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe, Gly--β--Ala, Phe-Gly--β--Ala, Phe-Phe--β--Ala, Leu-Gly--β--Ala, Val-Ala--β--Ala, Phe-Ala--β--Ala, Leu-Phe--β--Ala, Leu-Gly--β--Ala, Leu-Leu-Gly--β--Ala, Phe-Tyr-Ala-β--Ala, Phe-Gly-Phe-β--Ala, Phe-Phe-Gly-β--Ala, Phe-Leu-Gly-Phe-β--Ala or Gly-Phe-Leu-Gly-Phe-β--Ala which are interacted with an activated polymer consisting of 90-90.9 mole% links of the formula: and 10-0.1 mole% links of the formula: . Process is carried out in an anhydrous polar solvent at 15-40 C for 1-24 h in the presence of an organic or inorganic base followed by treatment of obtained conjugate with 2-hydroxypropylamine. Invention relates to a pharmaceutical composition showing an antitumor activity and containing a polymeric conjugate as an active component taken at effective amount. EFFECT: improved solubility, decreased toxicity of synthesized compounds as compared with that of paclitaxel. 7 cl, 2 tbl