DERIVATIVES OF NONAPEPTIDES OR THEIR SALTS WITH PHARMACEUTICALLY ACCEPTABLE ACIDS, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

FIELD: chemistry of peptides, medicine. SUBSTANCE: derivatives of nonapeptides of the general formula (I): X-A₁-A₂-Trp-Ala-Val-Gly-His-Leu-psi TriQ where Q is OMe, NH₂; X is hydrogen, acetyl, CONH₂; A₁ is D- or L-Tpi, D-p-Glu; A₂ is Gln, Glu(OMe), Glu(MeNH), Glu, His(Bz) or the formula (II): D-Tpi-A₂-Trp-Ala-Val-Gly-His-Leu-psiA₉NH₂ where A₂ is Gln, Glu(OMe), His, His(Bz); A₉ is Leu, Phe, Trp, Trp(For) or their salts with pharmaceutically acceptable acids. Peptides are synthesized by step splicing of peptide chain. Amino-group at α-position is protected and terminal carboxy-group is bound covalently with synthetic polymeric carrier used for this purpose. Then α-protective group is split off, carboxy-group of the next amino acid is reduced to group HC=O and the latter is bound with the above mentioned α-amino-group deblocked preliminary. Then α-amino-protective group of this second amino acid is deblocked and carboxy-group of the next amino acid is bound with above mentioned deblocked α-amino-group of the second amino acid. Then other amino acid are bound to sequence corresponding the structural formula (I) or (II). From obtained peptidylpolymer carrier is split off and if necessary protective groups also. Obtained peptides if necessary are acetylated and the end product is isolated in free form or as a salt with pharmaceutically acceptable acid. Pharmaceutical composition has an active component (compound of the formula I) taken at effective dose and pharmaceutically acceptable carrier. Synthesized compounds show antagonistic activity with respect to bombazine and can be used in medicine for therapy of malignant diseases in animals and human. EFFECT: improved method of synthesis, enhanced effectiveness. 19 cl, 2 tbl, 6 ex