PEPTIDE DERIVATIVES OR THEIR SALTS, PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

FIELD: chemistry of peptides. SUBSTANCE: invention proposes peptide derivatives of the general formula (I): R₁R₂-N-CH(X)CO-A-B-D-(E)_u-(F)_v-(G)_w-K where R¹ is AlkO, (lower)-Alk, FAlk, cyclo-Alk, aminosulfonyl being the latter can be substituted with Alk, OH or NR³R⁴ where each R³ and R⁴ can be hydrogen or alkyl; R² - hydrogen, Alk, FAlk, cyclo-Alk; R¹ and R² together form 5-membered heterocycle; A is a residue of amino acid taken from: Val, Ile, Leu, allo-Ile, α-aminoisobutanoyl, 3-tert.-butyl-Ala, 2-tert. -butyl-Gly, 3-cyclohexyl-Ala, 2-ethyl-Gly, 2-cyclohexyl-Gly, Nle, NVal; B is a residue: N-Alk-Val, NVal, Leu, Ile, 2-tert.-butyl-Gly, 3-tert. -butyl-Ala, 3-cyclohexyl-Ala, Phe, 2-cyclohexyl-Gly; D, E, F and G are taken independently from group containing: Pro, homo-Pro, hydroxy-Pro, thiazolidinyl-4-carbonyl, 1-aminopentyl-1-carbonyl, Val, 2-tert.-butyl-Gly, Ile, Leu, 2-cyclohexyl-Ala, Phe, N-methyl-Phe, tetrahydroisoquinolyl-2-carbonyl, 3-thiazolyl-Ala, 3-thienyl-Ala, His, 1-aminoindolyl-1-carbonyl, Arg, 3-pyridyl-Ala, 3-tert.-butyl-Ala, 2-cyclohexyl-Gly, NVal, NLeu and 3-naphthyl-Ala; x is hydrogen, alkyl, cycloalkyl, -CH₂-cyclohexyl or arylalkyl; E and F together form five-membered heterocyclic ring containing nitrogen and/or oxygen, sulfur; u, v and w are similar and mean independently 0 or 1; K is OH, AlkO, phenoxy, benxyloxy, substituted of free amino-group, or their salts with physiologically compatible acids, and pharmaceutical composition containing a carrier and an active component of the formula (I) taken at effective amount. Synthesized peptides is used in medicine since they provide potentially improved therapeutic effectiveness for neoplastic diseases treatment. EFFECT: improved method of synthesis of new peptides indicated above, enhanced effectiveness of peptides. 10 cl, 2 ex, 4 tbl, 3 dwg