PEPTIDE DERIVATIVES OR THEIR SALTS, PHARMACEUTICAL COMPOSITION

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 R is AlkO, (lower)-Alk, FAlk, cyclo-Alk, aminosulfonyl being the latter can be substituted with Alk, OH or NR3R where each R and R can be hydrogen o...

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Hauptverfasser: FRANTS EHMLING, ANDREAS KHAUPT, SINTIJA ROMERDAL
Format: Patent
Sprache:eng
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Zusammenfassung: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 R is AlkO, (lower)-Alk, FAlk, cyclo-Alk, aminosulfonyl being the latter can be substituted with Alk, OH or NR3R where each R and R can be hydrogen or alkyl; R - hydrogen, Alk, FAlk, cyclo-Alk; R and R together form 5-membered heterocycle; A is a residue of amino acid taken from: Val, Ile, Leu, allo-Ile, alpha-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 dwgK