BIOTIN DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF THEIR PREPARING Russian patent published in 2001 - IPC

FIELD: organic chemistry, vitamins, peptides. SUBSTANCE: invention describes novel biotin derivatives of the general formula (I) where Q is absent or means -NH-(CH₂)₅-CO-; R¹ means X-Arq-Gly-Asp-y; X is tripeptide: Gly-Gly-Gly-; y is dipeptide: -Ser-Pro- or R¹ means A-Cys-(R²)-B-U; R² means H, Trt; A means Asp or peptide fragment taken among the group consisting of: Ala-Asp; Thr-Ala- -Asp, Lys-Thr-Ala- Asp, Lys-Ala-Ala-Asp, Arq-Thr-Ala-Asp, Ser- -Ala-Asp, Gln-Ser-Ala-Asp, Gly-Lys-Thr-Ala- Asp, Ile-Ser-Ala- -Gly, Arq-Ser-Ala-Gly, Gly-Lys-Thr-Cys(Trt)-Asp; B is absent or means Pro or N-methylated derivative of Ala being if R¹ means A-Cys-(R²)-B-U then only one of residues A or B can absent; U means OH or NH_-2 or R¹ means cyclo-(Arq-Gly-Asp-Z); Z in side chain is bound with Q or if Q is absent with biotin; Z means di- or tripeptide residue. Amino acids are taken independently each of other among the group consisting of Ala, Val, Tyr, Trp, Phe, Cys, Lys, M and indicated amino acids can be derivatized and amino acid residues are bound with one another by peptide- -like bonds through N-amino- and α-carboxyl groups being M presents always and means: NH-(R⁸)-CH-(R³)-COOH; R³ is R⁶-R⁴ where R⁴ is OH; R⁶ is alkylenephenyl with 7-14 carbon atoms; R⁸ is H, alkyl with 1-6 carbon atoms. In the case of residues of optically active amino acids and amino acid derivatives both D- and L-forms and their salts can be included also. Invention describes also method of their synthesis, pharmaceutical compositions and method of their preparing. Compounds can be used as integrin inhibitors, in part, for prophylaxis and treatment of patients with diseases of circulation system, in thrombosis, heart infarctum, arteriosclerosis and in tumor therapy. EFFECT: new compounds indicated above, improved methods of synthesis and preparing, valuable medicinal properties. 5 cl, 1 tbl