SOMATOSTATIN RECEPTOR ANTAGONISTS Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry, peptide hormones. SUBSTANCE: invention describes novel compounds of the general formula (I): (R₁, R₂)A¹-A²-A³-A⁴-Lys-A⁶-A⁷-A⁸-R₃ where A¹ means D- or L-isomer of aromatic amino acid; A² means D-isomer taken among the group including Cys, Pen, aromatic amino acid or aliphatic amino acid; A³ means aromatic amino acid; A⁴ means D-Trp; A⁶ means Thr, Thr(Bzl), Gly, Ser or aliphatic amino acid; A⁷ means Cys, Pen or aromatic or aliphatic amino acid; A⁸ means D- or L-isomer taken among the group including Thr, Ser, aromatic amino acid or aliphatic amino acid; each of R₁ and R₂ means independently H or E, SO₂ or E, CO where E₁ means heterocycle, lower alkyl substituted by heterocycle with hydroxy-lower alkyl; R³ means NH₂ under condition that if A² is D-Cys or D-Pen and A⁷ is Cys or Pen then side chains A² and A⁷ are bound by disulfide bond; and if A¹ is p-HO₂-Phe, A² means D-Cys, A³ means Phe or Tyr, A⁶ means Thr or Val and A⁷ means Cys then A⁸ means β-Nal. new compounds are antagonists of somatostatin receptors and can be used for treatment of patients with diseases and disorders when activation of growth hormone or insulin secretion is necessary, for example, in methods of radiotreatment. EFFECT: new compounds indicated above, valuable medicinal properties. 19 cl, 1 tbl