| 摘要 |
FIELD: chemistry of peptides, medicine, endocrinology. SUBSTANCE: invention relates to new antagonists of LHRH and complexes formed by these antagonists and VB12. In part, this invention relates to oral administration of antagonists of LHRH to patients. Antagonists are taken from a group consisting of ANTIDE-1, ANTIDE-2 and ANTI-3 that are suitable for conjugation with VB12, namely: N-Ac-D-Nal (2), D-Phe(pCl), D-Pal (3), Ser, Lys(Nic), D-Lys, Leu, Lys(iPr), Pro, O-Ala-NH<SB>2</SB> (D-Lys<SB>6</SB>-ANTIDE or ANTIDE-1), N-Ac-D-Nal (2), D-Phe(pCl), D-Pal (3), Ser, Lys, (Nic), D-Lys(Nic), Leu, Lys, Pro, D-Ala-NH<SB>2</SB> (Lys<SB>8</SB>-ANTIDE or ANTIDE-3). Invention relates to also a complex formed by VB12 or VB12 analog and antagonists of LHRH considered above. For intake and transport of VB12 in host-vertebrate the indicated VB12 or its analog must show capability to react by binding reaction where activity of antagonist of LHRH is retained at constant level mainly. Invention describes also a method of chemical castration and/or treatment of patients with gonadotropin-dependent disorders that involves administration of the above indicated compounds. EFFECT: improved method of treatment. 9 cl, 6 tbl, 6 ex
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