ANALOGS OF LHRH ANTAGONISTS AND METHODS OF THEIR SYNTHESIS Russian patent published in 1998 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to new antagonists of LHRH of the formula: or or . New antagonists of LHRH of the formula: where DNal is DArAla where Ar is ; AA² is DarAla where Ar is ; AA³ is DArAla where Ar is or D -X--Ala where X is ; AA⁵ is Arg, Tyr or DArAla where Ar is or D-X--Ala where X is ; R¹ and R² are CH₃,CH₃CH₂,C₃H₇,C₄H₉; AA⁶ is DArPhe where Ar is or D-X--Ala where X is or NR¹R² where R¹ and R² are CH₃,CH₃CH₂;; AA⁸ is Arg or DArAla where Ar is or X is X--Ala where X is or NR¹R² where R¹,R² is CH₃,CH₃CH₂,C₃H₇,C₄H₉. These new peptides can be used for treatment of patients with endocrine system sicknesses, cancer and as male and female contraceptives. Invention involves also a method of synthesis of LHRH antagonists. Method involves addition reaction of C-terminal N-protected amino acid to benzhydrolylamine resin, protective group splitting off followed by peptide chain splicing at sequence corresponding to peptide of the formula (IV) under conditions of solid-phase synthesis. Peptide is split off from peptidylpolymer synthesized. Synthesized peptides have value properties, stimulate histamine decreased secretion and can be used in clinical practice. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 3 cl, 6 dwg, 4 tbl