LHRH ANTAGONISTS, THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND ITS PREPARING, METHOD FOR TREATMENT OF TUMOR AND INFERTILITY IN MAMMALS

摘要

FIELD: chemistry of peptides, hormones, medicine. ^ SUBSTANCE: invention relates to LHRH antagonists - decapeptides of the general formula (I): AXxx1-Xxx2-Xxx3-Xxx4-Xxx5-Xxx6-Xxx7-Xxx8-Xxx9-Xxx10-NH2 wherein A means acetyl group; Xxx1 is D-Nal(2); Xxx2 is D-Cpa; Xxx3 is D-Pal(3); Xxx4 is Ser; Xxx5 is N-Me-Tyr; Xxx6 means D-Cit, D-Hei, D-[epsilon-N1-4-(4-amidinophenyl)amino-1,4-dioxobutyl]-Lys-[D-Lys(B)]; Xxx7 means Leu, Nle; Xxx8 is Arg, Lys(iPr); Xxx9 means Pro; Xxx10 means D-Ala or Ser under condition that if Xxx6 means D-Lys(B) then Xxx7 means Nle; if Xxx6 means D-Cit then Xxx7 means Nle and Xxx10 means D-Ala; or if Xxx6 means D-Hci then Xxx7 means Leu, and Xxx10 means D-Ala. Also, invention relates to their salts with pharmaceutically acceptable acids, pharmaceutical composition, to a method for preparing pharmaceutical composition, a method for treatment of hormone-dependent tumors in mammals. Compounds show enhanced water-solubility property. ^ EFFECT: improved preparing method and treatment, valuable medicinal properties of compounds. ^ 16 cl, 2 tbl, 8 ex