LHRH ANTAGONISTS, THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND ITS PREPARING, METHOD FOR TREATMENT OF TUMOR AND INFERTILITY IN MAMMALS Russian patent published in 2005 - IPC

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-[ε-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