LHRH ANTAGONISTS AND METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION, METHOD FOR PREPARING MEDICINAL AGENT Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to LHRH antagonists representing compounds of the general formula (I): A-Xxx¹-Xxx²-Xxx³-Xxx⁴-Xxx⁵-Xxx⁶-Xxx⁷-Xxx⁸-Xxx⁹-Xxx¹⁰-NH₂ (I) wherein A means acetyl or 3-(4-fluorophenyl)propionyl group; Xxx¹ means D-Nal(1) or D-Nal(2); Xxx²-Xxx³ means D-Cpa-D-Pal(3) or a simple bond; Xxx⁴ means Ser; Xxx⁵ means N-Me-Tyr; Xxx⁶ means D-Hci or residue of D-amino acid of the general formula (II): wherein n means a number 3 or 4; R¹ means a group of the general formula (III): (III) wherein p means a whole number from 1 to 4; R² means hydrogen atom or alkyl group; R³ means unsubstituted or substituted aryl group or heteroaryl group; or R¹ means 3-amino-1,2,4-triazole-5-carbonyl group: ; Xxx⁷ means Leu or Nle; Xxx⁸ means Arg or Lys(iPr); Xxx⁹ means Pro; Xxx¹⁰ means Ala or Sar, and their salts with pharmaceutically acceptable acids. Invention relates to method for preparing these compounds, pharmaceutical composition eliciting properties of LHRH antagonist comprising compound of the general formula (I) as an active component. Invention relates to method for preparing a medicinal agent used for treatment of hormone- -dependent disturbances that elicits the enhanced solubility in water. EFFECT: improved preparing method, valuable medicinal properties. 15 cl, 6 dwg, 2 tbl