| 摘要 |
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 |
