DERIVATIVES OF QUINOLINE AS ANTAGONISTS OF GONADOTROPIN-RELEASING HORMONE AND METHOD FOR THEIR PREPARING (VARIANTS) Russian patent published in 2006 - IPC C07D215/56 C07D215/20 A61K31/47 A61P5/02 

FIELD: organic chemistry, medicine, endocrinology.

SUBSTANCE: invention relates to new derivatives of quinoline eliciting antagonistic activity with respect to gonadotropin-releasing hormone. Invention describes derivatives of quinoline of the general formula (1): wherein R₁ means carboxylic acid ester residue -CO-OR₁₂ wherein R₁₂ means direct or branched alkyl chain comprising 1-10 carbon atoms; R₂ means group -CH(R₂₁)R₂₂ wherein R₂₁ means hydrogen atom; R₂₂ means phenyl ring or naphthyl ring substituted with halogen atom or group -CF₃; each among R₃ and R₄ means independently hydrogen atom; R₅ means group jointed through residue Z: wherein G means -C=C-; Z means oxygen atom; L means NH-group; Q means carbonyl; R₅₁ means direct or branched (C₁-C₆)-alkyl group; R₆ means group -CH₂-N(R₆₁)R₆₂ wherein R₆₁ means independently hydrogen atom; R₆₂ means unsubstituted benzyl group; W and X means carbon atoms; Y means nitrogen atom, and their salts with physiologically acceptable acids or bases. Also, invention describes using derivatives of quinoline and a method for preparing derivatives of quinoline (variants).

EFFECT: improved preparing method, valuable medicinal properties of compounds.

7 cl, 1 tbl, 8 ex