DERIVATIVES OF QUINOLINE AS ANTAGONISTS OF GONADOTROPIN-RELEASING HORMONE AND METHOD FOR THEIR PREPARING (VARIANTS)

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...

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Hauptverfasser: SHMEES NORBERT, SHTREL'KE PETER, TER LAK ANTONIUS MARINUS, BJUMAN UL'RIKH, DRESHER PETER, GJUNTER EHKKHARD, KHESS-SHTUMP KHOL'GER, MUN PETER, KJUNE ROLAND, POLIMEROPULOS EHMMANUEHL
Format: Patent
Sprache:eng ; rus
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Zusammenfassung: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