FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of 8-pyridono[5,6-g] quinoline of the formulas (I) , or (III)
, or (IV)
wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine atom; R2 is CF3CF2H; R3 is hydrogen atom; R4 and R5 each independently means hydrogen atom, C1-C4-alkyl; R6 and
mean hydrogen atom; R8 is hydrogen atom, C1-C4-alkyl; R9-R18 each means hydrogen atom; R19 means fluorine atom or NO2; R24 is hydrogen atom, C1-C4-alkyl, NO2; R25 is hydrogen atom, C1-C4-alkyl; R26 is hydrogen atom, C1-C6-alkyl; R27 and R28 each independently means hydrogen atom or C1-C4-alkyl; m = 1; n = 0 or 1; o = 0 or 1; Y is oxygen atom; Z is NH, NR22; R22 is C1-C4-alkyl, and also pharmaceutical composition for effect on activity of androgenic receptors. Invention describes method of effect on activity of androgenic receptors, method for modulation process mediated by androgenic receptors, method for treatment of patient involving modulation of process mediated by androgenic receptors, method for treatment of patient needing androgen-receptor therapy using derivatives of 8-pyridono[5,6-g] quinoline. Proposed compounds are antagonists and agonists of androgenic receptors and can be used in treatment and/or modulation of acnes, male baldness, hirsutism, hypogonadism, hyperplasia of prostate and hormone-dependent cancers. EFFECT: valuable medicinal properties of compounds. 36 cl, 4 tbl, 31 ex
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Authors
Dates
2003-10-20—Published
1997-06-26—Filed