COMPOUNDS INHIBITING AROMATASE ACTIVITY SELECTIVELY, METHOD OF SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention describes new compounds of the formula (I) where R₁ means H or fluorine atom; R₂ means a heterocyclic radical taken from 1-imidazolyl, triazolyl, tetrazolyl, thiazolyl; R₃ means H or OH; R₄ means H; R₅ means H or OH; or R₄ means H and R₃ and R₅ in common form a bond; or R₃ means H and R₄ and R₅ in common form =O; R₆ means methylene, ethylene, -CHOH-, -CHOH-CH₂-, -CH=CH- or -C(=O)-; or R₄ means H and R₅ and R₆ in common mean =CH-, or their stereomers, or their nontoxic pharmaceutically acceptable acid-additive salts at condition that R₆ can not mean -C(= O)- when means -C=CH-. Invention describes also a method of synthesis of the compounds and preparing a pharmaceutical composition based on it which inhibits aromatase activity and a method of inhibition of aromatase activity. EFFECT: improved method of synthesis, inhibition of aromatase. 21 cl, 12 ex