DERIVATIVES OF ESTRA-1,3,5(10)-TRIENE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new estra-1,3,5(10)- -triene sulfamates of the general formula (I) where R means the group R¹R²N where R¹ and R² means independently hydrogen atom or C₁-C₅-alkyl group or in common with nitrogen atom form polymethyleneimino-group containing 4-6 carbon atoms or morpholino-group; R³ means hydrogen atom or C₁-C₅-alkyl group; R⁴ means hydrogen atom, hydroxyl group, esterified hydroxyl group, halogenalkyl group containing 1-5 carbon atoms or alkoxy-group contaning 1-5 carbon atoms; R⁵ and R⁶ each means hydrogen atom or in common means methylene group; R⁷, R⁸ and R⁹ mean independently each of other hydrogen atom or hydroxyl group and ring B can has one or two double bonds, or R⁸ means alkynyl residue containing up to 5 carbon atoms, or R⁸ and R⁹ in common can mean oxygen atom in the case when at least one of residues R³, R⁴, R⁵, R⁶ or R⁷ is not hydrogen atom. Compounds can be used for the hormonal contraception and substituent therapy of climacteric hormone (HRT) and for treatment of patients with gynecological and andrological illnesses. Compounds show low estrogenicite effect on the liver. Invention describes also methods of synthesis of compounds and pharmaceutical compositions preparing. EFFECT: improved method of synthesis and preparing, enhanced hormonal effectiveness. 4 cl, 1 tbl, 26 ex