DERIVATIVES OF ESTRA-1,3,5(10)-TRIENE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION

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 R and R 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; R means hydrogen atom or C1-C5-alkyl group; R means hydrogen atom, hydroxyl group, esterified hydroxyl group, halogenalkyl group containing 1-5 carbon atoms or alkoxy-group contaning 1-5 carbon atoms; R and R each means hydrogen atom or in common means methylene group; R7, R and R mean independently each of other hydrogen atom or hydroxyl group and ring B can has one or two double bonds, or R means alkynyl residue containing up to 5 carbon atoms, or R and R in common can mean oxygen atom in the case when at least one of residues R3, R4, R5, R or R 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