17α-ALKYL-17β-HYDROXYESTRATRIENES, THEIR USING AND PHARMACEUTICAL PREPARATION Russian patent published in 2006 - IPC C07J41/00 A61K31/567 A61P5/32 

FIELD: organic chemistry, steroids.

SUBSTANCE: invention describes 17α-alkyl-17β-hydroxyestra-1,3,5(10)-trienes possessing anti-estrogenic properties of the general formula (I): wherein Hal means fluorine (F), chlorine (Cl) atoms; R³ means hydrogen atom (H), (C₁-C₄)-alkyl, (C₁-C₄)-alkanoyl, simple cyclic (C₃-C₇)-ether comprising O-atom; R^17' means H, (C₁-C₄)-alkyl, (C₁-C₄)-alkanoyl; R^17'' means (C₁-C₄)-alkyl, (C₁-C₄)-alkynyl; SK means: U-V-W-X-Y-Z-E wherein U means (C₁-C₁₃)-alkylene; V means -CH_2; W means -N(R⁶) wherein R means H, (C₁-C₄)-alkyl; X means (C₁-C₁₂)-alkylene; Y means a direct bond between X and Z; Z means possibly fluorinated (C₁-C₉)-alkylene; E means -CF₃. Also, invention describes 17-oxoestra-1,3,5(10)-trienes and 17β-hydroxyestra-1,3,5(10)-trienes as intermediate substances used in synthesis of estratrienes proposed by the invention. Also, invention describes using 17α-alkyl-17β-hydroxyestratrienes for preparing corresponding medicinal agents and pharmaceutical preparations comprising at least one 17α-alkyl-17β-hydroxyestratriene and at least one pharmaceutically acceptable carrier.

EFFECT: valuable medicinal properties of steroids.

5 tbl, 7 dwg