abstract |
FIELD: organic chemistry, steroids, pharmacy. SUBSTANCE: invention relates to a new derivative of 11-(phenyl-substituted)-estra-4,9-diene of the formula (I) where A means a residue of 5- or 6-membered ring containing two heteroatoms which are not bound each with other and taken independently from O and S; indicated ring can be substituted with one or more halogen atoms; or residue of 5- or 6-membered ring where double bond C=C is absent has one heteroatom taken from O and S and heteroatom is bound with phenyl group at position noted by asterisk and ring can be substituted with one or more halogen atoms; R 1 means hydrogen atom; R 2 means hydrogen atom, (C 1-8 )-alkyl, halogen atom or CF 3 ; X means O or NOH; and dotted line means a possible bond. Compounds show antiglucocorticoid activity and can be used for treatment and prophylaxis of glucocortcoid-dependent diseases. Invention describes also a method of synthesis of the above indicated compounds and a pharmaceutical composition based on compounds of the formula (I). EFFECT: improved method of synthesis, valuable pharmacological properties. 9 cl, 1 tbl, 13 ex |