NEUROACTIVE STEROIDS, PHARMACEUTICAL PREPARATION, METHOD OF TREATMENT AND PROPHYLAXIS OF DIFFERENT DISORDERS, METHOD OF SLEEP INDUCTION AND METHOD OF ANESTHESIA INDUCTION WITH THEIR USING, METHOD OF MODULATION OF COMPLEX RECEPTOR GABAA-CHLORIDE IONOPHORE Russian patent published in 2002 - IPC

FIELD: organic chemistry, steroids, medicine, pharmacy. SUBSTANCE: invention describes novel neuroactive steroids of androstane and pregnane order of the formula (I) or their physiologically acceptable 3-esters where R means H or lower alkoxy-group; R₁ means H, C_1-10-alkyl, C_2-10-alkenyl, C_2-10-alkynyl, halogen-C_1-10-alkyl, trihalogen-C_1-10-alkyl, hydroxy-C_2-10-alkynyl, alkoxy-C_1-10- alkyl, optionally substituted phenylalkynyl, hydroxyalkynyldicarboxylic acid hemiester; R₂ means H or keto-group; R₃ means optionally substituted alkoxy-, alkynylhydroxy-, optionally substituted phenyl- alkynylhydroxy-group, -C(O)-CH₂-Y-G, -C(O)-CH₂-O-D, -C(O)-CH₂-O-E, -C(O)-CH₂-Z-G or C(O)- CH₂-Y-Z-A where Y means O, S, SO or SO₂; Z means C_1-10-alkyl; G means pyridyl or optionally substituted phenyl; D means quinoline joined to carbon atom; E means optionally substituted phenyl; A means OH, carboxyl or sulfonate; R₄ means H; R₅ means H; R₆ means H; R₇ means H or OH; R₈ means H; R₉ means H; R₁₀ means H under condition that: when R₃ means C_1-3-alkoxy-group and R means H then R₁ differs from H; when R₃ means C_1-4-alkoxy-C_1-4/ - -alkoxy-group then R₁ differ from H or 1-propenyl; when R₃ means -C(O)-CH₂-Y-G and G means pyridyl joined to carbon atom then R₁ differs from H or C_1-10-alkyl; or when R₃ means C(O)-CH₂-Z-G then R₁ differs from H. Compounds of the formula (I) are able to effect on brain excitability and relieve stress, insomnia, mood disorders caused by agents exhibiting activity with respect to GRC. EFFECT: improved method of treatment and prophylaxis, valuable medicinal properties. 39 cl, 10 tbl, 1 dwg, 49 ex