Novel neuroactive steroids, processes of their preparation and use

摘要

In the present invention, there are described steroids exhibiting neural activity having the general formula VI, in which Re1 represents a hydrogen atom, the group OH or NRe2Re3, wherein Re2 and Re3 can represent independently on each other a hydrogen atom or an alkyl group or together they form a heterocycle, Re4 represents a hydrogen atom or a fluorine atom, Re5 denotes a hydrogen atom or a fluorine atom, the group OH or a carboxymethyloxiline group, Re6 represents a hydrogen atom, a carboxymethyl group or a methylene carboxylic acid salt, containing preferably an alkali metal, a primary, secondary or tertiary amine and Re7 represents the group COCHi3 or the group COORe8, wherein Re8 denotes a hydrogen atom, a sodium atom, methyl or triethylammonium group. Disclosed is also a process for preparing the above-described novel neuroactive steroids, which process is characterized by introducing a fluorine atom into the position 3{alpha}. The neuroactive steroids according to the present invention are suitable for therapy of states controlled by the action of a neurotransmitter û a {gamma}-aminobutyric acid (GABA), i.e. as substances exhibiting activity against pain, anxiety and sleeplessness and further as anesthetics.