Steroidal 3-methylene derivative, pharmaceutical composition, use of the steroidal 3-methylene derivative, and method of treatment and / or prevention of arthritic and / or autoimmune diseases

摘要

"3-METHYLENE STERIDE DERIVATIVE, PHARMACEUTICAL COMPOSITION, USE OF 3-METHYLENE STERIDE DERIVATIVE, AND, METHOD OF TREATMENT AND / OR PREVENTION OF ARTHRITIC DISEASES AND / OR AUTO-IMMUNE DISEASES". The invention relates to a 3-methylene steroid derivative which has the general formula (1) where R ^ 1 ^ is H or together with R ^ 3 ^ epoxide form 225 or R ^ 1 ^ is absent if there is a double bond 5 -10 or 4-5; R ^ 2 ^ is (C ~ 1 ~ C ~ 5 ~) alkyl or CF ~ 3 ~; R ^ 3 ^ is 225 H, 225 CH ~ 3 ~ or together with R ^ 1 ^ form 225 -epoxide or R ^ 3 ^ is absent if there is a 5-10 double bond; R 4 is H, lower alkyl; Y is [H, H], [OH, H], = O, [OH, lower alkyl], [OH, (C ~ 2 ~ -C ~ 5 ~) alkenyl], [OH, (C ~ 2 ~ C ~ 5 ~) alkynyl] or (C ~ 1 ~ -C ~ 6 ~) alkylidene, whereby said alkyl, alkenyl, alkynyl and alkylidene is optionally halogenated; = NOR ^ 5 ^, whereby R ^ 5 ^ is H, lower alkyl; dotted lines represent optional double bonding, or its prodrugs for the treatment of arthritic and / or autoimmune diseases.