Patent ID: 6579864
Filing Date: 2003-06-17
Classification: A61P,C07J

Abstract:
A 3-methylene steroid derivative having the general formula 1 whereinR1 is H or together with R3 forms a &bgr;-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5)alkyl or CF3; R3 is &bgr;H, &bgr;CH3 or together with R1 forms a &bgr;-epoxide or R3 is absent if there is a 5-10 double bond; R4 is H, or lower alkyl; Y is [H, H] [OH, H], &boxH;O, [OH, lower alkyl], [OH, (C2-C5)alkenyl], [OH, (C2-C5)alkynyl] or (C1-C6)alkylidene, wherein said alkyl, alkenyl, alkynyl or alkylidene is optionally halogenated; or &boxH;NOR5, wherein R5 is H[,] or lower alkyl; dotted lines represent an optional double bond; or a salt, solvate or prodrug thereof, with the proviso that the 3-methylene steroid derivative is not (7&agr;,17&bgr;)-7&agr;-methyl-3-methylene-4-estren-17-ol, (7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-4-ene-17-ol, (7&agr;,17&agr;)-7-methyl-3-methylene-19,21-dinorpregn-4-ene-17-ol, (7&agr;)-17-keto-7-methyl-3-methylene-4-estrene, (7&agr;,17&agr;)-7-methyl-3-methylene-19-norpregn-4-en-20-yn-17-ol, 17&bgr;-hydroxy-7&agr;-methyl-3-methylene-17&agr;-propen-2-yl-4-estrene, or 17&bgr;-hydroxy-7&agr;-methyl-3-methylene-17&agr;-buten-2-yl-4-estrene.