Patent ID: 6339079
Filing Date: 2002-01-15
Classification: A61P,C07J,Y02P

Abstract:
Steroids of the gonane type and D-homo-gonane type and salts thereof, having the general formula I: whereinC atoms 2, 3, 4, 6, 7, 11, 12, 15, 16 and 17 are each independently unsubstituted or substituted by C1-C6-alkyloxy, C1-C4-alkyloxy-C1-C4-alkyloxy, hydroxy-C1-C4-alkyloxy, C1-C6-alkanoyloxy, tris-(C1-C6-alkyl)-silyloxy or hydroxy, wherein each secondary hydroxy group â€”CH(OH)â€” of the C1-C6-alkyloxy, C1-C4-alkyloxy-C1-C4-alkyloxy, hydroxy-C1-C4-alkyloxy, C1-C6-alkanoyloxy, tris-(C1-C4-alkyl)-silyloxy or hydroxy group is optionally substituted by a keto grouping â€”C(&boxH;O)â€” or keto grouping protected in the form of a ketal, thioketal, cyanhydrin, cyanosilyl ether or a germinal hydroxyethinyl group; n is 1 or 2; R1 is &agr;-methyl, &bgr;-methyl, &agr;-ethyl, &bgr;-ethyl or H; each sulfamoyloxy group â€”OSO2NHR2 is attached at a point selected from the group consisting of C atoms 1, 2, 3, 4, 6, 7, 11, 15, 16 and 17 and groups R4 and R5 with the proviso that the sulfamoyloxy group is not attached at the C atom 3 when m is 1; R2 is H,-C1-C5-alkyl, C1-C3-alkyl with annelated saturated ring, aryl-C1-C3-alkyl, C1-C5-alkanoyl, or C3-C7-cycloalkylcarbonyl; R3 is H, OH, halogen, pseudohalogen, C1-C3-alkyl, C3-C7-cycloalkyl, 11,11-cycloalkyl or aryl C1-C3-alkyl; R4 is H, aryl or C1-C12-alkyl; R5 is H, C1-C12-alkyl or C1-C12-alkylaryl; R6 is H or halogen; and m is 1 to 5; and optionally further comprising a feature selected from the group consisting of:a double bond between a pair of C atoms selected from the group consisting of C atoms 9 and 11, C atoms 8 and 9, C atoms 8 and 14, C atoms 6 and 7, and C atoms 7 and 8; a double bond between a pair of C atoms selected from the group consisting of C atoms 14 and 15 and C atoms 15 and 16 when n is 1; two double bonds, one between C atoms 8 and 9 and one between C atoms 14 and 15; two double bonds, one between C atoms 8 and 9 and one between C atoms 7 and 6; and a cyclopropane grouping or epoxide grouping with &agr;- or &bgr;-orientation between C atoms 14 and 15 or C atoms 15 and 16; and with the condition that R3 is not H or OH when m is 1 and the sulfamoyloxy group is bonded to the aromatic A ring;and with the exception of the compound estra-1,3,5(10)-trien-3,17&bgr;-diyl 3,17-diamidosulfonate.