Derivatives of 17-hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-benzylidene, process for their preparation and their use for treating diseases

2010 
Derivatives of 17-hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-benzylidene of the general formula (I) ** ** Formula wherein Y represents -CR 1> = CHR2 group or a -CR1> = NR3, in each case is linked to the phenyl ring in the meta position (m) or (p), wherein R1 is hydrogen or C1-C10 alkyl radical, R2 represents hydrogen, an alkyl radical C1 C10, C2-C10, aryl, C7-C20, C1 C10 acyl, CO2R4, CN, CH> = CH-CO2R4, -CH2CH (CO2R4) 2, CH2CH (CN) 2 or a radical and R3 represents a CH2NHCONHR5 C1-C10 alkyl, O-alkyl, O- (CH2) n-COOR 4, O-CH2-aryl, aryl, aralkyl C7- C20 or CH2CO2R4 radical, wherein R4 represents hydrogen or a group alkyl C1-C10 and R5 It represents an alkyl group C1-C10, C2-C10 alkenyl, aryl, C7-C20, (CH2) nCO2R4, ** ** Formula with n> = 1 or 2 and R4 in the meaning given, or represents a group and X means oxygen, a group or a NNHSO2R6 NOR6 group, wherein R6 is hydrogen alkyl, a radical or C1-C10 aryl or C7-C20 aralkyl, and salts, solvates or solvates of salts, including all crystal modifications, clathrates α-, s- or γ-cyclodextrin and compounds encapsulated with liposomes wherein alkyl represents and alkyl groups may also be perfluorinated, or may be substituted by 1-5 halogen atoms, hydroxy groups, C1-C4alkoxy, C6-C12 aryl groups (which again may be substituted with one -3 halogen atoms), alkenyl represents alkenyl groups and may be substituted with 1-5 halogen atoms, hydroxy groups, C1-C3 alkoxy or C6-C12 aryl groups (which again may be substituted with 1-3 atoms halogen), aryl represents carbocyclic radicals substituted and unsubstituted may be substituted once or several times with halogen, OH, O-alkyl, S-alkyl, S (O) -alkyl and SO2-alkyl, CO2H, CO2 groups -alkyl, NH2, NO2, N3, CN, C1-C10 alkyl, C1-C10 acyl, acilox i C1-C10, aralkyl represents aralkyl groups and may be substituted once or several times with halogen, OH, O, CO2H, CO2-alkyl, NO2, N3, CN, C1-C20, acyl C1-C20 or C1-C20 acyloxy.
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