8BETA-HYDROCARBYL-SUBSTITUTED ESTRATRIENES FOR USE AS SELECTIVE ESTROGENS

摘要

8 beta -Substituted 11 beta -(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives (I) are new. 8 beta -Substituted 11 beta -(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives of formula (I) are new. R2 = H, halo, R18, OR18 or OSO2R19; R3 = OR18, OSO2R19 or OC(O)R22; R18 = H or CF3, or 1-6C alkyl or 0-6C acyl (both optionally unsaturated); R19 = NR20R21; R20, R21 = H, 1-5C alkyl or C(O)R22; or NR20R21 = 4-6C polymethyleneimino or morpholino; R22 = 0-10C saturated or mono-, di- or triunsaturated hydrocarbyl (optionally substituted and optionally partially or completely halogenated), or 3-7C cycloalkyl, 4-15C cycloalkylalkyl, aryl, heteroaryl or aralkyl (all optionally substituted); R6, R6', R7, R7', R14-R16 = H; or R6+R7, R14+R15 or R15+R16 = additional bond; R8 = 1-5C alkyl or 2-5C alkenyl (both optionally partially or completely halogenated), or ethynyl or prop-1-ynyl; R11 = n-pentyl or n-hexyl; R15', R16' = H, halo or R3; one of R17 or R17' = H; and the other R17 or R17' = H, halo, benzyloxy or OSO2R19; or one of R17 or R17' = R18; and the other R17 or R17' = C(O)R22 or OC(O)R22; or one of R17 or R17' = OR18; and the other R17 or R17' = R18 or OC(O)R22; or R17+R17' = =CR23R24 or =O; and R23, R24 = H or halo. Independent claims are also included for: (1) use of a 11 beta -(R11)-8b-(R8)-estra-1,3,5(10)-triene fragment as a component of the overall structure of compounds for use as male or female contraceptives free of effects on other estrogen-sensitive organs (such the uterus or liver); and (2) use of a 11 beta -(R11)-8b-(R8)-estra-1,3,5(10)-triene fragment as a component of the overall structure of compounds for the treatment of benign or malignant proliferative ovarian diseases.