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18 Norsteroids as selectively active estrogens

  • US 6,958,327 B1
  • Filed: 11/02/2000
  • Issued: 10/25/2005
  • Est. Priority Date: 11/02/1999
  • Status: Expired due to Fees
First Claim
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1. A gona-1,3,5(10)-triene compound of formula I embedded imagein whichR1 means a halogen atom, or R18

  • O—

    , R18 means a hydrogen atom or a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 6 carbon atoms, R2 means a hydrogen atom R19 is an R20R21N group, R20 and R21, independently of one another, represent a hydrogen atom, a C1-C5 alkyl radical, a group C(O)R22, R22 can contain a straight-chain or branched-chain hydrocarbon radical with up to 12 carbon atoms, which in addition can contain up to three double bonds and/or triple bonds, a C3-C7 cycloalkyl radical, an aryl radical or a combination of these structural features, or, together with the N atom, a polymethylenimino radical with 4 to 6 C atoms or a morpholino radical;

    R3 means a group R18

    O—

    , R19SO2

    O—

    or —

    O—

    C(O)R22, or an —

    O-aryl —

    O-heteroaryl or —

    O-aralkyl radical;

    R6 is hydrogen, R7 is a hydrogen atom, a halogen atom, a group R18

    O—

    , R19SO2

    O—

    or —

    R22, a straight-chain or branched-chain, saturated or unsaturated, partially or completely halogenated alkyl group with up to 10 carbon atoms or an optionally substituted aryl, heteroaryl or aralkyl radical, R8 and R9 are hydrogen, R11 means a hydrogen atom, a halogen atom, a group R18

    O—

    , R19SO2

    O—

    or —

    R22, a group —

    X—

    R18, a nitrooxy group, a straight-chain or branched-chain, saturated or unsaturated, partially or completely halogenated hydrocarbon radical with up to 10 carbon atoms or an optionally substituted aryl, heteroaryl or aralkyl radical, X is an oxygen or sulfur atom, R11′

    , R14, R15, R15′

    and R16 each mean a hydrogen atom, and R17 and R17′

    mean a hydrogen atom and a halogen atom;

    a hydrogen atom and a group R19SO2

    O—

    ;

    hydrogen and a group —

    O—

    C(O)R22;

    or hydrogen and —

    R18

    O—

    .

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