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    New 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1
    2.
    发明申请
    New 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1 失效

    公开(公告)号：US20060009434A1

    公开(公告)日：2006-01-12

    申请号：US11154947

    申请日：2005-06-17

    申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    IPC分类号： A61K31/57 ,  C07J1/00

    CPC分类号： C07J1/00

    摘要： The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of general formula I in which R2 means a saturated or unsaturated C1-C8-alkyl group, a C1-C5-alkyloxy group, an aralkyl radical or alkylaryl radical, a radical —O—CnFmHo, whereby n=1, 2, 3, 4, 5 or 6, m≧1 and m+o=2n+1, or a group CH2XY, in which X stands for an oxygen atom and Y stands for an alkyl radical with 1 to 4 carbon atoms, as well as a halogen atom or a nitrile group, R13 means a hydrogen atom or a methyl group, R16 means a hydrogen atom or a fluorine atom, Z means an oxygen atom or a sulfur atom, R3 and R5, in each case independently of one another, mean an α- or β-position hydrogen atom, R4 and R6, in each case independently of one another, mean an α- or β-position hydrogen atom, a C1-C5-alkyl group, a C1-C5-alkyloxy group, a C1-C5-acyl group or a hydroxy group or an aralkyl radical or alkylaryl radical, R3 and R4 together mean an oxygen atom, R5 and R6 together mean an oxygen atom, R7 and R8 in each case mean a hydrogen atom or together a CH2 group, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.