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    3-methylene-4-androsten-17-ones, process for their production and pharmaceutical preparations containing them
    31.
    发明授权
    3-methylene-4-androsten-17-ones, process for their production and pharmaceutical preparations containing them 失效
    3-亚甲基-4-雄酮-17-酮，其制备方法和含有它们的药物制剂

    公开(公告)号：US4925834A

    公开(公告)日：1990-05-15

    申请号：US188569

    申请日：1988-04-29

    申请人： Rolf Bohlmann ,  Henry Laurent ,  David Henderson ,  Yukishige Nishino

    发明人： Rolf Bohlmann ,  Henry Laurent ,  David Henderson ,  Yukishige Nishino

    IPC分类号： A61K31/565 ,  C07J1/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J71/00

    CPC分类号： C07J71/001 ,  C07J1/0011 ,  C07J1/0022 ,  C07J17/00 ,  C07J31/006 ,  C07J41/0094

    摘要： A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein R.sub.a represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which R.sub.a is in the alpha- or beta-position, andR.sub.b represents a hydrogen atom, a hydroxyl or an --S(O).sub.n R.sub.c group, in which R.sub.c is a hydrogen atom or an alkyl or acyl group with 1-4 carbon atoms, n=0, 1 or 2, andX represents CH.sub.2, CHF, CHCl or CHBr, in which if R.sub.a is hydrogen and R.sub.b is hydroxyl or R.sub.a and R.sub.b each are hydrogen, X is not CH.sub.2.The new compounds of formula I are suitable for fertility control and for treatment of diseases which are promoted by estrogens.

    摘要翻译： 其中R a表示氢原子或具有1-6个碳原子的饱和或不饱和的直链或支链的任选取代的烷基的式I的3-亚甲基-4-雄酮-17-酮 ，其中Ra为α或β位，Rb表示氢原子，羟基或-S（O）nRc基团，其中Rc为氢原子或具有1-4个碳原子的烷基或酰基基团 碳原子，n = 0,1或2，X表示CH 2，CHF，CHCl或CHBr，其中如果Ra是氢，Rb是羟基或R a和R b各自是氢，X不是CH 2。 新的式I化合物适用于生育控制和治疗由雌激素促进的疾病。

    17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE
    38.
    发明申请
    17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE 失效
    17Beta-CYANO-19-NOR-ANDROST-4-ENE衍生物，其使用和药物包含衍生物

    公开(公告)号：US20090048217A1

    公开(公告)日：2009-02-19

    申请号：US12137111

    申请日：2008-06-11

    申请人： Joachim KUHNKE ,  Jan Huebner ,  Rolf Bohlmann ,  Thomas Frenzel ,  Ulrich Klar ,  Frederik Menges ,  Sven Ring ,  Steffen Borden ,  Hans-Peter Muhn ,  Xatja Prelle

    发明人： Joachim KUHNKE ,  Jan Huebner ,  Rolf Bohlmann ,  Thomas Frenzel ,  Ulrich Klar ,  Frederik Menges ,  Sven Ring ,  Steffen Borden ,  Hans-Peter Muhn ,  Xatja Prelle

    IPC分类号： A61K31/567 ,  C07J3/00 ,  A61P5/24

    CPC分类号： C07J53/008 ,  C07J41/0094 ,  C07J53/007

    摘要： The 17β-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7, R9, R10 are hydrogen or are omitted with formation of a double bond between C9 and C10, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, where at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 is unequal to hydrogen or R6b and R7 are omitted with formation of a double bond between C6 and C7, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts.

    摘要翻译： 本发明的17β-氰基-19-去甲 - 雄甾-4-烯衍生物具有孕激活作用。 它们具有一般化学式1，其中Z选自O，两个氢原子，NOR和NNHSO 2 R，其中R是氢或C 1 -C 4 - 烷基，R 4是氢或卤素，此外：R 6a， R6b一起形成亚甲基或1,2-乙二基或R6a为氢，R6b选自氢，甲基和羟基亚甲基，R7选自氢，C1-C4-烷基，C2-C3-烯基和 环丙基，或者：R6a是氢，R6b和R7一起形成亚甲基，或者在C6和C7之间形成双键被省略，R9，R10是氢或在C9与C10之间形成R15，R16 是氢或一起形成亚甲基，R 17选自氢，C 1 -C 4 - 烷基和烯丙基，其中至少一个取代基R4，R6a，R6b，R7，R15，R16和R17不等于氢或R6b 并且在C6和C7之间形成双键而省略R7，此外， 上升它们的溶剂合物，水合物，立体异构体，非对映异构体，对映体和盐。