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    17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE
    36.
    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。

    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter
    38.
    发明申请
    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter 失效
    18-甲基-19-去甲-17-孕-4-烯-21,17-碳内酯，以及含有后者的药物制剂

    公开(公告)号：US20060252737A1

    公开(公告)日：2006-11-09

    申请号：US11321449

    申请日：2005-12-30

    申请人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    发明人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    IPC分类号： A61K31/58 ,  C07J19/00

    CPC分类号： C07J19/00

    摘要： This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ═NOR or ═NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in α- or β-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an α- or β-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an α- or β-position methylene group or an additional bond. The new compounds have gestagenic and anti-mineralocorticoid action and are suitable for the production of pharmaceutical preparations, for example for oral contraception and the treatment of pre-, peri- and post-menopausal symptoms.

    摘要翻译： 本发明描述了通式I的新的18-甲基-19-去甲-17-孕甾-4-烯-21,17-碳内酯，其中Z表示氧原子，两个氢原子，-NOR或-NNHSO- R 2是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子 ，卤素原子，甲基或三氟甲基，R 6和/或R 7可以是α-或β-位，并且独立地为一个 另一个是指具有1至4或3至4个碳原子的直链或支链烷基，或R 6表示氢原子，R 7表示 具有1至4或3至4个碳原子的α-或β-位的直链或支链烷基，或R 6和R 7各自表示 氢原子或R 6和R 7一起是指α-或β-位亚甲基或另外的键。 新化合物具有孕激素和抗盐皮质激素的作用，并且适用于制备药物制剂，例如用于口服避孕和治疗绝经前，绝经期和绝经后症状。

    11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring
    40.
    发明授权
    11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring 失效
    11beta取代的19-nor-17-α-前 - 1,3,5（10） - 三烯-17β-酯与21,16α-内酯环

    公开(公告)号：US06956031B2

    公开(公告)日：2005-10-18

    申请号：US10397855

    申请日：2003-03-27

    申请人： Alexander Hillisch ,  Walter Elger ,  Rolf Bohlmann ,  Jens Hoffmann

    发明人： Alexander Hillisch ,  Walter Elger ,  Rolf Bohlmann ,  Jens Hoffmann

    IPC分类号： A61K31/58 ,  A61K31/585 ,  C07J17/00 ,  C07J71/00

    CPC分类号： C07J17/00

    摘要： This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II in which R11 is a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

    摘要翻译： 本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基 其中R 11是具有可以在末端被全氟烷基取代的氮原子的长链烷基。 化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。