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    17Beta-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE
    7.
    发明申请
    17Beta-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE 审中-公开
    17B-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENE DERIVATIVE，其使用和药物包含衍生物

    公开(公告)号：US20090048218A1

    公开(公告)日：2009-02-19

    申请号：US12137122

    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 ,  KATJA PRELLE

    发明人： JOACHIM KUHNKE ,  JAN HUEBNER ,  ROLF BOHLMANN ,  THOMAS FRENZEL ,  ULRICH KLAR ,  FREDERIK MENGES ,  SVEN RING ,  STEFFEN BORDEN ,  HANS-PETER MUHN ,  KATJA PRELLE

    IPC分类号： A61K31/567 ,  C07J3/00 ,  A61K31/565

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

    摘要： The 17β-cyano-18a-homo-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 either 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, at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 not being hydrogen or R6b and R7 being omitted with formation of a double bond between C6 and C7 or being omitted with formation of a double bond between C1 and C2, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts.

    摘要翻译： 本发明的17β-氰基-188-均聚-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：R 6a是氢，R 6b和R 7一起形成亚甲基或在C6和C7之间形成双键被省略，R9，R10是氢或在C9和C10之间形成双键时省略，R15， R 16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，取代基R 4，R 6a，R 6b，R 7，R 15，R 16和R 17中的至少一个不是氢或R 6b， 在C6和C7之间形成双键而省略了R7，或被省略 在C1和C2之间形成双键，并且还包含它们的溶剂合物，水合物，立体异构体，非对映异构体，对映异构体和盐。

    20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
    8.
    发明授权
    20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof 失效
    20-螺环和具有开环E的类似物，其制备方法及其药物制剂

    公开(公告)号：US4559332A

    公开(公告)日：1985-12-17

    申请号：US598109

    申请日：1984-04-09

    申请人： Jurgen Grob ,  Jaroslav Kalvoda

    发明人： Jurgen Grob ,  Jaroslav Kalvoda

    IPC分类号： A61K31/58 ,  A61P5/38 ,  A61P7/10 ,  C07J1/00 ,  C07J5/00 ,  C07J13/00 ,  C07J21/00 ,  C07J41/00 ,  C07J53/00 ,  C07J63/00 ,  C07J71/00 ,  A61K31/585

    CPC分类号： C07J41/0094 ,  C07J1/0011 ,  C07J13/005 ,  C07J21/00 ,  C07J21/003 ,  C07J21/008 ,  C07J5/0053 ,  C07J53/007 ,  C07J53/008 ,  C07J71/0015

    摘要： Steroid compounds of the 20-spiroxane series and their analogues having an open ring E of the formula, ##STR1## in which --A--A-- represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 represents hydrogen, andR.sup.2 represents an .alpha.-oriented lower alkoxycarbonyl radical, orR.sup.1 and R.sup.2 together represent an .alpha.- or a .beta.-oriented methylene radical,--B--B-- represents the group --CH.sub.2 --CH.sub.2 -- or an .alpha.- or .beta.-oriented group ##STR2## X represents two hydrogen atoms or oxo, Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--, orY.sup.1 represents hydroxy, andY.sup.2 represents hydroxy, lower alkoxy or, if X represents H.sub.2, also lower alkanoyloxy,and salts of compounds in which X represents oxo and Y.sup.2 represents hydroxy, are distinguished as effective aldosterone-antagonists with minimal side-effects and, for that reason, are especially suitable for the treatment of all forms of hyperaldosteronism.

    摘要翻译： 20-螺螺系列的类固醇化合物及其具有下式的开环E的类似物，其中-AA表示基团-CH 2 -CH 2 - 或-CH = CH-，R 1表示氢， 并且R 2表示α-取代的低级烷氧基羰基，或者R 1和R 2一起表示α或β取向的亚甲基，-BB-表示基团-CH 2 -CH 2 - 或α或β取向基团 X表示2个氢原子或氧代，Y1和Y2一起代表氧桥-O-，或Y1表示羟基，Y2表示羟基，低级烷氧基，或如果X表示H 2，还表示低级烷酰氧基， X表示氧代，Y2表示羟基，被认为是有效的醛固酮拮抗剂，副作用很小，因此特别适用于治疗所有形式的醛固酮增多症。

    17β-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative
    10.
    发明授权
    17β-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative 失效
    17-氰基-19-去甲 - 雄甾-4-烯衍生物，其用途和药物包含衍生物

    公开(公告)号：US08207150B2

    公开(公告)日：2012-06-26

    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 ,  Katja Prelle

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

    IPC分类号： A61K31/56 ,  C07J3/00

    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17α-氰基-19-去雄甾-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。