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    17β-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative
    17.
    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。

    17BETA-CYANO-19-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE
    18.
    发明申请
    17BETA-CYANO-19-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE 审中-公开
    17BETA-CYANO-19-ANDROST-4-ENE DERIVATIVE，其使用和药物包含衍生物

    公开(公告)号：US20100292184A1

    公开(公告)日：2010-11-18

    申请号：US12664099

    申请日：2008-06-12

    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 ,  C07J53/00 ,  C07J41/00 ,  A61K31/695 ,  A61K31/565 ,  A61P15/18 ,  A61P5/24 ,  A61P5/34 ,  A61P5/42

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

    摘要： The 17β-cyano-19-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, R1, R2 are each independently hydrogen or methyl, or R1 and R2 together form methylene or are omitted with formation of a double bond between C1 and C2, 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 hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7 or: R6a is methyl and R6b and R7 are omitted with formation of a double bond between C6 and C7, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts, with the proviso that particular compounds are excluded.

    摘要翻译： 本发明的17α-氰基-19-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 1，R 2各自独立地是氢或甲基，或 R1和R2一起形成亚甲基或被省略，在C1和C2之间形成双键，R4是氢或卤素，此外：R6a，R6b一起形成亚甲基或1,2-乙二基或R6a是氢，R6b选自 包括氢，甲基和羟基亚甲基的基团，并且R 7选自氢，C 1 -C 4 - 烷基，C 2 -C 3 - 烯基和环丙基，或者：R 6a氢和R 6b和R 7一起形成亚甲基或被形成 C6和C7之间的双键或：R6a是甲基，R6和C7之间形成双键，R6b和R7被省略，R15，R16是氢或一起形成亚甲基，R17选自氢，C1- C4-烷基和烯丙基，并且还包含它们的溶剂化物 es，水合物，立体异构体，非对映体，对映异构体和盐，条件是排除特定的化合物。

    Method for producing c1-c15 fragments of epothilones and the derivatives thereof
    20.
    发明申请
    Method for producing c1-c15 fragments of epothilones and the derivatives thereof 审中-公开
    埃坡霉素c1-c15片段及其衍生物的制备方法

    公开(公告)号：US20070142675A1

    公开(公告)日：2007-06-21

    申请号：US10563058

    申请日：2004-06-19

    申请人： Ulrich Klar ,  Bernd Buchmann ,  Wolfgang Schwede ,  Werner Skuballa

    发明人： Ulrich Klar ,  Bernd Buchmann ,  Wolfgang Schwede ,  Werner Skuballa

    IPC分类号： C07C45/45

    CPC分类号： C07D417/06 ,  C07C45/673 ,  C07C49/17 ,  C07D493/04

    摘要： This invention describes a process for the production of C1-C15-fragments of epothilones and derivatives thereof, in which a C1-C6-fragment is linked with a C7-C12-fragment to a C1-C12-fragment, and the latter then is reacted with a C13-15-fragment to form the C1-C15 initial epothilone product that is to be produced. The thus obtained C1-C15 initial epothilone products can be reacted according to known methods to form the actual active ingredients. In addition, the invention relates to the corresponding C1-C12-fragments.

    摘要翻译： 本发明描述了一种制备埃坡霉素及其衍生物的C 1 -C 15 - 片段的方法，其中C1-C6-片段与C7- C12片段与C1-C12片段反应，然后与C13-15片段反应形成待生产的C1-C15初始埃坡霉素产物。 由此获得的C1-C15初始埃坡霉素产物可以根据已知方法进行反应以形成实际的活性成分。 此外，本发明涉及相应的C1-C12片段。