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    Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain
    1.
    发明申请
    Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain 失效
    具有氟化17α-烷基链的抗发生活性类固醇

    公开(公告)号：US20050080060A1

    公开(公告)日：2005-04-14

    申请号：US10948652

    申请日：2004-09-24

    申请人： Wolfgang Schwede ,  Arwed Cleve ,  Ulrich Klar ,  Gunter Neef ,  Kristof Chwalisz ,  Martin Schneider ,  Ulrike Fuhrmann ,  Holger Heb-Stumpp

    发明人： Wolfgang Schwede ,  Arwed Cleve ,  Ulrich Klar ,  Gunter Neef ,  Kristof Chwalisz ,  Martin Schneider ,  Ulrike Fuhrmann ,  Holger Heb-Stumpp

    IPC分类号： A61K31/56 ,  A61P5/36 ,  C07J1/00 ,  C07J41/00 ,  C07J43/00 ,  C07J53/00

    CPC分类号： C07J1/0033 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003 ,  C07J53/002

    摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ═N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen atom, an —OH, —NO2, —N3, —CN, —NR9aR9b, —NHSO2R9, —CO2R9, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R9a and R9b are the same or different and in the same way as R9 represent a hydrogen atom or a C1-C10 alkyl group, and for —NR9aR9b radicals, as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.

    摘要翻译： 本发明描述了通式I的新型17α-氟烷基类固醇，其中R 1代表甲基或乙基，R 2代表式C n F m H o基团，其中n为2,3,4,5或 6，m> 1和m + o = 2n + 1，R 3表示游离的醚化或酯化的羟基，R 4和R 5各自代表氢原子，或一起代表另外的 键或亚甲基，St代表部分式A，B或C的甾族ABC-环体系，其中R 6表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基 或卤素原子，R 7表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基，或者如果St代表甾族ABC环系统A或B，另外R R 6和R 7一起可以表示另外的键，X表示氧原子，羟基亚氨基= N-OH或两个氢原子，R 8表示任意取代的基团Y或芳基 几个地方有一个Y组，Y是一个 氢原子，卤素原子，-OH，-NO 2，-N 3，-CN，-NR 9a R 9b，-NHSO 2 R 9，-CO 2 R 9，C 1 -C 10烷氧基，C 1 -C 10 烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟烷基或苯甲酰基，R 9a和R 9b相同或不同，并且R 9表示氢原子或C1- C10烷基，对于-NR 9a R 9b基团，以及它们与酸的生理上相容的盐以及具有R 9表示氢的-CO 2 R 9基团，以及它们与 基地 新化合物具有非常强的抗前体作用，适用于制备药物制剂。