发明名称 Antigestagenically active steroids with a fluorinated 17-alpha-alkyl chain
摘要 This invention describes the new 17a-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, alkyl, 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.
申请公布号 US2002045774(A1) 申请公布日期 2002.04.18
申请号 US20010978689 申请日期 2001.10.18
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 SCHWEDE WOLFGANG;CLEVE ARWED;KLAR ULRICH;NEEF GUNTER;CHWALISZ KRISTOF;SCHNEIDER MARTIN;FUHRMANN ULRIKE;HEB-STUMPP HOLGER
分类号 A61K31/56;A61P5/36;C07J1/00;C07J41/00;C07J43/00;C07J53/00;(IPC1-7):C07J53/00;C07J5/00;C07J7/00 主分类号 A61K31/56
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