发明名称 Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain
摘要 This invention describes the new 17alpha-fluoroalkyl steroids of general formula I in which R<1 >stands for a methyl or ethyl group, R<2 >stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R<3 >stands for a free, etherified or esterified hydroxy group, R<4 >and R<5 >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 R<6 >means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R<7 >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 R<6 >and R<7 >together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping =N-OH or two hydrogen atoms, R<8 >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, -NR<9a>R<9b>, -NHSO2R<9>, -CO2R<9>, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R<9a >and R<9b >are the same or different and in the same way as R<9 >represent a hydrogen atom or a C1-C10 alkyl group, and for -NR<9a>R<9b >radicals, as well as their physiologically compatible salts with acids and for -CO2R<9 >radicals with R<9 >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 US2005080060(A1) 申请公布日期 2005.04.14
申请号 US20040948652 申请日期 2004.09.24
申请人 SCHWEDE WOLFGANG;CLEVE ARWED;KLAR ULRICH;NEEF GUNTER;CHWALISZ KRISTOF;SCHNEIDER MARTIN;FUHRMANN ULRIKE;HEB-STUMPP HOLGER 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):A61K31/56 主分类号 A61K31/56
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