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    • 10. 发明授权
    • 9-Fluoroprostaglandin derivatives, and use as medicinal agents
    • 9-氟前列腺素衍生物,用作药物
    • US4454339A
    • 1984-06-12
    • US395448
    • 1982-07-06
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • A61K31/557A61K31/5575A61P43/00C07C67/00C07C401/00C07C405/00C07C177/00
    • C07C405/00C07C405/0016C07C405/0041
    • 9-Fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.-position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.
    • 其中R 1是CH 2 OH或其中R 2是氢,烷基,环烷基,芳基或杂环残基的式I的1-氟代衍生物(Ⅰ) 或R1是残基,其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-,B是-CH2-CH2-,反式-CH = CH-或-C3BOND C,W是游离的或官能改性的羟基亚甲基,其中OH基可以是α-或β-位,D和E共同是直接键,或D是1-10的直链或支链亚烷基或亚烯基 可以任选被氟原子取代的碳原子,E是氧或硫,直接键,-C 3 D或-CR 6 = CR 7 - ,其中R 6和R 7彼此不同,各自是氢,氯或烷基 R4是游离的或官能改性的羟基,R5是氢,任意取代的脂族基团,例如烷基或卤代取代的烷基,环烷基,任选取代的芳基或杂环基,当R 2是H时,其生理上相容的盐 具有碱性,具有有价值的药理学性质,例如作为纤溶素或流产。