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    Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof
    2.
    发明公开
    Fluorine-containing anthracycline derivatives having hydroxyl group(s) mono- or di-o-aminoalkanoylated in the sugar moiety thereof 失效
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    公开(公告)号：EP0761678A1

    公开(公告)日：1997-03-12

    申请号：EP96420288.1

    申请日：1996-09-06

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Takeuchi, Tomio, New Fuji Mansion 701, 1-11 ,  Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Takagi, Yasushi ,  Sohtome, Hiromi

    IPC分类号： C07H15/252 ,  A61K31/70

    CPC分类号： C07H15/252

    摘要： To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-O-(2,6-dideoxy-2-fluoro-3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-α-L-talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-O-(3-O- or -4-O-or -3,4-di-O-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetrafluoro-α-L-talopyranosyl- or -2,6-dideoxy-6,6,6-trifluoro-α-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:-

    wherein either one or both of A 1 and A 2 is or are an α-amino acid residue or an ω-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine-containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.

    摘要翻译： 为了提供具有高抗肿瘤活性和在水中的溶解性的新型含氟蒽环类衍生物，现在已经合成了7-O-（2,6-二脱氧-2-氟-3-O-或-4-O-或 -3,4-二-O-氨基链烷酰-α-L-吡喃葡萄糖基）道诺霉素酮或下列通式（I）的阿霉素酮，以及7-O-（3-O-或-4-O- -3,4-二-O-氨基烷酰基-2,6-二脱氧-2,6,6,6-四氟-α-L-吡喃木糖基或-2,6-二脱氧-6,6,6-三氟-α -L-赖肟基 - 六吡喃糖基）阿霉素酮，其如下所示： - CHEM>其中A 1和A 2中的任一个或两者是或是α-氨基酸残基或 ω-氨基酸残基，T表示氟或氢原子。 通式（I）和（II）的新型含氟蒽环类衍生物对肿瘤和水溶性高度有活性，可用作以可注射溶液形式给药的抗肿瘤剂。