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    Pradimicin derivatives
    2.
    发明公开
    Pradimicin derivatives 失效
    普拉定霉素衍。

    公开(公告)号：EP0428132A1

    公开(公告)日：1991-05-22

    申请号：EP90121709.1

    申请日：1990-11-13

    申请人： Bristol-Myers Squibb Company

    发明人： Kamachi, Hajime ,  Iimura, Seiji ,  Okuyama, Satsuki ,  Aburaki, Shimpei ,  Naito, Takayuki ,  Ueda, Yasutsugu ,  Crast, Leonard B., Jr. ,  Mikkilineni, Amarendra B.

    IPC分类号： C07H15/244 ,  A61K31/71

    CPC分类号： C07H15/244

    摘要： The present invention provides pradimicin analogs of formula (II) which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.
    wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid has the D -configuration;
    R² is H or β-D-xylosyl;
    R³ is H or methyl; and
    R⁴ is selected from the group consisting of (C₂₋₅)alkenyl; (C₂₋₅)alkynyl; substituted (C₁₋₅)alkyl; substituted (C₂₋₅)alkenyl; wherein the substituent for both the alkyl and alkenyl is a group selected from the group consisting of, carboxy, (C₁₋₅)alkoxycarbonyl, carbamyl, (C₁₋₅)alkylcarbamyl, di(C₁₋₅)alkylcarbamyl, and sulfonyl; (C₁₋₅)alkanoyl substituted with a group selected from the group consisting of amino, (C₁₋₅)alkylamino, and di(C₁₋₅)alkylamino; L-glutamyl; formyl; benzyl; and p-tolylsulfonylcarbamyl; or
    a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供了相对于母体化合物表现出改善的水溶性的式（II）的普拉迪霉素类似物。 这些新型药剂可用于治疗真菌感染。 其中R 1选自H，甲基和羟甲基，当R 1为甲基或羟甲基时，得到的氨基酸具有D-构型; R 2是H或β-D-木糖基; R 3是H或甲基; 和R 4选自（C 2-5）烯基; （C 2-5）炔基; 取代的（C 1-5）烷基; 取代的（C2-5）烯基; 其中烷基和链烯基的取代基是选自羧基，（C 1-5）烷氧基羰基，氨基甲酰基，（C 1-5）烷基氨基甲酰基，二（C 1-5）烷基氨基甲酰基和磺酰基的基团。 被选自氨基，（C 1-5）烷基氨基和二（C 1-5）烷基氨基的基团取代的（C 1-5）烷酰基; L-谷氨酰; 甲酰基; 苄基; 和对甲苯磺酰基氨基甲酰基; 或其药学上可接受的盐。