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    • 35. 发明申请
    • Phospolipid derivative
    • 磷脂衍生物
    • US20070031481A1
    • 2007-02-08
    • US10549630
    • 2004-03-19
    • Chika ItohSyunsuke OhhashiKazuhiro KuboTohru YasukohchiHiroshi KikuchiNorio SuzukiMiho TakahashiHitoshi Yamauchi
    • Chika ItohSyunsuke OhhashiKazuhiro KuboTohru YasukohchiHiroshi KikuchiNorio SuzukiMiho TakahashiHitoshi Yamauchi
    • A61K9/127A61K31/685C07F9/02
    • A61K9/127C07F9/10C11D1/345
    • A phospholipid derivative represented by the following formula (I) wherein R1CO and R2CO independently represent an acyl group; R3 represents hydrogen atom, or a hydrocarbon group; symbol “a” represents an integer of 0 to 4; symbol “b” represents 0 or 1, provided that when a is 0, b is 0; X represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium; A1O and A3O represent an oxyalkylene group containing oxyethylene group, wherein the ratio of the oxyethylene group to the oxyalkylene group in A1O and A3O is 0.5 or larger in terms of a weight ratio; A2O represents an oxyalkylene group; symbols “m” and “q” represent an average molar number of added oxyalkylene groups; and symbol “n” represent an average molar number of added oxyalkylene groups; provided that m, n and q satisfy the following conditions: 5≦m≦600, 1≦n≦45, 0≦q≦200, 10≦m+n+q≦600, 0.04≦n/(m+n+q), and q/(m+n+q)≦0.8, which can thicken the water shell of liposome surface by suppressing the spreading of the polyalkylene oxide structure on the surface and thus increase stability of the liposome.
    • 由下式(I)表示的磷脂衍生物,其中R 1 CO和R 2 CO独立地表示酰基; R 3表示氢原子或烃基; 符号“a”表示0〜4的整数, 符号“b”表示0或1,条件是当a为0时,b为0; X表示氢原子,碱金属原子,铵或有机铵; A 1 O和A 3 O表示含氧化乙烯基的氧化烯基,其中A 1 O 3中的氧乙烯基与氧化烯基的比例 O和A 3 O以重量比计为0.5以上; O 2表示氧化烯基; 符号“m”和“q”表示加成的氧化烯基团的平均摩尔数; 符号“n”表示加成的氧化烯基的平均摩尔数; 条件是m,n和q满足以下条件:5 <= m <= 600,1 <= n <= 45,0 <= q <= 200,10 <= m + n + q <= 600,0.04 < = n /(m + n + q)和q /(m + n + q)<= 0.8,这可以通过抑制聚环氧烷结构在表面上的扩散而增加脂质体表面的水壳,从而增加稳定性 的脂质体。