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    • 11. 发明授权
    • Phospholipid derivative
    • 磷脂衍生物
    • US07399877B2
    • 2008-07-15
    • US10549630
    • 2004-03-19
    • Chika ItohSyunsuke OhhashiKazuhiro KuboTohru YasukohchiHiroshi KikuchiNorio SuzukiMiho TakahashiHitoshi Yamauchi
    • Chika ItohSyunsuke OhhashiKazuhiro KuboTohru YasukohchiHiroshi KikuchiNorio SuzukiMiho TakahashiHitoshi Yamauchi
    • C07F9/02
    • 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
    • 17. 发明申请
    • Polyalkylene glycol derivative and modified bio-related substance
    • 聚亚烷基二醇衍生物和改性生物相关物质
    • US20060115450A1
    • 2006-06-01
    • US11142683
    • 2005-06-02
    • Ken-ichiro NakamotoSyunsuke OhashiYuji YamamotoKenji SakanoueChika ItohTohru Yasukohchi
    • Ken-ichiro NakamotoSyunsuke OhashiYuji YamamotoKenji SakanoueChika ItohTohru Yasukohchi
    • A61K31/765C08F283/00
    • C08G65/2609A61K47/48215A61K47/60C08G65/329C08G65/333
    • A polyalkylene glycol derivative containing a compound of the formula (1): wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are each an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, the groups represented by OA2 are the same or different from each other in one molecule, m is an average number of moles of the above oxyalkylene group added, m represents 10 to 1000, X represents a functional group capable of chemically reacting with a bio-related substance, and Y is a linker and represents an ether bond, an amide bond, a urethane bond, an ester bond, a secondary amino group, a carbonate bond, or an alkylene group containing these bonds, polydispersity Mw/Mn of the above polyalkylene glycol derivative in gel permeation chromatography satisfying the following relationship: Mw/Mn≦1.08 wherein Mw represents a weight average molecular weight and Mn represents a number average molecular weight.
    • 含有式(1)化合物的聚亚烷基二醇衍生物:其中R为碳原子数为1〜24的烃基,OA 1和O 2各自为氧化烯 具有2至4个碳原子的基团,由R表示的基团在一个分子中彼此相同或不同,在一个分子中由OA 2表示的基团彼此相同或不同, m是上述氧化烯基的平均加成摩尔数,m表示10〜1000,X表示与生物相关物质发生化学反应的官能团,Y为连接基,表示醚键,酰胺键 氨基甲酸酯键,酯键,仲氨基,碳酸酯键或含有这些键的亚烷基,上述聚亚烷基二醇衍生物在凝胶渗透色谱中的多分散性Mw / Mn满足以下关系: -formulae description =“In-line Formulas”end =“lead”?> Mw / Mn <= 1.08 < in-line-formula description =“In-line Formulas”end =“tail”?>其中Mw表示重均分子量,Mn表示数均分子量。