N-ACETYLCARBOXYMETHYLCHITOSAN DERIVATIVE AND PRODUCTION THEREOF
    1.
    发明授权
    N-ACETYLCARBOXYMETHYLCHITOSAN DERIVATIVE AND PRODUCTION THEREOF 失效
    N-乙酰半胱氨酸衍生物及其生产方法

    公开(公告)号:EP0544000B1

    公开(公告)日:1997-05-02

    申请号:EP91914632.4

    申请日:1991-08-16

    IPC分类号: C08B37/08 C08B37/00 A61K47/48

    CPC分类号: C08B37/003

    摘要: A novel N-acetylcarboxymethylchitosan derivative represented by general formula (I) and having the following properties (1) to (4): (1) degree of carboxymethylation: 0.5 - 1.2, (2) molecular weight (according to gel filtration): 3,000 - 300,000, (3) a/(a+b): 0.01 - 1 wherein a = a1 + a2, (4) P/X (by mole): 0.1 - 1. Formula (I), wherein R1 and R2 represent each hydrogen or carboxymethyl; P represents R3CO, R4NH or R5O; Q represents hydrogen or hydroxy; X represents a peptide chain containing 1 to 10 same or different amino acid residues; R3COOH, R4NH2 and R5OH represent carboxylic acid, amine and alcohol compounds, respectively; a1 and a2 represent each 0 or a positive integer except for the case where both of them are 0 at the same time; and b represents a positive integer. When the P group in the formula (I) represents a group derived from a pharmaceutical compound, the substance of the formula (I) is useful as a drug improved in the directivity toward a target organ.

    摘要翻译: (1)〜(4)所示的新型N-乙酰羧甲基壳聚糖衍生物:(1)羧甲基化度:0.5〜1.2,(2)分子量(根据凝胶过滤):3,000 式(I)中,R 1和R 2分别表示 - ( - ) - 300,000,(3)a /(a + b):0.01-1其中a = a1 + a2,(4)P / 氢或羧甲基; P表示R3CO,R4NH或R5O; Q代表氢或羟基; X代表含有1至10个相同或不同氨基酸残基的肽链; R 3 COOH,R 4 NH 2和R 5 OH分别代表羧酸,胺和醇化合物; 除了两者同时为0的情况之外,a1和a2分别表示0或正整数; b表示正整数。 当式(I)中的P基团表示来源于药物化合物的基团时,式(I)的物质可用作改善靶器官指向性的药物。

    N-ACETYLCARBOXYMETHYLCHITOSAN DERIVATIVE AND PRODUCTION THEREOF
    2.
    发明公开
    N-ACETYLCARBOXYMETHYLCHITOSAN DERIVATIVE AND PRODUCTION THEREOF 失效
    N-乙酰半胱氨酸衍生物及其生产方法

    公开(公告)号:EP0544000A1

    公开(公告)日:1993-06-02

    申请号:EP91914632.4

    申请日:1991-08-16

    IPC分类号: C08B37/08 C08B37/00 A61K47/48

    CPC分类号: C08B37/003

    摘要: A novel N-acetylcarboxymethylchitosan derivative represented by general formula (I) and having the following properties (1) to (4): (1) degree of carboxymethylation: 0.5 - 1.2, (2) molecular weight (according to gel filtration): 3,000 - 300,000, (3) a/(a+b) : 0.01 - 1 wherein a = a₁ + a₂ , (4) P/X (by mole): 0.1 - 1. Formula (I), wherein R₁ and R₂ represent each hydrogen or carboxymethyl; P represents R₃CO, R₄NH or R₅O; Q represents hydrogen or hydroxy; X represents a peptide chain containing 1 to 10 same or different amino acid residues; R₃COOH, R₄NH₂ and R₅OH represent carboxylic acid, amine and alcohol compounds, respectively; a₁ and a₂ represent each 0 or a positive integer except for the case where both of them are 0 at the same time; and b represents a positive integer. When the P group in the formula (I) represents a group derived from a pharmaceutical compound, the substance of the formula (I) is useful as a drug improved in the directivity toward a target organ.

    摘要翻译: (1)〜(4)所示的新型N-乙酰羧甲基壳聚糖衍生物:(1)羧甲基化度:0.5〜1.2,(2)分子量(根据凝胶过滤):3,000 式(I)中,R 1和R 2分别代表各自独立的碳原子数为1〜3的(a),(b), 氢或羧甲基; P代表R 3 CO,R 4 NH或R 5 O; Q代表氢或羟基; X代表含有1至10个相同或不同氨基酸残基的肽链; R 3 COOH,R 4 NH 2和R 5 OH分别代表羧酸,胺和醇化合物; a 1和a 2分别代表0或正整数,除了它们两者同时为0的情况; b表示正整数。 当式(I)中的P基团表示来源于药物化合物的基团时,式(I)的物质可用作改善靶器官指向性的药物。