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    • 12. 发明授权
    • Process for producing a polyoxyalkylene derivatives substituted with
succinimidyl group
    • 用琥珀酰亚胺基取代的聚氧化烯衍生物的制造方法
    • US5872191A
    • 1999-02-16
    • US867985
    • 1997-06-03
    • Kouzoh SanchikaTohru YasukohchiKei-ichi MaruyamaSyunsuke Ohhashi
    • Kouzoh SanchikaTohru YasukohchiKei-ichi MaruyamaSyunsuke Ohhashi
    • C07D207/46C08G65/32C08G65/329C08G65/332C08G65/333C08L71/02
    • C08G65/329C08G65/33337
    • A process for producing a polyoxyalkylene derivative substituted with succinimidyl group which comprises reacting a polyoxyalkylene compound having carboxyl group at ends with N-hydroxysuccinimide in an inert solvent in the presence of dicyclohexylcarbodiimide; dissolving an obtained reaction product into chloroform, an amount by weight of chloroform being 0.5 to 10 times as much as an amount by weight of the polyoxyalkylene compound having carboxyl group at ends; and crystallizing the polyoxyalkylene derivative substituted with succinimidyl group by adding an aliphatic hydrocarbon having 5 to 8 carbon atoms to a resultant solution, an amount by weight of the aliphatic hydrocarbon being 2 to 10 times as much as an amount by weight of chloroform. Materials can be handled with safety, and a highly pure polyoxyalkylene derivative substituted with succinimidyl group which does not cause turbidity in an aqueous solution and has an excellent quality as a material for drugs can be produced.
    • 一种制备被琥珀酰亚胺基取代的聚氧化烯衍生物的方法,包括在二环己基碳二亚胺的存在下,在惰性溶剂中使具有羧基的聚氧化烯化合物与N-羟基琥珀酰亚胺反应; 将得到的反应产物溶解在氯仿中,氯仿的重量为末端具有羧基的聚氧化烯化合物的重量的0.5〜10倍; 并通过向所得溶液中加入碳原子数为5〜8的脂肪族烃而使被琥珀酰亚胺基取代的聚氧化烯衍生物结晶化,所述脂肪族烃的重量比为氯仿的2〜10倍。 可以安全地处理材料,并且可以制备用琥珀酰亚胺基取代的高纯度聚氧化烯衍生物,其不会在水溶液中引起浊度并且具有作为药物的材料的优良品质。
    • 18. 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。