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    Liver-targeting agents and their synthesis
    1.
    发明授权
    Liver-targeting agents and their synthesis 有权
    肝靶向剂及其合成

    公开(公告)号：US08552163B2

    公开(公告)日：2013-10-08

    申请号：US12891004

    申请日：2010-09-27

    Applicant: Reiko Takasaka Lee ,  Yuan-Chuan Lee ,  Mei-Hui Wang ,  Wuu-Jyh Lin

    Inventor： Reiko Takasaka Lee ,  Yuan-Chuan Lee ,  Mei-Hui Wang ,  Wuu-Jyh Lin

    IPC: C07H17/02 ,  C07C229/00

    CPC classification number: C07H15/04

    Abstract: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilotriacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 molecules of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

    Abstract translation: 本发明提供新型肝靶向剂及其合成方法。 公开了以赖氨酸的次氮基三乙酸结构作为骨架的肝靶向剂，其以糖基取代多价，与半乳糖胺链或乳糖链结合。 特别地，仅涉及一个氨基酸L-赖氨酸以提供三价值。 Nepsilon-苄氧基羰基-Nalpha-二羧甲基-L-赖氨酸中的所有羧基可以在一个步骤中与ahGalNAc或ahLac的三种糖苷缀合。 本发明还提供了六乳糖苷。 特别地，TFA-AHA-Asp用于结合2分子的NTA（ahLac）3。 本发明还提供了一种在NTA和DTPA之间添加间隔物的方法。 延长的肝细胞特异性糖配体比未延长的肝细胞特异性糖配体具有更高的111In-放射性标记产率。

    RADIOLABELING METHOD USING MULTIVALENT GLYCOLIGANDS AS HEPATIC RECEPTOR IMAGING AGENT
    3.
    发明申请
    RADIOLABELING METHOD USING MULTIVALENT GLYCOLIGANDS AS HEPATIC RECEPTOR IMAGING AGENT 审中-公开
    使用多种甘氨酸作为胃肠吸收成像剂的放射性标记方法

    公开(公告)号：US20110097264A1

    公开(公告)日：2011-04-28

    申请号：US12779328

    申请日：2010-05-13

    Applicant: Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

    Inventor： Mei-Hui Wang ,  Wuu-Jyh Lin ,  Chuan-Yi Chien ,  Hung-Man Yu ,  Reiko Takasaka Lee ,  Yuan-Chuan Lee

    IPC: A61K51/08 ,  C07K5/083 ,  C07F5/00 ,  A61K51/04

    CPC classification number: A61K51/0491 ,  A61K51/0497 ,  C07F13/005 ,  C07K1/13

    Abstract: A radiolabeling method using a multivalent glycoligand as hepatic receptor imaging agent is provided. The multivalent glycoligand-DTPA derivatives (In-111-DTPA-hexa lactoside and In-111-DTPA-tri-galactosamine glycoside) labeled with In-111 are used as hepatic receptor imaging agent. The effects of imaging of a hepatic receptor in different species are evaluated, the lowest specific radioactivity values of hepatic receptor imaging required in different species are discovered. Since the specificity of the human ASGPR closely resembles that of the mouse. This kind of radiolabelling method, agent and related study about specific radioactivity could be used in clinical trial in the future.

    Abstract translation: 提供了一种使用多价糖配位体作为肝脏受体成像剂的放射性标记方法。 用In-111标记的多价甘油配体-DTPA衍生物（In-111-DTPA-hexa lactoside和In-111-DTPA-tri-galactosamine glycoside）用作肝脏受体显像剂。 对不同物种肝受体成像的影响进行了评估，发现了不同物种所需肝脏受体成像的最低比放射性值。 由于人类ASGPR的特异性与小鼠的特异性非常相似。 这种放射性标记方法，药剂和相关研究有关的放射性可以在今后的临床试验中使用。

    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS
    4.
    发明申请
    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS 有权
    新型肝脏靶向药物及其合成

    公开(公告)号：US20110077386A1

    公开(公告)日：2011-03-31

    申请号：US12891004

    申请日：2010-09-27

    Applicant: REIKO TAKASAKA LEE ,  YUAN-CHUAN LEE ,  MEI-HUI WANG ,  WUU-JYH LIN

    Inventor： REIKO TAKASAKA LEE ,  YUAN-CHUAN LEE ,  MEI-HUI WANG ,  WUU-JYH LIN

    IPC: C07H15/02 ,  C07C229/02

    CPC classification number: C07H15/04

    Abstract: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

    Abstract translation: 本发明提供新型肝靶向剂及其合成方法。 公开了以赖氨酸为基础的三乙酸结构作为骨架的肝靶向剂，其以糖基取代多价，与半乳糖胺链或乳糖链结合。 特别地，仅涉及一个氨基酸L-赖氨酸以提供三价值。 N，N-苄氧羰基-Nα-二羧甲基-L-赖氨酸中的所有羧基可以在一个步骤中与αGalNAc或ahLac的三种糖苷缀合。 本发明还提供了六乳糖苷。 特别地，TFA-AHA-Asp用于缀合2摩尔NTA（ahLac）3。 本发明还提供了一种在NTA和DTPA之间添加间隔物的方法。 延长的肝细胞特异性糖配体比未延长的肝细胞特异性糖配体具有更高的111In-放射性标记产率。

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