Blood-pool selective carrier for lipophilic imaging agents
    3.
    发明授权
    Blood-pool selective carrier for lipophilic imaging agents 失效
    用于亲脂显像剂的血液池选择性载体

    公开(公告)号:US06645463B1

    公开(公告)日:2003-11-11

    申请号:US09058715

    申请日:1998-04-10

    IPC分类号: A61K5100

    摘要: A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.

    摘要翻译: 用作脂溶性成像剂或水溶性成像剂的亲脂性衍生物的血液池选择性递送载体的表面改性脂蛋白样水包油乳液。 血液池选择性输送载体在血液中保持数小时,显示出非常少的早期肝脏螯合,并在24小时内从血液中清除。 油相的平均直径小于150nm,其最小化网状内皮系统的螯合。 用聚乙二醇修饰的磷脂修饰油相的表面以防止与肝细胞的受体位点的正常相互作用。 放射摄影成像中,放射性或稳定的合成或半合成多卤甘油三酸酯如2-油酰甘油-1,3-双[7-(3-氨基-2,4,6-三碘苯基)庚酸酯]或脂溶性衍生物 的传统的水溶性造影剂,如碘,脂肪族和代谢酸的脂肪族酯可以并入脂蛋白样乳液颗粒的亲脂性核心中。

    Blood-pool carrier for lipophilic imaging agents
    9.
    发明授权
    Blood-pool carrier for lipophilic imaging agents 失效
    用于亲脂显像剂的血液池载体

    公开(公告)号:US07582279B2

    公开(公告)日:2009-09-01

    申请号:US10692311

    申请日:2003-10-23

    IPC分类号: A61K51/00 A61M36/14

    摘要: A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.

    摘要翻译: 用作脂溶性成像剂或水溶性成像剂的亲脂性衍生物的血液池选择性递送载体的表面改性脂蛋白样水包油乳液。 血液池选择性输送载体在血液中保持数小时,显示出非常少的早期肝脏螯合,并在24小时内从血液中清除。 油相的平均直径小于150nm,其最小化网状内皮系统的螯合。 用聚乙二醇修饰的磷脂修饰油相的表面以防止与肝细胞的受体位点的正常相互作用。 放射摄影成像中,放射性或稳定的合成或半合成多卤甘油三酸酯如2-油酰甘油-1,3-双[7-(3-氨基-2,4,6-三碘苯基)庚酸酯]或脂溶性衍生物 的传统的水溶性造影剂,如碘,脂肪族和代谢酸的脂肪族酯可以并入脂蛋白样乳液颗粒的亲脂性核心中。

    Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use
    10.
    发明申请
    Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use 有权
    磷脂醚硼酸和酯的组合物及其合成和使用方法

    公开(公告)号:US20090018357A1

    公开(公告)日:2009-01-15

    申请号:US12156258

    申请日:2008-05-30

    IPC分类号: C07F5/02 A61K31/69 A61P35/00

    CPC分类号: C07F9/106 C07F9/094

    摘要: The present invention discloses boronic acids and esters of phospholipid ether analogs and methods for their synthesis and use. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells.

    摘要翻译: 本发明公开了硼酸和磷脂醚类似物的酯类及其合成和使用方法。 本文所述的磷酸酯类似物的硼酸和酯可用于治疗癌症,特别是可以与放射治疗结合使用,例如外部束放射治疗和中子俘获治疗以特异性靶向和杀死癌细胞。