Polyiodinated triglyceride analogs as radiologic agents
    11.
    发明授权
    Polyiodinated triglyceride analogs as radiologic agents 失效
    多碘化甘油三酯类似物作为放射剂

    公开(公告)号:US4957729A

    公开(公告)日:1990-09-18

    申请号:US358865

    申请日:1989-05-30

    摘要: Novel iodinated arylaliphatic triglyceride analogs as radiologic agents are liver and hepatocyte site-specific. The triglyceride backbone structure is preferably 1,3-disubstituted or 1,2,3-trisubstituted with, in some embodiments, a 3-substituted-2,4,6-triiodophenyl aliphatic chain wherein the chain has a structure similar to naturally occuring fatty acids. In another embodiment, a monoiodophenyl aliphatic chain is utilized. Any position remaining on the triglyceride backbone is substituted with a saturated or unsaturated aliphatic hydrocarbon chain of the type found in naturally occurring fatty acids. The triglyceride analogs can be radioiodinated. In a preferred embodiment, a lipid emulsion is provided as the carrier vehicle.

    摘要翻译: 新型碘化芳基脂肪酸甘油三酯类似物作为放射剂是肝脏和肝细胞位点特异性。 甘油三酯主链结构优选在一些实施方案中被3-取代-2,4,6-三碘苯基脂族链进行1,3-二取代或1,2,3-三取代,其中链的结构类似于天然存在的脂肪 酸。 在另一个实施方案中,使用单碘苯基脂族链。 在甘油三酯主链上残留的任何位置被天然存在的脂肪酸中所发现类型的饱和或不饱和脂族烃链所取代。 甘油三酯类似物可以放射性碘化。 在优选的实施方案中,提供脂质乳剂作为载体载体。

    Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use
    18.
    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。

    Method for the synthesis of phospholipid ethers
    20.
    发明授权
    Method for the synthesis of phospholipid ethers 有权
    磷脂醚合成方法

    公开(公告)号:US07893286B2

    公开(公告)日:2011-02-22

    申请号:US12156287

    申请日:2008-05-30

    IPC分类号: C07F9/02

    CPC分类号: C07F9/10

    摘要: Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

    摘要翻译: 公开了用于合成磷脂醚类似物和烷基磷酸胆碱类似物的改进方法。 所述方法允许所用反应物具有更大的通用性,并且更容易合成不同长度的烷基链,同时在室温或更低温度下提供反应温度。 本文公开的方法提供使用烷基卤和有机锌试剂的反应物和条件,因此不利用Gringard反应,从而更容易地分离和纯化产物。 通过本文公开的方法合成的PLE化合物也可用于合成高比活性磷脂醚(PLE)类似物,用于治疗和诊断癌症。