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    • 36. 发明申请
    • NANOSTRUCTURES AND APPLICATIONS THEREOF
    • 纳米结构及其应用
    • WO2015144891A1
    • 2015-10-01
    • PCT/EP2015/056739
    • 2015-03-27
    • SPAGO NANOMEDICAL AB
    • AXELSSON, OskarBÄCKSTRÖM, SaniaPETORAL JR, Rodrigo
    • A61K51/12A61P35/00
    • A61K51/065A61K51/1251C08G77/30
    • Disclosed herein are globular nanostructures having a hydrodynamic diameter (D h ) of 8-100 nm comprising a central part and a peripheral part, wherein said central part has a calculated diameter (D c ) of 6-90 nm and said peripheral part has an estimated thickness (T p ) so that D h =D c +2T p , wherein said central part comprises: (i) a crosslinked polymeric framework comprising monomer residues wherein at least 30 % by number of the monomer residues have crosslinked thereby forming the crosslinked polymeric framework and/or (ii) a branched polymeric framework comprising monomer residues wherein the number of branch points is at least 30 % of the number of monomer residues, wherein said central part comprises chelating groups of which at least 4 allow chelation of at least one multiply charged cation, wherein said chelating groups are independently selected from the group consisting of -COOR 1 , -P=O(OR 1 )(OR 2 ), and -S(=O) 2 OR 1 , wherein R 1 and R 2 are independently selected from the group consisting of a negative charge, H, and lower alkyls, and wherein said peripheral part comprises a synthetic polymer material covalently attached to the central part, wherein the synthetic polymer material is hydrophilic and bioinert, and electrically neutral or zwitterionic. Also disclosed are compositions comprising such nanoparticles, and optionally also a radionuclide, use of such compositions, kits containing such compositions and methods for obtaining such compositions.
    • 本文公开了具有8-100nm的流体动力学直径(Dh)的球状纳米结构,其包括中心部分和周边部分,其中所述中心部分具有6-90nm的计算直径(Dc),并且所述周边部分具有估计的厚度 (Tp),使得Dh = Dc + 2Tp,其中所述中心部分包​​含:(i)包含单体残基的交联聚合物骨架,其中至少30%数量的单体残基已经交联从而形成交联的聚合物骨架和/或 ii)包含单体残基的支化聚合物框架,其中分支数目为单体残基数量的至少30%,其中所述中心部分包​​含螯合基团,其至少4个允许螯合至少一个多电荷阳离子,其中 所述螯合基团独立地选自-COOR1,-P = O(OR1)(OR2)和-S(= O)2OR1,其中R1和R2独立地选自: 负电荷,H和低级烷基,并且其中所述外围部分包括共价连接到中心部分的合成聚合物材料,其中合成聚合物材料是亲水的和生物惰性的,并且是电中性的或两性离子的。 还公开了包含这样的纳米颗粒,任选地还有放射性核素的组合物,这种组合物的使用,含有这些组合物的试剂盒和获得这种组合物的方法。
    • 38. 发明申请
    • METHOD OF TREATING CANCER
    • 治疗癌症的方法
    • WO2014040143A1
    • 2014-03-20
    • PCT/AU2013/001059
    • 2013-09-17
    • GRAY, Bruce N.
    • GRAY, Bruce N.
    • A61K51/12A61K103/32A61K103/00A61K103/30A61P35/00
    • A61K51/1251A61K51/025A61K51/06Y10T428/2982
    • The present invention relates to small particles comprising a radionuclide and in particular to small particles comprising a radionuclide for implantation in organs or tissues or tumours of subjects. Embodiments of the invention have been particularly developed for embolisation into the arterial system using a technique known as radioembolisation or Selective Internal Radiation Therapy (SIRT) and will be described hereinafter with reference to this application. However, it will be appreciated that the invention is not limited to this particular field of use. The small particles are preferably radioactive microspheres comprising a matrix and a radionuclide stably attached. These microspheres have a diameter ranging from 5 to 45 μπι and the radionuclide has a specific activity ranging from 100 to 2000 Bq per microsphere.
    • 本发明涉及包含放射性核素的小颗粒,特别涉及包含用于植入受试者的器官或组织或肿瘤中的放射性核素的小颗粒。 本发明的实施例已经特别开发用于使用已知为放射栓塞或选择性内部放射治疗(SIRT)的技术栓塞入动脉系统,并且将在下文中参考本申请进行描述。 然而,应当理解,本发明不限于该特定的使用领域。 小粒子优选为包含基质和稳定连接的放射性核素的放射性微球。 这些微球的直径范围为5至45μ,而每个微球的放射性核素的比活性为100至2000Bq。