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    • 45. 发明申请
    • NOVEL MANGANESE COMPRISING NANOSTRUCTURES
    • 包含纳米结构的新型锰
    • WO2013041623A1
    • 2013-03-28
    • PCT/EP2012/068541
    • 2012-09-20
    • SPAGO IMAGING AB
    • AXELSSON, OskarPETORAL JR., Rodrigo M.EK, FredrikLAURITZSON, Petter
    • A61K49/12A61K49/18B82Y5/00B82Y15/00
    • A61K51/065A61K49/12A61K49/124A61K49/128A61K49/1818A61K49/1857B82Y5/00B82Y15/00C08G73/0206C08G73/0213
    • Disclosed herein are nanostructures comprising a polymeric framework comprising at least five geminal bisphosphonate groups, wherein the geminal bisphosphonate groups independently of each other are incorporated as - R 3 R 4 C(P=O(OR 1 )(OR 2 )) 2 , wherein R 1 and R 2 are independently selected from the group consisting of a negative charge, H, alkyl and aryl, and wherein at least one of R 3 and R 4 is a group connected to the polymeric framework with the proviso that when only one of R 3 and R 4 is such a connected group, the other of R 3 and R 4 is either a group being able to connect to the polymeric framework, or the residue of such a group, or selected from the group consisting of H, OH, OR 5 and R 5 , wherein R 5 is a lower alkyl. The polymeric framework may comprise manganese ions. Disclosed are also methods for producing such manganese containing nanostructures, compositions comprising such manganese containing nanostructures and use of such manganese con¬ taining nanostructures, i.a. as MRI contrasting agents.
    • 本文公开了包含包含至少五个偕二膦酸酯基团的聚合物骨架的纳米结构,其中偕双膦酸酯基团彼此独立地并入作为-R 3 R 4 C(P = O(OR 1)(OR 2))2),其中R 1和R 2独立地选自 由负电荷,H,烷基和芳基组成的组,并且其中R 3和R 4中的至少一个是与聚合物骨架连接的基团,条件是当只有R3和R4之一是这样的连接基团时, R3和R4中的另一个是能够连接到聚合物骨架的基团,或这种基团的残基,或选自H,OH,OR 5和R 5,其中R 5是低级烷基。 聚合物骨架可以包含锰离子。 还公开了生产这种含锰纳米结构的方法,包含这种含锰纳米结构的组合物和使用这种含有纳米结构的锰,例如, 作为MRI造影剂。
    • 48. 发明申请
    • APTAMER LABELED WITH F-19 NUCLEUS FOR TARGETED MOLECULAR IMAGING BY MRI
    • 标有F-19核子的APTAMER通过MRI进行靶向分子成像
    • WO2012076191A1
    • 2012-06-14
    • PCT/EP2011/006255
    • 2011-12-12
    • MERCK PATENT GMBHGUENTHER, RalfHOCK, BjoernGOODMAN, SimonPIATER, Birgit
    • GUENTHER, RalfHOCK, BjoernGOODMAN, SimonPIATER, Birgit
    • A61K49/12
    • C12N15/115A61K49/12A61K49/126
    • Magnetic Resonance Imaging, usually based on 1 H as the magnetic nucleus, is an important diagnostic technique that is commonly used in hospitals for the diagnosis of disease. MRI allows for the non- invasive imaging of soft tissue with a superb spatial resolution. Magnetic Resonance Imaging based on 19 F instead of 1 H opens up new diagnostic possibilities. The 19 F nucleus has a high gyromagnetic ratio (40 MHz/T) and a natural isotopic abundance ratio of 100%. In the human body, 19 F containing structures are exclusively present in the form of solid salts in e.g. teeth and bones. As a consequence, the J2 relaxation times of the endogenous 19 F atoms are extremely short and the MR signal is hardly detectable, in other words, the lack of endogenous, 19 F-based structures with relatively high transverse relaxation times assures a very low background MR signal. Therefore, exogenous 19 F-based MRI contrast agents allow for "hot spot" imaging in a way similar to other techniques such as PET (positron emission tomography). As a useful extension of its diagnostic use, MRI is also proposed for the monitoring of the delivery of bio-active agents such as therapeutic or diagnostic agents. I.e., MRI can not only be used for treatment planning, but also to control local drug delivery under image guidance.
    • 磁共振成像通常以1H为磁核,是医院常用于诊断疾病的重要诊断技术。 MRI允许具有极好的空间分辨率的软组织的非侵入性成像。 基于19F而不是1H的磁共振成像开辟了新的诊断可能性。 19F核具有高回旋比(40MHz / T)和100%的天然同位素丰度比。 在人体中,含有19F的结构仅以例如固体盐的形式存在。 牙齿和骨头。 因此,内源性19F原子的J2松弛时间非常短,并且MR信号几乎不可检测,换句话说,缺乏具有相对较高的横向弛豫时间的内源性19F基结构,确保非常低的背景MR信号 。 因此,外源性基于19F的MRI造影剂允许以与PET(正电子发射断层摄影)等其他技术相似的方式进行“热点”成像。 作为其诊断用途的有用扩展,还提出了用于监测生物活性剂如治疗剂或诊断剂的递送的MRI。 即,MRI不仅可以用于治疗计划,还可以在图像引导下控制局部药物传播。