Polymerization method for the synthesis of polypeptide imaging agents
    62.
    发明申请
    Polymerization method for the synthesis of polypeptide imaging agents 失效
    用于合成多肽成像剂的聚合方法

    公开(公告)号:US20060104908A1

    公开(公告)日:2006-05-18

    申请号:US10987662

    申请日:2004-11-12

    IPC分类号: A61K49/14 C07K1/02 C07F5/00

    摘要: A method for synthesizing extended poly(amino acids) conjugated to imaging agents, such as DTPA, is disclosed. The amino acid is initially conjugated to the imaging agent at the monomer stage, followed by formation of the corresponding N-carboxyanhydride. The method utilizes catalyzed ring opening polymerization of the N-carboxyanhydride of the amino acid-imaging agent monomer allowing the formation of a poly(amino acid) backbone having 100% imaging agent conjugation if desired. However, the present method also permits the degree of conjugation to be controlled by copolymerizing the N-carboxyanhydride of the amino acid-imaging agent monomer with one or more unconjugated monomers, i.e. N-carboxyanhydrides of the same or of other amino acids. Various imaging agents may be employed, and new hybrid random, block, and mixed copolymers may be prepared.

    摘要翻译: 公开了用于合成与显影剂缀合的延伸的聚(氨基酸)的方法,例如DTPA。 氨基酸最初在单体阶段与成像剂缀合,然后形成相应的N-羧酸酐。 该方法利用氨基酸显影剂单体的N-羧酸酐的催化开环聚合,如果需要,允许形成具有100%成像剂共轭的聚(氨基酸)主链。 然而,本方法还允许通过使氨基酸显影剂单体的N-羧酸酐与一种或多种非共轭单体,即相同或其它氨基酸的N-羧酸酐共聚来控制缀合度。 可以使用各种成像剂,并且可以制备新的杂化随机,嵌段和混合共聚物。

    Magnetic resonance contrast-enhancing agents and method for detecting and imaging artherosclerotic plaque
    64.
    发明申请
    Magnetic resonance contrast-enhancing agents and method for detecting and imaging artherosclerotic plaque 审中-公开
    磁共振对比增强剂和用于检测和成像动脉粥样硬化斑块的方法

    公开(公告)号:US20040265235A1

    公开(公告)日:2004-12-30

    申请号:US10609269

    申请日:2003-06-26

    IPC分类号: A61K049/00

    CPC分类号: A61K49/146 A61K49/085

    摘要: Magnetic resonance (nullMRnull) contrast-enhancing agents comprise poly(amino acid) backbone chain conjugated to chelating moieties that comprise a plurality of carboxylic acid groups that form coordination complexes with paramagnetic ions. A method for detecting atherosclerotic plaque areas comprises administering at least one of these contrast agents into a subject; and obtaining and comparing MR images of and MR signals from the plaque areas before and after administering the contrast agent. The method can be used to assess an effectiveness of a prescribed course of treatment for atherosclerosis.

    摘要翻译: 磁共振(“MR”)对比度增强剂包含与螯合部分结合的聚(氨基酸)主链,螯合部分包含与顺磁性离子形成配位络合物的多个羧酸基团。 用于检测动脉粥样硬化斑块区域的方法包括将这些造影剂中的至少一种施用于受试者; 并且在施用造影剂之前和之后获得和比较来自斑块区域的MR图像和MR信号。 该方法可用于评估规定的动脉粥样硬化治疗过程的有效性。

    Extended-linear polymeric contrast agents, and synthesizing methods, for medical imaging
    66.
    发明申请
    Extended-linear polymeric contrast agents, and synthesizing methods, for medical imaging 审中-公开
    扩展线性聚合造影剂,以及用于医学成像的合成方法

    公开(公告)号:US20040170562A1

    公开(公告)日:2004-09-02

    申请号:US10793376

    申请日:2004-03-04

    IPC分类号: A61K049/00 C07K014/00

    摘要: Linear extended polymeric paramagnetic chelates for use as MRI contrast agents are synthesized by conjugating DTPA chelator moieties to higher than 90% of the monomer residues of the polyamino acid backbone chain. The resulting polymer can be labeled with Gd, since each chelator moiety holds a Gd ion, and the resulting conformation is of an unfolded, extended linear type, capable of entering small pores and moving around obstacles in the extracellular space of tissues. The efficient production of these extended polymers is critical for the application of such contrast agents to medical imaging. One such agent is a reptating polymer containing technetium-99.

    摘要翻译: 用作MRI造影剂的线性延伸的聚合顺磁螯合物是通过将DTPA螯合剂部分与聚氨基酸主链的单体残基的高于90%结合而合成的。 所得到的聚合物可以用Gd标记,因为每个螯合剂部分保持Gd离子,并且所得构象是能够进入小孔并在组织的细胞外空间内的障碍物周围移动的展开的延伸线型。 这些延伸聚合物的有效生产对于将这种造影剂应用于医学成像是至关重要的。 一种这样的试剂是含有锝-99的吸收性聚合物。

    Extended-linear polymeric contrast agents, and synthesizing methods, for medical imaging

    公开(公告)号:US20040136911A1

    公开(公告)日:2004-07-15

    申请号:US10743200

    申请日:2003-12-22

    IPC分类号: A61K049/00

    摘要: Linear extended polymeric paramagnetic chelates for use as MRI contrast agents are synthesized by conjugating DTPA chelator moieties to higher than 90% of the monomer residues of the polyamino acid backbone chain. The resulting polymer can be labeled with Gd, since each chelator moiety holds a Gd ion, and the resulting conformation is of an unfolded, extended linear type, capable of entering small pores and moving around obstacles in the extracellular space of tissues. The efficient production of these extended polymers is critical for the application of such contrast agents to medical imaging. One such agent is a reptating polymer containing technetium-99.

    Synthesis of highly conjugated polymers
    69.
    发明申请
    Synthesis of highly conjugated polymers 审中-公开
    高共轭聚合物的合成

    公开(公告)号:US20040022857A1

    公开(公告)日:2004-02-05

    申请号:US10209726

    申请日:2002-07-31

    IPC分类号: A61K009/14

    摘要: Improved methods for forming substituted polymers having a high degree of conjugation include the steps of activating a steric hindrance molecule under conditions that ensure substantially all the steric hindrance molecules are mono-activated and then reacting with a polymer. An improved method for recovering polypeptides substituted with steric hindrance molecules and having an elongate configuration removes impurities and volatiles without achieving complete dryness of the copolymer.

    摘要翻译: 用于形成具有高度共轭度的取代聚合物的改进方法包括在确保基本上所有空间位阻分子被单活化然后与聚合物反应的条件下活化空间位阻分子的步骤。 用空间位阻分子取代并具有细长构型的多肽的改进方法可以除去杂质和挥发物而不使共聚物完全干燥。