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    • 4. 发明授权
    • Polymerization method for the synthesis of polypeptide imaging agents
    • 用于合成多肽成像剂的聚合方法
    • US07205385B2
    • 2007-04-17
    • US10987662
    • 2004-11-12
    • Brian James GrimmondBahram MoasserMohan Mark Amaratunga
    • Brian James GrimmondBahram MoasserMohan Mark Amaratunga
    • C07K1/04C07K2/00A61K38/00A61K38/02
    • C07D263/44A61K49/085A61K49/146
    • 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.
    • 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。