申请人:ACCESS PHARMACEUTICALS, INC.
公开号:US20010038830A1
公开(公告)日:2001-11-08
The present invention relates to purified platinum complexes in which platinum is coordinated to form a single N,O- or O,O-chelate of an amidomalonate. The chelates, and pharmaceutically acceptable formulations thereof, are useful for the treatment of cancer. The platinum chelates may additionally be linked to one or more functional groups which increases water solubility and/or assists in tumor targeting of the chelate. Examples of tumor targeting moieties include polymers, in which one or more platinum chelates are attached to the polymer backbone via linkers capable of being cleaved in the body, and molecules with a high affinity for receptors which are concentrated or upregulated in tumor tissue and/or the tumor vasculature.
本发明涉及纯化的铂络合物,其中铂配位形成氨基丙二酸单个 N,O-或 O,O-螯合物。这些螯合物及其药学上可接受的制剂可用于治疗癌症。铂螯合物还可与一个或多个官能团连接,以增加水溶性和/或协助螯合物的肿瘤靶向作用。肿瘤靶向分子的例子包括聚合物(其中一种或多种铂螯合物通过可在体内裂解的连接体连接到聚合物骨架上),以及对肿瘤组织和/或肿瘤血管中集中或上调的受体具有高亲和力的分子。