ANTIZYME MODULATORS AND THEIR USE
    19.
    发明公开
    ANTIZYME MODULATORS AND THEIR USE 有权
    抗氧化剂调节剂及其用途

    公开(公告)号:EP1159261A2

    公开(公告)日:2001-12-05

    申请号:EP00913365.3

    申请日:2000-02-04

    IPC分类号: C07C279/00

    摘要: The present invention is directed to agmatine and polyamine analogs and their use as drugs, as well as agricultural or environmentally useful agents. As drugs, the analogs decrease cellular polyamine levels, possibly by inducing antizyme, and can be used to treat disorders of undesired cell proliferation, including cancer, viral infections and bacterial infections. The analogs may be utilized in pharmaceutical compositions either alone or in combination with other agents, particularly other inhibitors of polyamine synthesis or transport, but including other inhibitors of cell proliferation. The analogs are not necessarily metabolized to contribute to the polyamine pool and are designed to enter cells by pathways independent of polyamine transport. The invention further defines structural elements/motifs within these analogs that are key to their induction of antizyme.

    摘要翻译: 本发明涉及胍丁胺和多胺类似物及其作为药物的用途,以及农业或环境有用的药剂。 作为药物,类似物可能通过诱导抗酶来降低细胞多胺的水平,并且可用于治疗不希望的细胞增殖的疾病,包括癌症,病毒感染和细菌感染。 类似物可以单独或与其他药剂组合使用在药物组合物中,特别是其他多胺合成或转运抑制剂,但包括其他细胞增殖抑制剂。 类似物不一定被代谢以促成多胺库,并且被设计为通过独立于多胺转运的途径进入细胞。 本发明进一步定义了这些类似物内的结构元件/基序,这些类似物是它们诱导抗酶的关键。