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    • 7. 发明申请
    • TRACEABLE RETINOID ACID FOR IMAGING, DISEASE PREVENTION AND THERAPY
    • 用于成像,疾病预防和治疗的可追踪的抗感染药
    • US20120244079A1
    • 2012-09-27
    • US13319012
    • 2010-05-06
    • Shi KeMichel MawadWei Wang
    • Shi KeMichel MawadWei Wang
    • C07D403/08A61K49/04A61K49/00
    • A61K49/0052A61K49/0032G01N33/5008G01N33/5014G01N33/5088G01N33/574G01N33/582G01N2800/56
    • The present invention provides nonradioactive NIR optical imaging agents based up on the structure of retinoid acid derivatives. The nonradioactive NIR optical imaging agent has been evaluated at the cellular level by confocal microscopy, and in vivo in a whole animal using a various xenograft models. The specific uptake of this agent in human cancer cells and multiple xenograft models demonstrate that nonradioactive near infrared dye labeled retinoid metabolites and/or analogs are useful for early stage cancer studies and diagnoses. Also, the present invention provides that nonradioactive near infrared dye labeled retinoid metabolites and/or analogs are useful for visualization of drug redistribution within the body which is useful in determining the optimal biological dose. Ultimately, the visualization data can be used as an analytical tool to reduce any systemic toxicity.
    • 本发明提供了基于类视黄酸衍生物结构的非放射性近红外光学成像剂。 已经通过共聚焦显微镜在细胞水平上评估了非放射性近红外光学成像剂,并且在使用各种异种移植模型的整个动物体内进行了评估。 该药物在人类癌细胞和多种异种移植物模型中的特异性摄取表明,非放射性近红外染料标记的类视黄醇代谢物和/或类似物可用于早期癌症研究和诊断。 此外,本发明提供非放射性近红外染料标记的类视黄醇代谢物和/或类似物可用于体内药物再分布的可视化,其可用于确定最佳生物剂量。 最终,可视化数据可用作分析工具,以减少任何全身毒性。