Porphyrin-based compounds for tumor imaging and photodynamic therapy
    2.
    发明申请
    Porphyrin-based compounds for tumor imaging and photodynamic therapy 有权
    卟啉基化合物用于肿瘤成像和光动力学治疗

    公开(公告)号:US20100184970A1

    公开(公告)日:2010-07-22

    申请号:US12462535

    申请日:2009-08-05

    IPC分类号: C07D487/22

    摘要: This invention describes a first report on the synthesis of certain 124I-labelled photosensitizers related to chlorines and bacteriochlorins with long wavelength absorption in the range of 660-800 nm. In preliminary studies, these compounds show a great potential for tumor detection by positron emission tomography (PET) and treatment by photodynamic therapy (PDT). The development of tumor imaging or improved photodynamic therapy agent(s) itself represent an important step, but a dual function agent (PET imaging and PDT) provides the potential for diagnostic body scan followed by targeted therapy.

    摘要翻译: 本发明描述了关于在660-800nm范围内具有长波长吸收的氯和细菌二氢红素相关的某些124I标记的光敏剂的合成的第一报告。 在初步研究中,这些化合物通过正电子发射断层扫描(PET)和光动力学治疗(PDT)治疗显示出巨大的潜力。 肿瘤成像或改进的光动力治疗剂本身的发展本身就是重要的一步,但双重功能试剂(PET成像和PDT)提供诊断身体扫描的潜力,然后进行靶向治疗。

    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY
    3.
    发明申请
    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY 审中-公开
    用于肿瘤成像和治疗的多功能剂

    公开(公告)号:US20110223102A1

    公开(公告)日:2011-09-15

    申请号:US12677381

    申请日:2008-09-11

    摘要: A compound that is a conjugate of an antagonist to an integrin expressed by a tumor cell and at least one of a tumor avid tetrapyrollic photosensitizer, a fluorescent dye, and a radioisotope labeled moiety wherein the radioisotope is 11C, 18F, 64Cu, 124I, 99Tc, 111In or GdIII and its method of use for diagnosing, imaging and/or treating hyperproliferative tissue such as tumors. Preferably the photosensitizer is a tumor avid tetrapyrollic photosensitizer, e.g. a porphyrin, chlorin or bacteriochlorin, e.g. pheophorbides and pyropheophorbides. Such conjugates have extreme tumor avidity and can be used to inhibit or completely destroy the tumor by light absoption. The integrin is usually αvβ3, α5β1, αvβ5, α4β1, or α2β1. Preferably, the antagonist is an RGD peptide or another antagonist that may be synthetic such as a 4-{2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)ethyloxy}-benzoyl]amino-2-(S)-amino-ethyl-sulfonylamino group. Such compounds provide tumor avidity and imaging ability thus permitting selective and clear tumor imaging.

    摘要翻译: 作为拮抗剂与由肿瘤细胞表达的整联蛋白结合的化合物,以及至少一种肿瘤病毒四级光敏剂,荧光染料和放射性同位素标记部分,其中放射性同位素为11C,18F,64Cu,124I,99Tc ,111In或GdIII及其用于诊断,成像和/或治疗过度增生组织如肿瘤的方法。 优选地,光敏剂是肿瘤急性四分光敏光敏剂,例如。 卟啉,二氢卟酚或细菌二氢卟酚。 脱镁叶绿素和焦偏镁偏磷酸盐。 这种缀合物具有极端的肿瘤亲合力,可用于通过光吸收抑制或完全破坏肿瘤。 整合素通常为αv&bgr; 3,α5和bgr; 1,αv&bgr; 5,α4和bgr; 1或α2和bgr; 1。 优选地,拮抗剂是可以是合成的RGD肽或另一种拮抗剂,例如4- {2-(3,4,5,6-四 - 嘧啶-2-基氨基)乙氧基} - 苯甲酰基]氨基-2-( S) - 氨基 - 乙基 - 磺酰基氨基。 这样的化合物提供了肿瘤亲合力和成像能力,从而允许选择性和清晰的肿瘤成像。

    Porphyrin-based compounds for tumor imaging and photodynamic therapy
    4.
    发明申请
    Porphyrin-based compounds for tumor imaging and photodynamic therapy 审中-公开
    卟啉基化合物用于肿瘤成像和光动力学治疗

    公开(公告)号:US20060198783A1

    公开(公告)日:2006-09-07

    申请号:US11353626

    申请日:2006-02-14

    IPC分类号: A61K51/00 A61M36/14 C07H17/02

    摘要: This invention describes a first report on the synthesis of certain 124I-labelled photosensitizers related to chlorines and bacteriochlorins with long wavelength absorption in the range of 660-800 nm. In preliminary studies, these compounds show a great potential for tumor detection by positron emission tomography (PET) and treatment by photodynamic therapy (PDT). The development of tumor imaging or improved photodynamic therapy agent(s) itself represent an important step, but a dual function agent (PET imaging and PDT) provides the potential for diagnostic body scan followed by targeted therapy.

    摘要翻译: 本发明描述了关于在660-800nm范围内具有长波长吸收的氯和细菌二氢红素相关的某些124 I-标记的光敏剂的合成的第一报告。 在初步研究中,这些化合物通过正电子发射断层扫描(PET)和光动力学治疗(PDT)治疗显示出巨大的潜力。 肿瘤成像或改进的光动力治疗剂本身的发展本身就是重要的一步,但双重功能试剂(PET成像和PDT)提供诊断身体扫描的潜力,然后进行靶向治疗。