Tumor-targeted optical contrast agents

    公开(公告)号:US06641798B2

    公开(公告)日:2003-11-04

    申请号:US09863971

    申请日:2001-05-23

    IPC分类号: A61B1000

    CPC分类号: A61K41/0033

    摘要: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologes. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1,300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

    Cyanine-sulfenates for dual phototherapy

    公开(公告)号:US07351807B2

    公开(公告)日:2008-04-01

    申请号:US09898809

    申请日:2001-07-03

    摘要: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds comprise sulfenates having the formula, t,0080where E is selected from the group consisting of somatostatin receptor binding molecules, heat sensitive bacterioendotoxin receptor binding molecules, neurotensin receptor binding molecules, bombesin receptor binding molecules, cholecystekinin receptor binding molecules, steroid receptor binding molecules, and carbohydrate receptor binding molecules, and dihydoxyindolecarboxylic acid; L and X are independently selected from the group consisting of —(R5)NOC—, —(R5)NOCCH2O—, —(R5)NOCCH2CH2O—, —OCN(R5)—, —HNC(═S)NH—, and HNC(═O)NH—; DYE is an aromatic or a heteroaromatic radical derived from the group consisting of cyanines, indocyanines, phthalocyanines, rhodamines, phenoxazines, phenothiazines, phenoselenazines, fluoresceins, porphyrins, benzoporphyrins, squaraines, corrins, croconiums, azo dyes, methine dyes, indolenium dyes, crellins, and hypocrellins; R1 to R5 are independently selected from the group comprising hydrogen, C1-C10 alkyl, C5-C10 aryl, C1-C10 polyhydroxyalkyl, and C1-C10 polyalkoxyalkyl; and Ar is an aromatic or heteroaromatic radical derived from the group consisting of benzenes, naphthalenes, naphthoquinones, diphenylmethanes, fluorenes, anthracenes, anthraquinones, phenanthrenes, tetracenes, naphthacenediones, pyridines, quinolines, isoquinolines, indoles, isoindoles, pyrroles, imidiazoles, oxazoles, thiazoles, pyrazoles, pyrazines, purines, benzimidazoles, furans, benzofurans, dibenzofurans, carbazoles, acridines, acridones, phenanthridines, thiophenes, benzothiophenes, dibenzothiophenes, xanthenes, xanthones, flavones, coumarins, and anthacylines. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effects at once using a dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

    Receptor-avid exogenous optical contrast and therapeutic agents
    8.
    发明授权
    Receptor-avid exogenous optical contrast and therapeutic agents 失效
    受体 - 狂热的外源性光学对比和治疗剂

    公开(公告)号:US06706254B2

    公开(公告)日:2004-03-16

    申请号:US09864011

    申请日:2001-05-23

    IPC分类号: A61B1000

    摘要: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologes. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1,300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

    摘要翻译: 公开了可用于诊断成像和治疗的花青染料生物缀合物。 缀合物包括几种具有多种双和四(羧酸)同系物的花青染料。 化合物可以与生物活性肽,碳水化合物,激素,药物或其他生物活性剂缀合。 与较大的分子量成像剂相比,化合物的小尺寸允许更有利于肿瘤细胞的递送。 各种染料在350至1,300nm的范围内是有用的,精确的范围取决于特定的染料。 使用二甲基亚砜有助于维持化合物的荧光。 本发明化合物可用于诊断成像和治疗,用于检测肿瘤和其他异常的内窥镜应用,局部治疗,光声肿瘤成像,检测和治疗以及用于声发射肿瘤成像,检测和治疗。

    Aromatic sulfenates for type I phototherapy
    10.
    发明授权
    Aromatic sulfenates for type I phototherapy 失效
    用于I型光疗法的芳族亚磺酸盐

    公开(公告)号:US07235685B2

    公开(公告)日:2007-06-26

    申请号:US09898887

    申请日:2001-07-03

    IPC分类号: C07K313/08

    CPC分类号: A61K41/0057

    摘要: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.

    摘要翻译: 本发明公开了用于肿瘤和其他病变光疗的新型次氯酸盐衍生物及其生物缀合物。 本发明的次氯酸盐被设计成吸收电磁光谱的低能量紫外线,可见光或近红外(NIR)区域。 光疗效应是由自由基(在次硫酸盐部分的光分解产生的反应性中间体)与感兴趣的组织的直接相互作用引起的。