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    Novel aromatic azides for type I phototherapy
    2.
    发明申请
    Novel aromatic azides for type I phototherapy 审中-公开
    用于I型光疗法的新型芳族叠氮化物

    公开(公告)号：US20040180864A1

    公开(公告)日：2004-09-16

    申请号：US10808184

    申请日：2004-03-24

    Applicant: MALLINCKRODT INC.

    Inventor： Raghavan Rajagopalan ,  Gary Cantrell ,  Samuel I. Achilefu ,  Joseph E. Bugai ,  Richard B. Dorshow

    IPC: A61K031/655

    CPC classification number: A61K41/0057 ,  C07J41/00

    Abstract: The present invention discloses novel aromatic azide derivatives and their bioconjugates for phototherapy of tumors and other lesions. The organic azides 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 nitrene, the reactive intermediate produced upon photoexcitation of the aromatic azide, with the tissue of interest. The compounds of the present invention are administered to a patient, allowed to accumulate at the site of the tumor or other lesion, and are exposed to light in order to perform a phototherapeutic procedure.

    Abstract translation: 本发明公开了新颖的芳族叠氮衍生物及其生物缀合物用于肿瘤和其他病变的光疗。 本发明的有机叠氮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。 光疗效果是由硝酸（通过芳香叠氮化物的光激发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。 将本发明的化合物施用于患者，允许在肿瘤或其他损伤部位积聚，并暴露于光以进行光疗法。

    Dye-azide compounds for dual phototherapy
    3.
    发明申请
    Dye-azide compounds for dual phototherapy 失效
    用于双重光疗的染料叠氮化合物

    公开(公告)号：US20040161430A1

    公开(公告)日：2004-08-19

    申请号：US10776840

    申请日：2004-02-11

    Applicant: MALLINCKRODT INC.

    Inventor： Raghavan Rajagopalan ,  Samuel I. Achilefu ,  Joseph E. Bugai ,  Richard B. Dorshow

    IPC: A61K039/395

    CPC classification number: B82Y5/00 ,  A61K41/0057 ,  A61K41/0071 ,  A61K47/62 ,  A61K47/64 ,  A61K47/66 ,  A61K49/0021 ,  A61K49/0056 ,  C09B47/045 ,  Y10S435/968 ,  Y10S436/80

    Abstract: The present invention discloses dye-azide derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and nitrene at the lesion of interest.

    Abstract translation: 本发明公开了染料叠氮化物衍生物及其生物缀合物用于肿瘤和其他病变的双重光疗。 本发明的化合物可以含有1型和2型试剂的混合物，或者可以将相同分子中的两个单元整合的单个实体。 该化合物被设计成同时使用将在感兴趣的病变处产生单线态氧和氮烯的双波长光源产生1型和2型光疗效应。

    Aromatic sulfenates for type I phototherapy
    4.
    发明申请
    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：US20030158127A1

    公开(公告)日：2003-08-21

    申请号：US09898887

    申请日：2001-07-03

    Applicant: MALLINCKRODT INC.

    Inventor： Raghavan Rajagopalan ,  Gary L. Cantrell ,  Samuel I. Achilefu ,  Joseph E. Bugaj ,  Richard B. Dorshow

    IPC: A61K031/704 ,  A61K031/52 ,  A61K031/497 ,  A61K031/4709 ,  A61K031/4184 ,  A61K031/473 ,  A61K031/4178 ,  A61K031/416

    CPC classification number: A61K41/0057

    Abstract: 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.

    Abstract translation: 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。

    Internal image antibodies for optical imaging and therapy
    5.
    发明申请
    Internal image antibodies for optical imaging and therapy 审中-公开
    用于光学成像和治疗的内部图像抗体

    公开(公告)号：US20030031627A1

    公开(公告)日：2003-02-13

    申请号：US09919243

    申请日：2001-07-31

    Applicant: MALLINCKRODT INC.

    Inventor： Raghavan Rajagopalan ,  Joseph E. Bugaj ,  Samuel I. Achilefu ,  Richard B. Dorshow

    IPC: A61K049/00 ,  A61K039/395 ,  C07K016/28

    CPC classification number: A61K49/0058 ,  A61K41/0071 ,  A61K49/0032 ,  A61K2039/505 ,  C07K16/4208

    Abstract: Compositions and methods using internal image antibodies for photodiagnosis and/or phototherapy. The internal image antibodies are conjugated with a photoactive molecule such as a dye or photosensitizer, to target specific regions, such as biological receptors. The photoactive molecules are then activated for diagnosis or therapy. Advantageously, the internal image antibody is specific for a biological receptor, but does not require isolation of the receptor to prepare the antibody, and provides the desired specificity and selectivity for targeted diagnosis for therapy.

    Abstract translation: 使用内部图像抗体进行光诊断和/或光疗的组合物和方法。 将内部图像抗体与光活性分子例如染料或光敏剂共轭，以靶向特定区域，例如生物受体。 然后激活光活性分子进行诊断或治疗。 有利地，内部图像抗体对于生物受体是特异性的，但不需要分离受体以制备抗体，并且为治疗的靶向诊断提供期望的特异性和选择性。

    Receptor-avid exogenous optical contrast and therapeutic agents
    6.
    发明申请
    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：US20020156117A1

    公开(公告)日：2002-10-24

    申请号：US09864011

    申请日：2001-05-23

    Applicant: MALLINCKRODT INC.

    Inventor： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj

    IPC: A61K031/405 ,  C07D43/02

    CPC classification number: A61K49/0032 ,  A61K41/0033 ,  A61K41/0057 ,  A61K49/0056 ,  C09B23/0066 ,  C09B23/08

    Abstract: 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.

    Abstract translation: 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。

    Tumor-targeted optical contrast agents
    7.
    发明申请
    Tumor-targeted optical contrast agents 有权
    肿瘤靶向光学造影剂

    公开(公告)号：US20020044909A1

    公开(公告)日：2002-04-18

    申请号：US09863971

    申请日：2001-05-23

    Applicant: MALLINCKRODT INC.

    Inventor： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj

    IPC: A61K049/00 ,  C07D43/02

    CPC classification number: A61K41/0033

    Abstract: 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.

    Abstract translation: 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。

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