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    Optical diagnostic and therapeutic agents and compositions
    2.
    发明授权
    Optical diagnostic and therapeutic agents and compositions 有权
    光学诊断和治疗剂及组合物

    公开(公告)号：US07767194B2

    公开(公告)日：2010-08-03

    申请号：US11146377

    申请日：2005-06-06

    申请人： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj ,  Muthunadar P. Periasamy

    发明人： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj ,  Muthunadar P. Periasamy

    IPC分类号： A61K49/00

    CPC分类号： A61K49/0032 ,  A61K41/0033 ,  A61K41/0057 ,  A61K49/0056 ,  C07D209/12 ,  C07D405/14 ,  C09B23/0066 ,  C09B23/0075 ,  C09B23/08 ,  C09B23/086

    摘要： Cyanine and indocyanine dye compounds and bioconjugates are disclosed. The present invention includes several cyanine and indocyanine dyes, including bioconjugates of the same, with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds of the invention may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of compounds of the invention allows favorable delivery to tumor cells as compared to larger molecular weight imaging agents. Further, use of a biocompatible organic solvent such as dimethylsulfoxide may be said to assist in maintaining the fluorescence of compounds of the invention. The compounds and bioconjugates herein disclosed are useful in a variety of medical applications including, but not limited to, diagnostic imaging and therapy, endoscopic applications for the detection of tumors and other abnormalities, localized therapy, photoacoustic tumor imaging, detection and therapy, and sonofluorescence tumor imaging, detection and therapy.

    摘要翻译： 公开了花青和靛蓝染料化合物和生物共轭物。 本发明包括几种花青和靛蓝染料，其包括与其各种双和四（羧酸）同系物的生物缀合物。 本发明的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，本发明化合物的小尺寸允许有利地递送到肿瘤细胞。 此外，使用生物相容性有机溶剂如二甲基亚砜可以说有助于维持本发明化合物的荧光。 本文公开的化合物和生物缀合物可用于各种医学应用，包括但不限于诊断成像和治疗，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，检测和治疗以及声发射 肿瘤成像，检测和治疗。

    RECEPTOR-AVID EXOGENOUS OPTICAL CONTRAST AND THERAPEUTIC AGENTS
    3.
    发明申请
    RECEPTOR-AVID EXOGENOUS OPTICAL CONTRAST AND THERAPEUTIC AGENTS 审中-公开
    受体 - 异常光学对比和治疗药物

    公开(公告)号：US20100022449A1

    公开(公告)日：2010-01-28

    申请号：US12470310

    申请日：2009-05-21

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

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

    IPC分类号： A61K38/08 ,  A61K31/403 ,  A61K38/06 ,  A61P43/00

    CPC分类号： A61K49/0021 ,  A61K49/0032 ,  A61K49/0056 ,  C07D209/12 ,  C07D403/06 ,  C07D403/08 ,  C07D405/14 ,  C09B23/0016 ,  C09B23/0025 ,  C09B23/0066 ,  C09B23/0075 ,  C09B23/086

    摘要： Cyanine and indocyanine dye compounds and bioconjugates are disclosed. The present invention includes several cyanine and indocyanine dyes, including bioconjugates of the same, with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds of the invention may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of compounds of the invention allows favorable delivery to tumor cells as compared to larger molecular weight imaging agents. Further, use of a biocompatible organic solvent such as dimethylsulfoxide may be said to assist in maintaining the fluorescence of compounds of the invention. The compounds and bioconjugates herein disclosed are useful in a variety of medical applications including, but not limited to, diagnostic imaging and therapy, endoscopic applications for the detection of tumors and other abnormalities, localized therapy, photoacoustic tumor imaging, detection and therapy, and sonofluorescence tumor imaging, detection and therapy.

    摘要翻译： 公开了花青和靛蓝染料化合物和生物共轭物。 本发明包括几种花青和靛蓝染料，其包括与其各种双和四（羧酸）同系物的生物缀合物。 本发明的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，本发明化合物的小尺寸允许有利地递送到肿瘤细胞。 此外，使用生物相容性有机溶剂如二甲基亚砜可以说有助于维持本发明化合物的荧光。 本文公开的化合物和生物缀合物可用于各种医学应用，包括但不限于诊断成像和治疗，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，检测和治疗以及声发射 肿瘤成像，检测和治疗。

    Receptor-avid exogenous optical contrast and therapeutic agents
    4.
    发明授权
    Receptor-avid exogenous optical contrast and therapeutic agents 有权
    受体 - 狂热的外源性光学对比和治疗剂

    公开(公告)号：US07504087B2

    公开(公告)日：2009-03-17

    申请号：US11075792

    申请日：2005-03-09

    申请人： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj ,  Muthunadar P. Periasamy

    发明人： Samuel I. Achilefu ,  Raghavan Rajagopalan ,  Richard B. Dorshow ,  Joseph E. Bugaj ,  Muthunadar P. Periasamy

    IPC分类号： A61K51/00 ,  A61M36/14

    CPC分类号： A61K49/0032 ,  A61K41/0033 ,  A61K41/0057 ,  A61K49/0056 ,  C07D209/12 ,  C07D405/14 ,  C09B23/0066 ,  C09B23/0075 ,  C09B23/08 ,  C09B23/086

    摘要： Cyanine and Indocyanine dye compounds and bioconjugates are disclosed. The present invention includes several cyanine and indocyanine dyes, including bioconjugates of the same, with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds of the invention may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of compounds of the invention allows favorable delivery to tumor cells as compared to larger molecular weight imaging agents. Further, use of a biocompatible organic solvent such as dimethylsulfoxide may be said to assist in maintaining the fluorescence of compounds of the invention. The compounds and bioconjugates herein disclosed are useful in a variety of medical applications including, but not limited to, diagnostic imaging and therapy, endoscopic applications for the detection of tumors and other abnormalities, localized therapy, photoacoustic tumor imaging, detection and therapy, and sonofluorescence tumor imaging, detection and therapy.

    摘要翻译： 公开了花青和吲哚菁染料化合物和生物共轭物。 本发明包括几种花青和靛蓝染料，其包括与其各种双和四（羧酸）同系物的生物缀合物。 本发明的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，本发明化合物的小尺寸允许有利地递送到肿瘤细胞。 此外，使用生物相容性有机溶剂如二甲基亚砜可以说有助于维持本发明化合物的荧光。 本文公开的化合物和生物缀合物可用于各种医学应用，包括但不限于诊断成像和治疗，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，检测和治疗以及声发射 肿瘤成像，检测和治疗。

    Internal image antibodies for optical imaging and therapy
    5.
    发明授权
    Internal image antibodies for optical imaging and therapy 失效
    用于光学成像和治疗的内部图像抗体

    公开(公告)号：US07431925B2

    公开(公告)日：2008-10-07

    申请号：US10761634

    申请日：2004-01-21

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

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

    IPC分类号： A61K39/395 ,  C07K16/42

    CPC分类号： A61K49/0058 ,  A61K41/0071 ,  A61K49/0032 ,  A61K2039/505 ,  C07K16/4208

    摘要： 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 or therapy.

    摘要翻译： 使用内部图像抗体进行光诊断和/或光疗的方法。 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，并且为靶向诊断或治疗提供期望的特异性和选择性。

    Aromatic sulfenates for type 1 phototherapy
    6.
    发明授权
    Aromatic sulfenates for type 1 phototherapy 失效
    用于1型光疗法的芳香族亚磺酸盐

    公开(公告)号：US07427657B1

    公开(公告)日：2008-09-23

    申请号：US11276971

    申请日：2006-03-20

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

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

    IPC分类号： A61K38/16

    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。

    Versatile hydrophilic dyes
    7.
    发明授权
    Versatile hydrophilic dyes 失效
    多用途亲水染料

    公开(公告)号：US06939532B2

    公开(公告)日：2005-09-06

    申请号：US09757333

    申请日：2001-01-09

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

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

    IPC分类号： C07H15/26 ,  A61B1/00 ,  A61K38/00 ,  A61K41/00 ,  A61K49/00 ,  A61P35/00 ,  C07D405/14 ,  C07K7/06 ,  C09B23/00 ,  C09K11/06 ,  A61B10/00 ,  A61B5/00 ,  A61B8/00

    CPC分类号： A61K49/0032 ,  A61K41/0033 ,  A61K41/0057 ,  A61K49/0056

    摘要： Dye-peptide conjugates useful for diagnostic imaging and therapy are disclosed. The dye-peptide conjugates include several cyanine dyes with a variety of bis- and tetrakis(carboxylic acid) homologues. 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 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The molecules of the invention are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities and for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

    摘要翻译： 公开了用于诊断成像和治疗的染料 - 肽缀合物。 染料 - 肽缀合物包括具有多种双和四（羧酸）同系物的几种花青染料。 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350-1300nm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。 本发明的分子可用于诊断成像和治疗，用于检测肿瘤和其他异常以及用于局部治疗，用于光声肿瘤成像，检测和治疗以及用于声发射肿瘤成像，检测和治疗的内窥镜应用中。

    Cyanine-sulfenates for dual phototherapy
    10.
    发明授权
    Cyanine-sulfenates for dual phototherapy 失效

    公开(公告)号：US07351807B2

    公开(公告)日：2008-04-01

    申请号：US09898809

    申请日：2001-07-03

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

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

    IPC分类号： C07K1/00 ,  C07K16/00 ,  C12P21/08 ,  C07D401/00 ,  C07D403/00

    CPC分类号： A61K41/0033 ,  A61K41/0057 ,  A61K41/0071 ,  A61K49/0032 ,  A61K49/0056 ,  C09B23/083 ,  C09B47/065 ,  C09B47/0678 ,  C09B47/26

    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.