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1. 发明申请

US20040180864A1 Novel aromatic azides for type I phototherapy 审中-公开
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Gary Cantrell , Samuel I. Achilefu , Joseph E. Bugai , Richard B. Dorshow
IPC分类号： A61K031/655
CPC分类号： A61K41/0057 , C07J41/00
摘要： 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.
摘要翻译：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。

2. 发明申请

US20040161430A1 Dye-azide compounds for dual phototherapy 失效
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Samuel I. Achilefu , Joseph E. Bugai , Richard B. Dorshow
IPC分类号： A61K039/395
CPC分类号： B82Y5/00 , A61K41/0057 , A61K41/0071 , A61K47/62 , A61K47/64 , A61K47/66 , A61K49/0021 , A61K49/0056 , C09B47/045 , Y10S435/968 , Y10S436/80
摘要： 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.
摘要翻译：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。

3. 发明申请

US20040156783A1 Compounds for dual photodiagnosis and therapy 失效
标题翻译：用于双重光诊断和治疗的化合物
公开(公告)号：US20040156783A1
公开(公告)日：2004-08-12
申请号：US10685172
申请日：2003-10-14
申请人： Mallinckrodt Inc.
发明人： Raghavan Rajagopalan , Samuel I. Achilefu , Joseph E. Bugaj , Richard B. Dorshow , Muthunadar P. Periasamy
IPC分类号： A61K049/00 , C07K014/705
CPC分类号： C09B23/083 , A61K41/0057 , A61K41/0061 , A61K41/0071 , A61K47/546 , A61K47/66 , B82Y5/00 , C09B47/045 , C09B47/30 , Y10S436/80 , Y10T436/13
摘要： The invention discloses compounds and compositions for dual phototherapy and combined therapy and diagnosis of tumors and other lesions. The compounds have a Dye that, when photoactivated, operates via Type I and/or Type II mechanisms. Other Dye or azide components may operate by the same or different mechanisms. Selection of particular components in a compound, and formulation of the compound(s) in a composition permit different activation wavelengths to be used for different therapies. A targeting moiety may be added to the compound or composition so that the Dye locates at a particular site, such as a hormone-sensitive tumor, for diagnosis and/or treatment. The compounds and compositions may be incorporated within liposomes.
摘要翻译：本发明公开了用于双光疗法和组合治疗和诊断肿瘤和其他病变的化合物和组合物。化合物具有染料，当光活化时，它们通过I型和/或II型机制进行操作。其他染料或叠氮化物组分可以通过相同或不同的机理操作。选择化合物中的特定组分以及组合物中化合物的配制允许不同的激活波长用于不同疗法。可以将靶向部分加入到化合物或组合物中，使得染料位于特定部位，例如激素敏感性肿瘤，用于诊断和/或治疗。化合物和组合物可以掺入脂质体中。

4. 发明申请

US20020164287A1 AZO COMPOUNDS FOR TYPE I PHOTOTHERAPY 失效
标题翻译：用于I型照相机的AZO化合物
公开(公告)号：US20020164287A1
公开(公告)日：2002-11-07
申请号：US09849163
申请日：2001-05-04
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Gary L. Cantrell , Joseph E. Bugaj , Samuel I. Achilefu , Richard B. Dorshow
IPC分类号： A61K049/00 , C08B037/00 , A61K039/395
CPC分类号： A61K49/0026 , A61K41/0057 , A61K47/64 , A61K49/0039 , A61K49/0041 , A61K49/0056 , C07D471/06
摘要： Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the 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 photoexcitation of the azo compound, with the tissue of interest.
摘要翻译：新型偶氮化合物及其生物缀合物用于光疗和/或光化学诊断肿瘤和其他病变。本发明的偶氮衍生物被设计成在电磁光谱的低能量紫外线，可见光或近红外（NIR）区域吸收。光疗效果是由自由基（通过偶氮化合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。

5. 发明申请

US20030036538A1 Dye-sulfenates for dual phototherapy 失效
标题翻译：用于双光疗的染料 - 次硫酸盐
公开(公告)号：US20030036538A1
公开(公告)日：2003-02-20
申请号：US09898809
申请日：2001-07-03
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Samuel I. Achilefu , Joseph E. Bugaj , Richard B. Dorshow
IPC分类号： A61K031/7052 , C07H017/02 , C07D279/18 , C09B047/04 , C07J043/00
CPC分类号： A61K41/0033 , A61K41/0057 , A61K41/0071 , A61K49/0032 , A61K49/0056 , C09B23/083 , C09B47/065 , C09B47/0678 , C09B47/26
摘要： The present invention discloses dye-sulfenate 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 free radicals at the lesion of interest.
摘要翻译：本发明公开了用于肿瘤和其他病变双光疗法的染料 - 次硫酸盐衍生物及其生物缀合物。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。这些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自由基的双波长光源产生1型和2型光疗效应。

6. 发明申请

US20020169107A1 Novel aromatic azides for type I phototherapy 审中-公开
标题翻译：用于I型光疗法的新型芳族叠氮化物
公开(公告)号：US20020169107A1
公开(公告)日：2002-11-14
申请号：US09766347
申请日：2001-01-19
申请人： Mallinckrodt Inc.
发明人： Raghavan Rajagopalan , Gary Cantrell , Samuel I. Achilefu , Joseph E. Bugaj , Richard B. Dorshow
IPC分类号： A61K038/16 , A61K031/70 , A61K031/665 , C07J041/00 , C07K016/00 , C07K014/00
CPC分类号： A61K41/0057 , C07J41/00
摘要： 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.
摘要翻译：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。

7. 发明申请

US20030158127A1 Aromatic sulfenates for type I phototherapy 失效
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Gary L. Cantrell , Samuel I. Achilefu , Joseph E. Bugaj , Richard B. Dorshow
IPC分类号： A61K031/704 , A61K031/52 , A61K031/497 , A61K031/4709 , A61K031/4184 , A61K031/473 , A61K031/4178 , A61K031/416
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。

8. 发明申请

US20030031627A1 Internal image antibodies for optical imaging and therapy 审中-公开
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Raghavan Rajagopalan , Joseph E. Bugaj , Samuel I. Achilefu , Richard B. Dorshow
IPC分类号： A61K049/00 , A61K039/395 , C07K016/28
CPC分类号： A61K49/0058 , A61K41/0071 , A61K49/0032 , A61K2039/505 , C07K16/4208
摘要： 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.
摘要翻译：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。

9. 发明申请

US20020156117A1 Receptor-avid exogenous optical contrast and therapeutic agents 失效
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Samuel I. Achilefu , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugaj
IPC分类号： A61K031/405 , C07D43/02
CPC分类号： A61K49/0032 , A61K41/0033 , A61K41/0057 , A61K49/0056 , C09B23/0066 , C09B23/08
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。

10. 发明申请

US20020044909A1 Tumor-targeted optical contrast agents 有权
标题翻译：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
申请人： MALLINCKRODT INC.
发明人： Samuel I. Achilefu , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugaj
IPC分类号： A61K049/00 , C07D43/02
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.
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。

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