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1. 发明申请

US20100222538A1 NOVEL PHOTOSENSITIZER BASED ON POLYMER DERIVATIVES-PHOTOSENSITIZER CONJUGATES FOR PHOTODYNAMIC THERAPY 有权
标题翻译：基于聚合物衍生物的新型光敏剂 - 光致变色治疗光敏剂
公开(公告)号：US20100222538A1
公开(公告)日：2010-09-02
申请号：US12595103
申请日：2008-04-23
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Jong-Ho Kim , Kyeong-Soon Park
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Jong-Ho Kim , Kyeong-Soon Park
IPC分类号： C08F251/00
CPC分类号： A61K41/0071 , A61K47/61 , A61K47/6929
摘要： Disclosed is a novel photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy capable of being selectively accumulated in cancerous tissues and producing singlet oxygen or free radical by laser irradiation. The polymer derivatives-photosensitizer conjugates for photodynamic therapy are prepared as nano-sized particles, and have excellent selection and accumulation ratio for cancerous tissues. The photosensitizer conjugates can produce singlet oxygen or free radical by a specific laser wavelength. Owing to the excellent selection and accumulation ratio for cancerous tissues, the conjugates minimizes photo-cytotoxicity of the conventional photosensitizer having a low molecular amount. Accordingly, the conjugates are very useful as a photosensitizes for photodynamic therapy with reduced side effects and excellent therapeutic effectiveness.
摘要翻译：公开了一种基于用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物的新型光敏剂，其能够选择性地积累在癌组织中并通过激光照射产生单线态氧或自由基。用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物制备为纳米尺寸颗粒，并且对于癌组织具有优异的选择和积累比。光敏剂共轭物可以通过特定的激光波长产生单线态氧或自由基。由于癌组织的优异的选择和积累比，共轭物使具有低分子量的常规光敏剂的光细胞毒性最小化。因此，缀合物对于具有降低的副作用和优异治疗有效性的光动力疗法的光敏剂是非常有用的。

2. 发明申请

US20100233085A1 IONIC COMPLEX NANOPARTICLES FOR DETECTING HEPARANASE ACTIVITIES AND METHOD FOR PREPARING THE SAME 有权
标题翻译：用于检测HEPARANASE活性的离子复合纳米颗粒及其制备方法
公开(公告)号：US20100233085A1
公开(公告)日：2010-09-16
申请号：US12472405
申请日：2009-05-27
申请人： Ick-Chan KWON , Kwang-Meyung KIM , Kui-Won CHOI , Kyeong-Soon PARK , Seul-Ki LEE
发明人： Ick-Chan KWON , Kwang-Meyung KIM , Kui-Won CHOI , Kyeong-Soon PARK , Seul-Ki LEE
IPC分类号： A61K49/00 , C12Q1/34
CPC分类号： C12Q1/34 , A61K49/0054 , G01N2333/924
摘要： Disclosed are Ionic complex nanoparticles for detecting heparanase activities and a method for preparing the same. More specifically, disclosed are Ionic complex nanoparticles for detecting heparanase activities, wherein negative-ion substrate polymers specifically degraded by heparanase and positive-ion biocompatible polymers ionically bind to each other, and fluorophores or quenchers bind to each of the polymers. The ionic complex nanoparticles for detecting heparanase activities may be applied to a method for screening novel drugs such as inhibitors that prevent over-expression of heparanase. Various cells and tissues where over-expression of heparanase occurs may be non-invasively imaged in cancer cells, cancer tissues, and tissues of various inflammatory diseases. Accordingly, the ionic complex nanoparticles for detecting heparanase activities may be effectively used to early diagnose various diseases and incurable diseases including autoimmune diseases such as cancers, osteoarthritis, rheumatoid arthritis, and dementia.
摘要翻译：公开了用于检测乙酰肝素酶活性的离子复合纳米粒子及其制备方法。更具体地，公开了用于检测乙酰肝素酶活性的离子复合纳米颗粒，其中由肝素酶和阳离子生物相容性聚合物特异性降解的负离子底物聚合物彼此离子地结合，并且荧光团或猝灭剂与每种聚合物结合。用于检测乙酰肝素酶活性的离子络合物纳米颗粒可以应用于筛选新型药物的方法，例如防止肝素酶过度表达的抑制剂。发生肝素酶过度表达的各种细胞和组织可能在癌细胞，癌组织和各种炎性疾病的组织中非侵入性成像。因此，用于检测乙酰肝素酶活性的离子络合物纳米颗粒可以有效地用于早期诊断各种疾病和不治之症，包括自身免疫疾病如癌症，骨关节炎，类风湿性关节炎和痴呆。

3. 发明授权

US08614285B2 Photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy 有权
标题翻译：基于聚合物衍生物的光敏剂 - 用于光动力疗法的光敏剂共轭物
公开(公告)号：US08614285B2
公开(公告)日：2013-12-24
申请号：US12595103
申请日：2008-04-23
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Jong-Ho Kim , Kyeong-Soon Park
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Jong-Ho Kim , Kyeong-Soon Park
IPC分类号： C08F251/00 , A61K31/555
CPC分类号： A61K41/0071 , A61K47/61 , A61K47/6929
摘要： Disclosed is a novel photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy capable of being selectively accumulated in cancerous tissues and producing singlet oxygen or free radical by laser irradiation. The polymer derivatives-photosensitizer conjugates for photodynamic therapy are prepared as nano-sized particles, and have excellent selection and accumulation ratio for cancerous tissues. The photosensitizer conjugates can produce singlet oxygen or free radical by a specific laser wavelength. Owing to the excellent selection and accumulation ratio for cancerous tissues, the conjugates minimizes photo-cytotoxicity of the conventional photosensitizer having a low molecular amount. Accordingly, the conjugates are very useful as a photosensitizes for photodynamic therapy with reduced side effects and excellent therapeutic effectiveness.
摘要翻译：公开了一种基于用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物的新型光敏剂，其能够选择性地积累在癌组织中并通过激光照射产生单线态氧或自由基。用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物制备为纳米尺寸颗粒，并且对于癌组织具有优异的选择和积累比。光敏剂共轭物可以通过特定的激光波长产生单线态氧或自由基。由于癌组织的优异的选择和积累比，共轭物使具有低分子量的常规光敏剂的光细胞毒性最小化。因此，缀合物对于具有降低的副作用和优异治疗有效性的光动力疗法的光敏剂是非常有用的。

4. 发明申请

US20110213121A1 NANOPARTICLE SENSOR FOR MEASURING PROTEASE ACTIVITY AND METHOD FOR MANUFACTURING THE SAME 有权
标题翻译：用于测量蛋白酶活性的纳米颗粒传感器及其制造方法
公开(公告)号：US20110213121A1
公开(公告)日：2011-09-01
申请号：US13060902
申请日：2009-08-27
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park , Dae-Hyuk Moon , Dae-Yoon Chi , Seung-Jin Lee , Seung-Jae Myung
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park , Dae-Hyuk Moon , Dae-Yoon Chi , Seung-Jin Lee , Seung-Jae Myung
IPC分类号： C07K9/00 , B82Y5/00
CPC分类号： C12Q1/37 , G01N33/54346 , Y10S977/773 , Y10S977/774 , Y10S977/807 , Y10S977/811 , Y10S977/953
摘要： Disclosed are a nanoparticle sensor for measuring protease activity, for protease imaging, and a method for preparing the same. More specifically, the present invention relates to a nanoparticle sensor for measuring protease activity in which a fluorophore- and a quencher-conjugated peptide substrate is conjugated to a biocompatible polymer nanoparticle. The peptide substrate is specifically lysed by a protease. The sensor according to the present invention is capable of inhibiting emission of fluorescence with high extinctive activity of the quencher on a fluorescent material. But strong fluorescence is specifically emitted only if the peptide substrate is lysed by a specific protease. Therefore, the sensor is especially useful as a method for screening a novel drug such as a protease overexpression inhibitor, and early diagnosis of incurable diseases and various diseases such as autoimmune diseases including cancer, osteoarthritis, rheumatoid arthritis and dementia.
摘要翻译：公开了用于测定蛋白酶活性的蛋白酶成像用纳米粒子传感器及其制备方法。更具体地，本发明涉及用于测量蛋白酶活性的纳米颗粒传感器，其中荧光团和猝灭剂缀合的肽底物与生物相容性聚合物纳米颗粒缀合。肽底物被蛋白酶特异性裂解。根据本发明的传感器能够抑制荧光材料上猝灭剂具有高灭绝活性的荧光发射。但是如果肽底物被特异性蛋白酶裂解，则强荧光是特异性发射的。因此，该传感器作为筛选新型药物如蛋白酶过表达抑制剂的方法，以及早期诊断不治之症以及各种疾病，如自身免疫性疾病，包括癌症，骨关节炎，类风湿性关节炎和痴呆症，都是特别有用的。

5. 发明授权

US08323622B2 Ionic complex nanoparticles for detecting heparanase activities and method for preparing the same 有权
标题翻译：用于检测肝素酶活性的离子复合纳米颗粒及其制备方法
公开(公告)号：US08323622B2
公开(公告)日：2012-12-04
申请号：US12472405
申请日：2009-05-27
申请人： Ick-Chan Kwon , Kwang-Meyung Kim , Kui-Won Choi , Kyeong-Soon Park , Seul-Ki Lee
发明人： Ick-Chan Kwon , Kwang-Meyung Kim , Kui-Won Choi , Kyeong-Soon Park , Seul-Ki Lee
IPC分类号： A61B5/00
CPC分类号： C12Q1/34 , A61K49/0054 , G01N2333/924
摘要： Disclosed are Ionic complex nanoparticles for detecting heparanase activities and a method for preparing the same. More specifically, disclosed are Ionic complex nanoparticles for detecting heparanase activities, wherein negative-ion substrate polymers specifically degraded by heparanase and positive-ion biocompatible polymers ionically bind to each other, and fluorophores or quenchers bind to each of the polymers. The ionic complex nanoparticles for detecting heparanase activities may be applied to a method for screening novel drugs such as inhibitors that prevent over-expression of heparanase. Various cells and tissues where over-expression of heparanase occurs may be non-invasively imaged in cancer cells, cancer tissues, and tissues of various inflammatory diseases. Accordingly, the ionic complex nanoparticles for detecting heparanase activities may be effectively used to early diagnose various diseases and incurable diseases including autoimmune diseases such as cancers, osteoarthritis, rheumatoid arthritis, and dementia.
摘要翻译：公开了用于检测乙酰肝素酶活性的离子复合纳米粒子及其制备方法。更具体地，公开了用于检测乙酰肝素酶活性的离子复合纳米颗粒，其中由肝素酶和阳离子生物相容性聚合物特异性降解的负离子底物聚合物彼此离子地结合，并且荧光团或猝灭剂与每种聚合物结合。用于检测乙酰肝素酶活性的离子络合物纳米颗粒可以应用于筛选新型药物的方法，例如防止肝素酶过度表达的抑制剂。发生肝素酶过度表达的各种细胞和组织可能在癌细胞，癌组织和各种炎性疾病的组织中非侵入性成像。因此，用于检测乙酰肝素酶活性的离子络合物纳米颗粒可以有效地用于早期诊断各种疾病和不治之症，包括自身免疫疾病如癌症，骨关节炎，类风湿性关节炎和痴呆。

6. 发明授权

US08841085B2 Nanoparticle sensor for measuring protease activity and method for manufacturing the same 有权
标题翻译：用于测量蛋白酶活性的纳米粒子传感器及其制造方法
公开(公告)号：US08841085B2
公开(公告)日：2014-09-23
申请号：US13060902
申请日：2009-08-27
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park , Dae-Hyuk Moon , Dae-Yoon Chi , Seung-Jin Lee , Seung-Jae Myung
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park , Dae-Hyuk Moon , Dae-Yoon Chi , Seung-Jin Lee , Seung-Jae Myung
IPC分类号： C12Q1/34 , C12Q1/37 , G01N33/543 , C12Q1/04 , C12Q1/06
CPC分类号： C12Q1/37 , G01N33/54346 , Y10S977/773 , Y10S977/774 , Y10S977/807 , Y10S977/811 , Y10S977/953
摘要： Disclosed are a nanoparticle sensor for measuring protease activity, for protease imaging, and a method for preparing the same. More specifically, the present invention relates to a nanoparticle sensor for measuring protease activity in which a fluorophore- and a quencher-conjugated peptide substrate is conjugated to a biocompatible polymer nanoparticle. The peptide substrate is specifically lysed by a protease. The sensor according to the present invention is capable of inhibiting emission of fluorescence with high extinctive activity of the quencher on a fluorescent material. But strong fluorescence is specifically emitted only if the peptide substrate is lysed by a specific protease. Therefore, the sensor is especially useful as a method for screening a novel drug such as a protease overexpression inhibitor, and early diagnosis of incurable diseases and various diseases such as autoimmune diseases including cancer, osteoarthritis, rheumatoid arthritis and dementia.
摘要翻译：公开了用于测定蛋白酶活性的蛋白酶成像用纳米粒子传感器及其制备方法。更具体地，本发明涉及用于测量蛋白酶活性的纳米颗粒传感器，其中荧光团和猝灭剂缀合的肽底物与生物相容性聚合物纳米颗粒缀合。肽底物被蛋白酶特异性裂解。根据本发明的传感器能够抑制荧光材料上猝灭剂具有高灭绝活性的荧光发射。但是如果肽底物被特异性蛋白酶裂解，则强荧光是特异性发射的。因此，该传感器作为筛选新型药物如蛋白酶过表达抑制剂的方法，以及早期诊断不治之症以及各种疾病，如自身免疫性疾病，包括癌症，骨关节炎，类风湿性关节炎和痴呆症，都是特别有用的。

7. 发明授权

US08551727B2 Gold nanoparticle based protease imaging probes and use thereof 有权
标题翻译：基于金纳米颗粒的蛋白酶成像探针及其用途
公开(公告)号：US08551727B2
公开(公告)日：2013-10-08
申请号：US12595078
申请日：2008-04-10
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , Cheol-Hee Ahn , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , Cheol-Hee Ahn , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park
IPC分类号： C12Q1/37 , C12Q1/34 , B82B3/00 , C12N11/14 , C12N11/18
CPC分类号： A61K49/0056 , A61K49/0032 , A61K49/0065 , A61K49/0093 , C12Q1/37
摘要： Disclosed are a metal nanoparticle onto which a peptide substrate specifically degraded by protease and fluorophore are chemically modified for selectively imaging protease expressed in cell and in tissue in a human body, and the use thereof. Also, a quantitative analysis method of protease using the metal nanoparticle, a cell imaging method and a drug screening method of inhibiting a protease overexpression are provided. In detail, the present invention is directed to a metal nanoparticle having a peptide substrate and fluorophore coupled thereto, the peptide substrate and the fluorophore being specifically degraded by due to a protease activated in various ways in cell and in a human body to exhibit fluorescence. Hence, the metal nanoparticle can be used to rapidly screen activation and inhibition of the protease in the imaging manner. Also, the metal nanoparticle is capable of being selectively absorbed into a cell and a tissue so as to be possibly used as a sensor for real-time cell imaging and early diagnosis of non-invasive diseases.
摘要翻译：公开了一种金属纳米颗粒，其上通过蛋白酶和荧光团特异性降解的肽底物被化学修饰以选择性地成像在细胞和人体组织中表达的蛋白酶及其用途。另外，提供了使用金属纳米粒子的蛋白酶的定量分析方法，细胞成像方法和抑制蛋白酶过表达的药物筛选方法。详细地说，本发明涉及一种具有肽底物和与其连接的荧光团的金属纳米颗粒，肽底物和荧光团由于在细胞和人体中以各种方式活化的蛋白酶而被特异性地降解以显示出荧光。因此，金属纳米颗粒可用于以成像方式快速筛选蛋白酶的活化和抑制。此外，金属纳米粒子能够被选择性地吸收到细胞和组织中，以便可能用作用于实时细胞成像和非侵入性疾病的早期诊断的传感器。

8. 发明申请

US20100124757A1 GOLD NANOPARTICLE BASED PROTEASE IMAGING PROBES AND USE THEREOF 有权
标题翻译：基于金纳米粒子的蛋白成像探针及其应用
公开(公告)号：US20100124757A1
公开(公告)日：2010-05-20
申请号：US12595078
申请日：2008-04-10
申请人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , Cheol-Hee Ahn , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park
发明人： Ick-Chan Kwon , Kui-Won Choi , Kwang-Meyung Kim , Cheol-Hee Ahn , In-Chan Youn , Seul-Ki Lee , Kyeong-Soon Park
IPC分类号： C12Q1/37 , C07K2/00
CPC分类号： A61K49/0056 , A61K49/0032 , A61K49/0065 , A61K49/0093 , C12Q1/37
摘要： Disclosed are a metal nanoparticle onto which a peptide substrate specifically degraded by protease and fluorophore are chemically modified for selectively imaging protease expressed in cell and in tissue in a human body, and the use thereof. Also, a quantitative analysis method of protease using the metal nanoparticle, a cell imaging method and a drug screening method of inhibiting a protease overexpression are provided. In detail, the present invention is directed to a metal nanoparticle having a peptide substrate and fluorophore coupled thereto, the peptide substrate and the fluorophore being specifically degraded by due to a protease activated in various ways in cell and in a human body to exhibit fluorescence. Hence, the metal nanoparticle can be used to rapidly screen activation and inhibition of the protease in the imaging manner. Also, the metal nanoparticle is capable of being selectively absorbed into a cell and a tissue so as to be possibly used as a sensor for real-time cell imaging and early diagnosis of non-invasive diseases.
摘要翻译：公开了一种金属纳米颗粒，其上通过蛋白酶和荧光团特异性降解的肽底物被化学修饰以选择性地成像在细胞和人体组织中表达的蛋白酶及其用途。另外，提供了使用金属纳米粒子的蛋白酶的定量分析方法，细胞成像方法和抑制蛋白酶过表达的药物筛选方法。详细地说，本发明涉及一种具有肽底物和与其连接的荧光团的金属纳米颗粒，肽底物和荧光团由于在细胞和人体中以各种方式活化的蛋白酶而被特异性地降解以显示出荧光。因此，金属纳米颗粒可用于以成像方式快速筛选蛋白酶的活化和抑制。此外，金属纳米粒子能够被选择性地吸收到细胞和组织中，以便可能用作用于实时细胞成像和非侵入性疾病的早期诊断的传感器。

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