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1. 发明申请

US20110021973A1 FORMULATIONS FOR COSMETIC AND WOUND CARE TREATMENTS WITH PHOTOSENSITIZERS AS FLUORESCENT MARKERS 审中-公开
标题翻译：使用光敏剂作为荧光标记的化妆和治疗护理品的配方
公开(公告)号：US20110021973A1
公开(公告)日：2011-01-27
申请号：US12896614
申请日：2010-10-01
申请人： Wolfgang Neuberger , Susanna Gräfe , Nikolay E. Nifantiev
发明人： Wolfgang Neuberger , Susanna Gräfe , Nikolay E. Nifantiev
IPC分类号： A61M37/00
CPC分类号： A61L27/50
摘要： Photoactive materials, such as photosensitizers, are used as fluorescent markers for in vivo detection of the distribution of the injected filler material during cosmetic treatments. In one preferred embodiment, liposomal formulated temoporfin is used, as the photoactive component, in very small concentrations along with fillers for cosmetic and wound healing applications. Fillers, which can be used in the invention, include collagen, hyaluronic acids and other synthetic or natural products which are generally used in wound healing, scar reduction and other such medical applications. In a preferred embodiment, the formulated photosensitizer is coupled to the filler so that tracking is possible over longer periods of time A liposomal formulated photosensitizer is injected with the fillers into the treatment area, and is irradiated with laser light shortly after injection. The emitted fluorescence is measured by a special non-invasive device. Thereby it is possible to monitor the injection site and the distribution of the injected solution around the injection site. When irradiated with laser or other light source, the fluorescence of the photosensitizer is detected using a fluorescence detector, which permits tracking the filler at injection site and in the injection volume.
摘要翻译：光敏剂如光敏剂被用作荧光标记物，用于在化妆品处理期间体内检测注入的填充材料的分布。在一个优选的实施方案中，作为光活性成分的脂质体配制的temoporfin以非常小的浓度与用于化妆品和伤口愈合应用的填充剂一起使用。可用于本发明的填充剂包括胶原蛋白，透明质酸和通常用于伤口愈合，瘢痕减少等医学应用中的其它合成或天然产物。在优选的实施方案中，将配制的光敏剂偶联到填料，使得可以在更长时间内进行跟踪。将脂质体配制的光敏剂注射到处理区域中，并在注射后不久用激光照射。发射的荧光通过特殊的非侵入性装置测量。因此，可以监测注射部位和注射部位周围注射溶液的分布情况。当用激光或其他光源照射时，使用荧光检测器检测光敏剂的荧光，其允许在注射部位和注射体积中追踪填料。

2. 发明申请

US20080214460A1 Formulations for cosmetic and wound care treatments with photosensitizers as fluorescent markers 审中-公开
标题翻译：用光敏剂作为荧光标记的化妆品和伤口护理治疗的配方
公开(公告)号：US20080214460A1
公开(公告)日：2008-09-04
申请号：US12006911
申请日：2008-01-07
申请人： Wolfgang Neuberger , Susanna Grafe , Nikolay E. Nifantiev
发明人： Wolfgang Neuberger , Susanna Grafe , Nikolay E. Nifantiev
IPC分类号： A61K38/00
CPC分类号： A61L27/50
摘要： Photoactive materials, such as photosensitizers, are used as fluorescent markers for in vivo detection of the distribution of the injected filler material during cosmetic treatments. In one preferred embodiment, liposomal formulated temoporfin is used, as the photoactive component, in very small concentrations along with fillers for cosmetic and wound healing applications. Fillers, which can be used in the invention, include collagen, hyaluronic acids and other synthetic or natural products which are generally used in wound healing, scar reduction and other such medical applications. In a preferred embodiment, the formulated photosensitizer is coupled to the filler so that tracking is possible over longer periods of time A liposomal formulated photosensitizer is injected with the fillers into the treatment area, and is irradiated with laser light shortly after injection. The emitted fluorescence is measured by a special non-invasive device. Thereby it is possible to monitor the injection site and the distribution of the injected solution around the injection site. When irradiated with laser or other light source, the fluorescence of the photosensitizer is detected using a fluorescence detector, which permits tracking the filler at injection site and in the injection volume.
摘要翻译：光敏剂如光敏剂被用作荧光标记物，用于在化妆品处理期间体内检测注射的填充材料的分布。在一个优选的实施方案中，作为光活性成分的脂质体配制的temoporfin以非常小的浓度与用于化妆品和伤口愈合应用的填充剂一起使用。可用于本发明的填充剂包括胶原蛋白，透明质酸和通常用于伤口愈合，瘢痕减少等医学应用中的其它合成或天然产物。在优选的实施方案中，配制的光敏剂与填料偶联，使得可以在更长的时间内进行跟踪。将脂质体配制的光敏剂与填料一起注入处理区域，并在注射后不久用激光照射。发射的荧光通过特殊的非侵入性装置测量。因此，可以监测注射部位和注射部位周围注射溶液的分布情况。当用激光或其他光源照射时，使用荧光检测器检测光敏剂的荧光，其允许在注射部位和注射体积中追踪填料。

3. 发明申请

US20090162423A1 Formulations for cosmetic and wound care treatments with photosensitizes as fluorescent markers 审中-公开
标题翻译：用于化妆品和伤口护理治疗的制剂，作为荧光标记物进行光敏化
公开(公告)号：US20090162423A1
公开(公告)日：2009-06-25
申请号：US12004325
申请日：2007-12-20
申请人： Wolfgang Neuberger , Susanna Grafe , Nikolay E. Nifantiev
发明人： Wolfgang Neuberger , Susanna Grafe , Nikolay E. Nifantiev
IPC分类号： A61K9/127 , A61K38/00 , A61P17/00 , A61K31/715
CPC分类号： A61K31/715 , A61K9/0019 , A61K9/06 , A61L27/50
摘要： Photoactive materials, such as photosensitizers, are used as fluorescent markers for in vivo detection of the distribution of the injected filler material during cosmetic treatments. In one preferred embodiment, liposomal formulated temoporfin is used, as the photoactive component, in very small concentrations along with fillers for cosmetic and wound healing applications. Fillers, which can be used in the invention, include collagen, hyaluronic acids and other synthetic or natural products which are generally used in wound healing, scar reduction and other such medical applications. In a preferred embodiment, the formulated photosensitizer is coupled to the filler so that tracking is possible over longer periods of time A liposomal formulated photosensitizer is injected with the fillers into the treatment area, and is irradiated with laser light shortly after injection. The emitted fluorescence is measured by a special non-invasive device. Thereby it is possible to monitor the injection site and the distribution of the injected solution around the injection site. When irradiated with laser or other light source, the fluorescence of the photosensitizer is detected using a fluorescence detector, which permits tracking the filler at injection site and in the injection volume.
摘要翻译：光敏剂如光敏剂被用作荧光标记物，用于在化妆品处理期间体内检测注射的填充材料的分布。在一个优选的实施方案中，作为光活性成分的脂质体配制的temoporfin以非常小的浓度与用于化妆品和伤口愈合应用的填充剂一起使用。可用于本发明的填充剂包括胶原蛋白，透明质酸和通常用于伤口愈合，瘢痕减少等医学应用中的其它合成或天然产物。在优选的实施方案中，将配制的光敏剂偶联到填料，使得可以在更长时间内进行跟踪。将脂质体配制的光敏剂注射到处理区域中，并在注射后不久用激光照射。发射的荧光通过特殊的非侵入性装置测量。因此，可以监测注射部位和注射部位周围注射溶液的分布情况。当用激光或其他光源照射时，使用荧光检测器检测光敏剂的荧光，其允许在注射部位和注射体积中追踪填料。

4. 发明申请

US20090030257A1 Anti-microbial photodynamic therapy 审中-公开
标题翻译：抗微生物光动力疗法
公开(公告)号：US20090030257A1
公开(公告)日：2009-01-29
申请号：US11880974
申请日：2007-07-25
申请人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
发明人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
IPC分类号： A61N5/00 , A61K31/407 , A61P31/04
CPC分类号： A61K31/407 , A61K41/0071 , A61K47/64
摘要： Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The key to these conjugates is a special spacer connecting at least one photosensitizer to a microorganism receptor (vector) which in turn binds selectively to the surface of a microorganism bringing about photo-destruction upon irradiation. Spacers having hydrophilic structure such as ethylene glycol units and amino carboxyl end capped ethylene glycol units must be used for linking the vector to the photosensitizer. In a preferred embodiment a spacer would have at least 3 ethylene glycol units and be end capped with a carboxyl group on one end and a amino group at the other end. The present invention effectively works to combat bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or at least nearby of selected length and structure, in preferred embodiments, are used for linking the vector to the photosensitizer. These conjugate are found to be very effective in combating bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or a least nearby. A method of use is also provided.
摘要翻译：提供了用于治疗和预防人和动物中致病微生物引起的感染性疾病的抗微生物分子缀合物。这些缀合物的关键是连接至少一种光敏剂与微生物受体（载体）的特殊间隔物，微生物受体（载体）又依赖于微生物的表面结合，从而在照射时引起光损伤。必须使用具有亲水性结构的间隔物，例如乙二醇单元和氨基羧基封端的乙二醇单元，用于将载体与光敏剂连接。在优选的实施方案中，间隔物将具有至少3个乙二醇单元，并且在一端具有羧基并在另一端具有氨基末端封端。本发明有效地用于抵抗真实的患者相关环境中的细菌感染，其中血液，血清和其他体液总是存在或至少在选定的长度和结构附近，在优选的实施方案中，用于将载体连接到光敏剂。发现这些结合物在血液，血清和其他体液总是存在或至少在附近的真实患者相关环境中对抗细菌感染是非常有效的。还提供了一种使用方法。

5. 发明授权

US06777402B2 Water-soluble porphyrin derivatives for photodynamic therapy, their use and manufacture 失效
标题翻译：水溶性卟啉衍生物用于光动力学治疗，其使用和制造
公开(公告)号：US06777402B2
公开(公告)日：2004-08-17
申请号：US10151764
申请日：2002-05-20
申请人： Nikolay E. Nifantiev , Dmitri V. Yashunsky
发明人： Nikolay E. Nifantiev , Dmitri V. Yashunsky
IPC分类号： C07D48722
CPC分类号： C07D487/22 , A61K41/0071
摘要： High purity pharmaceutical-grade water-soluble porphyrin derivatives given by formula 1 or 2 in the specification, and new methods to prepare and use such porphyrin derivatives are disclosed. A preferred method comprises the steps of one- or two-step direct acidic alcoholysis of biological raw material producing a crystalline alkyl pheophorbide, conversion of the obtained alkyl pheophorbide into an acidic porphyrin, and reaction of the acidic porphyrin in water or in an aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises reaction of acidic porphyrins prepared in water or in aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises the additional step of purification of the resultant water-soluble porphyrin derivative by reversed phase chromatography using volatile solvents. The disclosed compounds are useful as photosensitizers for the photodynamic therapy of cancer, infectious and other diseases as well as for light irradiation treatments in other cases.
摘要翻译：公开了通式1或2所示的高纯度药物级水溶性卟啉衍生物，以及制备和使用这种卟啉衍生物的新方法。一种优选的方法包括以下步骤：生成生物原料的一步或两步直接酸性醇解产生结晶烷基脱镁叶绿体，将获得的烷基脱镁叶酸转化为酸性卟啉，以及酸性卟啉在水或有机水中的反应溶液与亲水性有机胺。另一个优选的方法包括在水中或在有机水溶液中制备的酸性卟啉与亲水性有机胺的反应。另一个优选的方法包括通过使用挥发性溶剂的反相色谱法纯化所得水溶性卟啉衍生物的附加步骤。所公开的化合物可用作癌症，感染性和其它疾病的光动力学治疗的光敏剂以及其它情况下的光照射治疗。

6. 发明申请

US20090326434A1 Anti-Microbial Photodynamic Therapy 有权
标题翻译：抗微生物光动力疗法
公开(公告)号：US20090326434A1
公开(公告)日：2009-12-31
申请号：US12375241
申请日：2007-07-27
申请人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
发明人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
IPC分类号： A61N5/06 , C12N15/63 , C07K2/00 , A61K31/7088
CPC分类号： A61K31/407 , A61K41/0071 , A61K47/64
摘要： Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The key to these conjugates is a special spacer connecting at least one photosensitizer to a microorganism receptor (vector) which in turn binds selectively to the surface of a microorganism bringing about photo-destruction upon irradiation. Spacers having hydrophilic structure such as ethylene glycol units and amino carboxyl end capped ethylene glycol units must be used for linking the vector to the photosensitizer. In a preferred embodiment a spacer would have at least 3 ethylene glycol units and be end capped with a carboxyl group on one end and a amino group at the other end. The present invention effectively works to combat bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or at least nearby. Spacers of selected length and structure, in preferred embodiments, are used for linking the vector to the photosensitizer. These conjugate are found to be very effective in combating bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or a least nearby. A method of use is also provided.
摘要翻译：提供了用于治疗和预防人和动物中致病微生物引起的感染性疾病的抗微生物分子缀合物。这些缀合物的关键是连接至少一种光敏剂与微生物受体（载体）的特殊间隔物，微生物受体（载体）又依赖于微生物的表面结合，从而在照射时引起光损伤。必须使用具有亲水性结构的间隔物，例如乙二醇单元和氨基羧基封端的乙二醇单元，用于将载体与光敏剂连接。在优选的实施方案中，间隔物将具有至少3个乙二醇单元，并且在一端具有羧基并在另一端具有氨基末端封端。本发明有效地抵抗在血液，血清和其他体液总是存在或至少在附近的真实的患者相关环境中的细菌感染。在优选实施方案中，所选长度和结构的间隔物用于将载体连接至光敏剂。发现这些结合物在血液，血清和其他体液总是存在或至少在附近的真实患者相关环境中对抗细菌感染是非常有效的。还提供了一种使用方法。

7. 发明授权

US09216166B2 Anti-microbial photodynamic therapy 有权
标题翻译：抗微生物光动力疗法
公开(公告)号：US09216166B2
公开(公告)日：2015-12-22
申请号：US12375241
申请日：2007-07-27
申请人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
发明人： Nikolay E. Nifantiev , Burkhard Gitter , Dmitri V. Yashunsky
IPC分类号： A61K31/407 , A61K47/48 , A61K41/00
CPC分类号： A61K31/407 , A61K41/0071 , A61K47/64
摘要： Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The key to these conjugates is a special spacer connecting at least one photosensitizer to a microorganism receptor (vector) which in turn binds selectively to the surface of a microorganism bringing about photo-destruction upon irradiation. Spacers having hydrophilic structure such as ethylene glycol units and amino carboxyl end capped ethylene glycol units must be used for linking the vector to the photosensitizer. In a preferred embodiment a spacer would have at least 3 ethylene glycol units and be end capped with a carboxyl group on one end and a amino group at the other end. The present invention effectively works to combat bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or at least nearby. Spacers of selected length and structure, in preferred embodiments, are used for linking the vector to the photosensitizer. These conjugate are found to be very effective in combating bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or a least nearby. A method of use is also provided.
摘要翻译：提供了用于治疗和预防人和动物中致病微生物引起的感染性疾病的抗微生物分子缀合物。这些缀合物的关键是将至少一种光敏剂与微生物受体（载体）连接的特殊间隔物，微生物受体（载体）又依赖于微生物的表面结合，从而在照射时引起光损伤。必须使用具有亲水性结构的间隔物，例如乙二醇单元和氨基羧基封端的乙二醇单元，用于将载体与光敏剂连接。在优选的实施方案中，间隔物将具有至少3个乙二醇单元，并且在一端具有羧基并在另一端具有氨基末端封端。本发明有效地抵抗在血液，血清和其他体液总是存在或至少在附近的真实的患者相关环境中的细菌感染。在优选实施方案中，所选长度和结构的间隔物用于将载体连接至光敏剂。发现这些结合物在血液，血清和其他体液总是存在或至少在附近的真实患者相关环境中对抗细菌感染是非常有效的。还提供了一种使用方法。

8. 发明申请

US20090081281A1 Photosensitizer Formulation for Topical Applications 审中-公开
标题翻译：用于局部应用的光敏剂配方
公开(公告)号：US20090081281A1
公开(公告)日：2009-03-26
申请号：US12226893
申请日：2007-05-08
申请人： Gerard Farmer , Dietrich Scheglmann , Volker Albrecht , Nikolay E. Nifantiev
发明人： Gerard Farmer , Dietrich Scheglmann , Volker Albrecht , Nikolay E. Nifantiev
IPC分类号： A61K9/127 , A61K31/40
CPC分类号： A61K9/127 , A61K9/0014 , A61K41/0071
摘要： Highly flexible penetrating liposomal carrier systems are formulated with enhanced skin penetration properties. These specialized formulations of highly flexible penetrating liposomal delivery systems comprise one or more phospholipids, lysophosphatides and hydrophobic photosensitizer. This new formulations can squeeze liposomal particles through intercellular regions of stratum corneum as intact structures, and, in this way, deliver encapsulated photosensitizer to the epidermis, dermis, hypodermis and surroundings. The penetrating liposomal formulation provides therapeutically effective amounts of the hydrophobic photosensitizer through topical application with better skin penetration thus improving drug targeting and the efficacy of photodynamic therapy (PDT).
摘要翻译：高度灵活的渗透性脂质体载体体系被配制成具有增强的皮肤渗透性能。高度灵活的渗透性脂质体递送系统的这些专门制剂包含一种或多种磷脂，溶血磷脂和疏水性光敏剂。这种新配方可以将脂质体颗粒通过角质层的细胞间隙挤压成为完整的结构，并以这种方式将包封的光敏剂递送到表皮，真皮，皮下组织和周围环境。渗透性脂质体制剂通过局部应用提供治疗有效量的疏水性光敏剂，具有更好的皮肤渗透性，从而改善药物靶向和光动力疗法（PDT）的功效。

9. 发明申请

US20080274169A1 Photosensitizer formulations for topical applications 审中-公开
标题翻译：用于局部应用的光敏剂配方
公开(公告)号：US20080274169A1
公开(公告)日：2008-11-06
申请号：US11800147
申请日：2007-05-04
申请人： Gerard Farmer , Dietrich Scheglmann , Volker Albrecht , Nikolay E. Nifantiev
发明人： Gerard Farmer , Dietrich Scheglmann , Volker Albrecht , Nikolay E. Nifantiev
IPC分类号： A61K9/127 , A61K31/11 , A61K31/18 , A61P17/00 , A61K31/35 , A61K31/40
CPC分类号： A61K9/0014 , A61K9/127 , A61K31/11 , A61K31/18 , A61K31/35 , A61K31/40 , A61K41/0071
摘要： Highly flexible penetrating liposomal carrier systems are formulated with enhanced skin penetration properties. These specialized formulations of highly flexible penetrating liposomal delivery systems comprise one or more phospholipids, lysophosphatides and hydrophobic photosensitizer. This new formulations can squeeze liposomal particles through intercellular regions of stratum corneum as intact structures, and, in this way, deliver encapsulated photosensitizer to the epidermis, dermis, hypodermis and surroundings. The penetrating liposomal formulation provides therapeutically effective amounts of the hydrophobic photosensitizer through topical application with better skin penetration thus improving drug targeting and the efficacy of photodynamic therapy (PDT).
摘要翻译：高度灵活的渗透性脂质体载体体系被配制成具有增强的皮肤渗透性能。高度灵活的渗透性脂质体递送系统的这些专门制剂包含一种或多种磷脂，溶血磷脂和疏水性光敏剂。这种新配方可以将脂质体颗粒通过角质层的细胞间隙挤压成为完整的结构，并以这种方式将包封的光敏剂递送到表皮，真皮，皮下组织和周围环境。渗透性脂质体制剂通过局部应用提供治疗有效量的疏水性光敏剂，具有更好的皮肤渗透性，从而改善药物靶向和光动力疗法（PDT）的功效。

10. 发明授权

US06949581B2 Water-soluble mono-PEGylated tetrapyrrole derivatives for photodynamic therapy and method of production 有权
标题翻译：用于光动力学治疗的水溶性单PEG化四吡咯衍生物及其制备方法
公开(公告)号：US06949581B2
公开(公告)日：2005-09-27
申请号：US10394877
申请日：2003-03-21
申请人： Nikolay E. Nifantiev , Dmitri V. Yashunsky
发明人： Nikolay E. Nifantiev , Dmitri V. Yashunsky
IPC分类号： C07D487/22 , A61K31/409 , A61P35/00
CPC分类号： C07D487/22 , A61K41/0071 , A61K47/60
摘要： Water-soluble mono-PEGylated tetrapyrrole derivatives are disclosed, having a formula given by formula 1, 2, or 3 in the specification. A method to produce the above water-soluble mono-PEGylated compounds is also disclosed, comprising an interaction of a tetrapyrrole with an aminopolyethylene glycol containing a functionalized terminal fragment, as well as their use as photosensitizers in photodynamic therapy.
摘要翻译：公开了水溶性单PEG化四吡咯衍生物，其具有在说明书中由式1,2或3给出的式。还公开了产生上述水溶性单PEG化化合物的方法，其包括四吡咯与含有官能化末端片段的氨基聚乙二醇的相互作用，以及它们在光动力疗法中作为光敏剂的用途。

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