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1. 发明申请

WO2010078941A1 CALCIUMPHOSPHATE-BASED NANOPARTICLES AS CARRIER-SYSTEMS FOR PHOTODYNAMIC THERAPY 审中-公开
标题翻译：基于钙磷酸盐的纳米颗粒作为光化学治疗的载体系统
公开(公告)号：WO2010078941A1
公开(公告)日：2010-07-15
申请号：PCT/EP2009/009142
申请日：2009-12-18
申请人： BIOLITEC AG , UNIVERSITÄT DUISBURG-ESSEN , SCHWIERTZ, Janine , GANESAN, Kathirvel , EPPLE, Matthias , WIEHE, Arno , GRÄFE, Susanna , GITTER, Burkhard , ALBRECHT, Volker
发明人： SCHWIERTZ, Janine , GANESAN, Kathirvel , EPPLE, Matthias , WIEHE, Arno , GRÄFE, Susanna , GITTER, Burkhard , ALBRECHT, Volker
IPC分类号： A61K41/00 , A61K9/16
CPC分类号： A61K9/5115 , A61K41/0057 , A61K41/0071 , A61K49/0093 , Y10S977/773
摘要： The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, p TPPP is a preferred hydrophilic photosensitizer for photodynamic tumor therapy. In another preferred embodiment, hydrophilic cationic and anionic photosensitizers, especially those of the phenazinium, phenothiazinium and xanthenes series have been found to inactive pathogen bacteria and are the preferred photosensitizers to be formulated in calcium phosphate nanoparticle formulations for antibacterial photodynamic therapy. In another embodiment, photosensitizing nanoparticle formulations are useful to locate cells, tissues or bacteria by using fluorescence imaging methods.
摘要翻译：本发明提供负载药物的光敏剂纳米颗粒制剂及其制备光动力疗法的方法，其包括疏水或亲水性光敏剂，纳米颗粒磷酸钙，在某些情况下，辅助试剂如稳定剂。本发明的基于磷酸钙的纳米颗粒制剂提供优异的储存稳定性和用于静脉内或局部给药的治疗有效量的光敏剂。在优选的实施方案中，四吡咯衍生物如卟啉，二氢卟酚和细菌二氢卟酚是拟配制在用于光动力学肿瘤治疗的磷酸钙纳米颗粒制剂中的优选的疏水性光敏剂。另外，pTPPP是用于光动力学肿瘤治疗的优选的亲水性光敏剂。在另一个优选的实施方案中，亲水性阳离子和阴离子光敏剂，特别是phenazineium，吩噻嗪和呫吨系列的光敏剂已经被发现为无活性的病原体细菌，并且是配制在用于抗菌光动力学治疗的磷酸钙纳米颗粒制剂中的优选光敏剂。在另一个实施方案中，光敏纳米颗粒制剂可用于通过使用荧光成像方法定位细胞，组织或细菌。

2. 发明申请

WO2011071970A2 NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT) 审中-公开
标题翻译：基于聚合（DL-LACTIC-CO-GLYCOLIC ACID）（PLGA）用于光化学治疗（PDT）的纳米载体系统
公开(公告)号：WO2011071970A2
公开(公告)日：2011-06-16
申请号：PCT/US2010/059367
申请日：2010-12-08
申请人： BIOLITEC, INC. , LANGER, Klaus , KNOBLOCH, Thomas , RÖDER, Beate , PREUSS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , von BRIESEN, Hagen , LÖW, Karin , WAGNER, Sylvia
发明人： LANGER, Klaus , KNOBLOCH, Thomas , RÖDER, Beate , PREUSS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , von BRIESEN, Hagen , LÖW, Karin , WAGNER, Sylvia
IPC分类号： A61K47/30 , A61K33/20 , A61K9/127 , A61P35/00 , A61P27/02 , A61P29/00
CPC分类号： A61K9/5153 , A61K33/20 , A61K41/0071
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticutate formulations for clinical use in photodynamic therapy comprising a hydrophobic photosensitizer, poly(lactic-co-glycolic) acid and stabilizing agents are provided. These nanoparticulate pharmaceutical formulations provide therapeutically effective amounts of photosensitizer for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers, whose efficacy and safety are enhanced by such nanoparticulate formulations. It also leaches the method of preparing PLGA-based nanoparticles under sterile conditions. In one of the preferred embodiments of the present invention PLGA-based nanoparticles have a mean particle size less than 500nm and the photosensitizer is temoporfϊn, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin ( m THPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3- hydroxyphenyl)-chlorin ( m THPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3- hydroxyphenyl)-porphyrin ( m THPP). The formulations can be used for treating hyperptasic and neoplasia conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：提供了在储存中稳定的组合物以及用于临床用于光动力疗法的基于药物的纳米颗粒制剂的方法，其包括疏水性光敏剂，聚（乳酸 - 共 - 乙醇酸）酸和稳定剂。这些纳米颗粒药物制剂提供治疗有效量的用于肠胃外给药的光敏剂。特别地，四吡咯衍生物可以用作光敏剂，其功效和安全性通过这种纳米颗粒制剂增强。它还浸出了在无菌条件下制备基于PLGA的纳米颗粒的方法。在本发明的一个优选实施方案中，基于PLGA的纳米颗粒具有小于500nm的平均粒度，并且光敏剂是temoporf TM，5,10,15,20-四（3-羟基苯基） - 氯化物（mTHPC）。在另一个实施方案中，将光敏剂2,3-二羟基-5,10,15,20-四（3-羟基苯基） - 青霉素（mTHPD-OH）配制成用于肠胃外给药的纳米颗粒。然而，在另一个实施方案中，优选的光敏剂是5,10,15,20-四（3-羟基苯基） - 卟啉（mTHPP）。该制剂可用于治疗高血压和瘤形成症状，炎症问题，更具体地用于靶向肿瘤细胞。

3. 发明申请

WO2011071968A3 NANOPARTICLE CARRIER SYSTEMS BASED ON HUMAN SERUM ALBUMIN FOR PHOTODYNAMIC THERAPY 审中-公开
公开(公告)号：WO2011071968A3
公开(公告)日：2011-06-16
申请号：PCT/US2010/059364
申请日：2010-12-08
申请人： BIOLITEC, INC. , LANGER, Klaus , WACKER, Matthias , RÖDER, Beate , PRUESS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , VON BRIESEN, Hagen , WAGNER, Sylvia
发明人： LANGER, Klaus , WACKER, Matthias , RÖDER, Beate , PRUESS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , VON BRIESEN, Hagen , WAGNER, Sylvia
IPC分类号： A61K38/38 , A61K38/18 , A61K31/54 , A61K31/40 , A61K49/00 , A61P35/00
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate formulations for photodynamic therapy comprising a hydrophobic photosensitizer, human serum albumin (HSA) and stabilizing agent are provided. These nanoparticulate formulations provide therapeutically effective amounts of photosensitizer (PS) for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers whose efficacy and safety are enhanced by such nanoparticulate formulations. A method of preparing the HSA-based nanoparϋcles under sterile conditions is also provided. In one of the preferred embodiments of the present invention temoporfin, a hydrophobic PS, is formulated as a nanoparticle for parenteral administration. The formulations are useful for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells.

4. 发明申请

WO2005082878A1 HKI10311129, NEUES ANTIBIOTIKUM, VERFAHREN ZU DESSEN HERSTELLUNG UND DESSEN VERWENDUNG 审中-公开
标题翻译： HKI10311129，新的抗生素，方法ITS和使用
公开(公告)号：WO2005082878A1
公开(公告)日：2005-09-09
申请号：PCT/DE2005/000186
申请日：2005-02-02
申请人： HANS-KNÖLL-INSTITUT FÜR NATURSTOFF-FORSCHUNG e.V. , GRÄFE, Karin, Brigitte, Charlotte , GRÄFE, Andrea , GRÄFE, Susanna , MÖLLMANN, Ute , HEROLD, Kerstin , ROTH, Martin , GROTH, Ingrid , GOLLMICK, Friedrich
发明人： MÖLLMANN, Ute , HEROLD, Kerstin , ROTH, Martin , GROTH, Ingrid , GOLLMICK, Friedrich
IPC分类号： C07D309/10
CPC分类号： C07D309/10
摘要： Die Erfindung betrifft ein neues Antibiotikum, HKI10311129, mit dem Molekulargewicht 1113 und der Summenformel C 56 H 75 NO 22 , ein Verfahren zu dessen Herstellung unter Verwendung eines Mikroorganismus, Streptomyces spec. DSM 13059, und dessen Verwendung als antibakterielles Heilmittel mit besonderer Wirksamkeit gegen Infektionen mit grampositiven Bakterien, insbesondere mit Antibiotika-resistenten Keimen.
摘要翻译：本发明涉及一种新的抗生素，HKI10311129，与分子量1113的具有经验式C56H75NO22，其制造通过使用微生物，链霉菌的方法。 DSM 13059，其与抗革兰氏阳性菌，特别是耐抗生素细菌感染特别有效的抗菌药使用。

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