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1. 发明申请

WO2011071970A3 NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT) 审中-公开
标题翻译：基于用于光动力疗法（PDT）的聚（DL-乳酸 - 共 - 甘油酸）（PLGA）的纳米颗粒载体系统
公开(公告)号：WO2011071970A3
公开(公告)日：2011-11-17
申请号：PCT/US2010059367
申请日：2010-12-08
申请人： BIOLITEC INC , LANGER KLAUS , KNOBLOCH THOMAS , ROEDER BEATE , PREUSS ANNEGRET , ALBRECHT VOLKER , GRAEFE SUSANNA , WIEHE ARNO , VON BRIESEN HAGEN , LOEW KARIN , WAGNER SYLVIA
发明人： LANGER KLAUS , KNOBLOCH THOMAS , ROEDER BEATE , PREUSS ANNEGRET , ALBRECHT VOLKER , GRAEFE SUSANNA , WIEHE ARNO , VON BRIESEN HAGEN , LOEW KARIN , WAGNER SYLVIA
IPC分类号： A61K47/30 , A61K9/127 , A61K33/20 , A61P27/02 , A61P29/00 , A61P35/00
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 temoporf?n, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin (mTHPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3- hydroxyphenyl)-chlorin (mTHPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3- hydroxyphenyl)-porphyrin (mTHPP). The formulations can be used for treating hyperptasic and neoplasia conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：提供贮存稳定的组合物和临床用于光动力治疗的药物基纳米颗粒剂制剂的制备方法，其包含疏水性光敏剂，聚（乳酸 - 共 - 乙醇酸）酸和稳定剂。这些纳米微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而得到增强。它也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的纳米粒子具有小于500nm的平均粒径，并且光敏剂是temoporfΔn，5,10,15,20-四（3-羟基苯基） - 二氢卟酚（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） - 二氢卟酚（mTHPD-OH）配制成用于胃肠外施用的纳米颗粒。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）。所述制剂可用于治疗过度炎症和瘤形成病症，炎症问题，并且更具体地用于靶向肿瘤细胞。

2. 发明申请

WO2011071968A2 NANOPARTICLE CARRIER SYSTEMS BASED ON HUMAN SERUM ALBUMIN FOR PHOTODYNAMIC THERAPY 审中-公开
标题翻译：基于人血清白蛋白的纳米载体系统用于光化学治疗
公开(公告)号：WO2011071968A2
公开(公告)日：2011-06-16
申请号：PCT/US2010059364
申请日：2010-12-08
申请人： BIOLITEC INC , LANGER KLAUS , WACKER MATTHIAS , ROEDER BEATE , PRUESS ANNEGRET , ALBRECHT VOLKER , GRAEFE SUSANNA , WIEHE ARNO , VON BRIESEN HAGEN , WAGNER SYLVIA
发明人： LANGER KLAUS , WACKER MATTHIAS , ROEDER BEATE , PRUESS ANNEGRET , ALBRECHT VOLKER , GRAEFE SUSANNA , WIEHE ARNO , VON BRIESEN HAGEN , WAGNER SYLVIA
IPC分类号： A61K38/38 , A61K31/40 , A61K31/54 , A61K38/18 , A61K49/00 , A61P35/00
CPC分类号： A61K31/409 , A61K9/5169 , A61K41/0071
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 nanopar?cles 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.
摘要翻译：提供了在储存中稳定的组合物以及用于光动力疗法的药物基纳米颗粒制剂的制备方法，其包括疏水性光敏剂，人血清白蛋白（HSA）和稳定剂。这些纳米颗粒制剂提供用于胃肠外给药的治疗有效量的光敏剂（PS）。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样的纳米颗粒制剂增强。还提供了在无菌条件下制备基于HSA的纳米颗粒的方法。在本发明的一个优选实施方案中，将Temoporfin，疏水性PS配制成用于肠胃外给药的纳米颗粒。该制剂可用于治疗过度和肿瘤状况，炎症问题，更具体地涉及靶向肿瘤细胞。

3. 发明申请

WO2010129337A2 NEW ORAL FORMULATIONS FOR TETRAPYRROLE DERIVATIVES 审中-公开
标题翻译：新的口服制剂用于四环素衍生物
公开(公告)号：WO2010129337A2
公开(公告)日：2010-11-11
申请号：PCT/US2010032766
申请日：2010-04-28
申请人： CERAMOPTEC IND INC , GRAEFE SUSANNA , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , GERHARD WIELAND , WIEHE ARNO , FAHR ALBERT
发明人： GRAEFE SUSANNA , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , GERHARD WIELAND , WIEHE ARNO , FAHR ALBERT
IPC分类号： A61K9/16 , A61K9/20 , A61K31/122 , A61K31/495 , A61P31/04 , A61P35/00
CPC分类号： A61K31/409 , A61K9/0065 , A61K9/127 , A61K9/1271 , A61K31/498
摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.
摘要翻译：提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热熔融挤出物和纳米颗粒。在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

4. 发明申请

WO2010129340A3 NOVEL PHOTOSENSITIZER FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口腔管理的新型光敏剂配方
公开(公告)号：WO2010129340A3
公开(公告)日：2011-04-07
申请号：PCT/US2010032780
申请日：2010-04-28
申请人： CERAMOPTEC IND INC , FARMER GERARD , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , GERHARD WIELAND , WIEHE ARNO , GRAEFE SUSANNA
发明人： FARMER GERARD , NIFANTIEV NIKOLAY , ALBRECHT VOLKER , NEUBERGER WOLFGANG , SCHEGLMANN DIETRICH , GERHARD WIELAND , WIEHE ARNO , GRAEFE SUSANNA
IPC分类号： A61K31/498 , A61K31/122 , A61K31/40 , A61P31/04 , A61P35/00
CPC分类号： A61K31/122 , A61K31/40 , A61K31/498 , A61K41/0071
摘要： The present invention provides novel drug formulations for oral administration for diverse medical applications including anticancer, antimetastatic, antibacterial, antifungal, antiprotozoic, antiviral, antiprionic and PDT treatments for diagnostic and therapeutic purposes. In a preferred embodiment the oral drug formulation comprises a photosensitizer and suitable excipients and may be administered in multiple doses over an extended period of time with exposure to activating radiation occurring generally between individual doses or in a light-independent manner. In another preferred embodiment PDT methods for treating hyperplasia and neoplasia, for localizing hyperplasic and neoplasic tissues and pathogen bacteria by fluorescence, for treating infections caused by pathogen bacteria in complex body fluids and for fat reduction, skin disorders and vascular diseases are provided.
摘要翻译：本发明提供用于口服给药以用于各种医学应用的新型药物制剂，包括用于诊断和治疗目的的抗癌，抗转移，抗细菌，抗真菌，抗原生动脉，抗病毒，止痒和PDT治疗。在优选的实施方案中，口服药物制剂包含光敏剂和合适的赋形剂，并且可以在延长的时间段内以多个剂量施用，暴露于通常在单独剂量之间或以轻轻独立的方式发生的活化辐射。在另一个优选实施方案中，提供了用于治疗增生和瘤形成的PDT方法，用于通过荧光定位超基质和新生组织和病原体细菌，用于治疗复杂体液中由病原体引起的感染和用于减脂，皮肤病和血管疾病。

5. 发明申请

WO2012012809A3 APPLICATION OF ß-FUNCTIONALIZED DIHYDROXY-CHLORINS FOR PDT 审中-公开
标题翻译： ß-功能化二羟基氯在PDT中的应用
公开(公告)号：WO2012012809A3
公开(公告)日：2012-05-18
申请号：PCT/US2011047576
申请日：2011-08-12
申请人： CERAMOPTEC GMBH , CERAMOPTEC IND INC , AICHER DANIEL , WIEHE ARNO , STARK CHRISTIAN B W , ALBRECHT VOLKER , GRAFE SUSANNA
发明人： AICHER DANIEL , WIEHE ARNO , STARK CHRISTIAN B W , ALBRECHT VOLKER , GRAFE SUSANNA
IPC分类号： C07D487/22 , A61K31/409 , A61P17/00 , A61P35/00
CPC分类号： A61K31/409 , C07D487/22
摘要： The present invention provides methods to obtain biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders. An embodiment of the present invention consists of a method to synthesize diketo-chlorins as precursors. In yet another embodiment these precursors are converted to ß-unctionalized hydroxy- and dihydroxy-chlorins. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT-efficacy. Another embodiment consists of the formulation of the desired isomer into a liposomal formulation to be injected avoiding undesirable effects like precipitation at the injection site or delayed pharmacokinetics of the tetrapyrrole systems.
摘要翻译：本发明提供了获得可用作光敏剂的生物活性化合物的方法，所述光敏剂用于诊断和治疗应用，特别是用于癌症的PDT，感染和其他过度增殖性疾病，非肿瘤性适应症如关节炎，炎症的荧光诊断和PDT治疗疾病，病毒或细菌感染，皮肤病，眼科或泌尿系统疾病。本发明的一个实施方案由合成作为前体的二酮 - 二氢卟酚的方法组成。在又一个实施方案中，将这些前体转化成β-官能化羟基 - 和二羟基 - 二氢卟酚。另一个实施方案是提供具有较高膜亲和性和增加的PDT-功效的两亲化合物。另一个实施方案包括将期望的异构体配制成待注射的脂质体制剂，避免不希望的效应，如注射部位的沉淀或四吡咯系统的延迟的药代动力学。

6. 发明申请

WO2010033678A8 NOVEL METHOD AND APPLICATION OF UNSYMMETRICALLY MESO-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PDT 审中-公开
标题翻译：用于PDT的非对称性取代的PORPHYRINS和CHLORIN的新方法和应用
公开(公告)号：WO2010033678A8
公开(公告)日：2014-12-18
申请号：PCT/US2009057283
申请日：2009-09-17
申请人： CERAMOPTEC IND INC , WIEHE ARNO , AICHER DANIEL , STARK CHRISTIAN B W , ALBRECHT VOLKER , GRAFE SUSANNA
发明人： WIEHE ARNO , AICHER DANIEL , STARK CHRISTIAN B W , ALBRECHT VOLKER , GRAFE SUSANNA
IPC分类号： C07D403/14 , A61K31/40 , A61K31/409 , A61P35/00 , C07D403/06
CPC分类号： C07D487/22 , C07H15/26
摘要： Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproiiferative diseases, fluorescence diagnosis and PDT treatment of a non- turaorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, opthamologica! or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso- substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT- efficacy. In another embodiment a method to reductsvely cleave the osmate(V&Idigr;)ester avoiding the use of gaseous H2S is provided. In another embodiment substituents are identified that via their steric and/or electronic influence direct the dihydroxylation or reduction with diimine so that one isomer is favored. Another embodiment consists of formulate the desired isomer into a liposomal formulation to be injected avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems.
摘要翻译：可用作诊断和治疗应用的光敏剂的生物活性化合物，特别是用于癌症，感染和其它过度增生性疾病的PDT，荧光诊断和PDT治疗非变性指征如关节炎，炎性疾病，病毒或细菌感染，皮肤科，眼科学！或提供泌尿系统疾病，并提供以药物质量获得它们的方法。一个实施方案由合成具有定义的中间取代基排列的卟啉的方法组成，然后通过二羟基化或还原将该卟啉系统转化为二氢卟酚体系，并且如果形成多于一种异构体，则通过色谱法分离，或者在正常或反向相二氧化硅。在另一个实施方案中，选择卟啉上的取代基以指导还原或二羟基化为二氢卟酚，从而选择性地形成某种异构体。另一个实施方案是提供具有更高的膜亲和力和增加的PDT功效的两性化合物。在另一个实施方案中，提供了避免使用气态H 2 S的方法来还原劈裂锇酸酯（V＆Idigr）酯。在另一个实施方案中，鉴定了取代基，通过它们的空间和/或电子影响直接使二羟基化或还原与二亚胺，使得一种异构体是有利的。另一个实施方案包括将所需的异构体配制成待注射的脂质体制剂，避免不期望的作用，如四吡咯体系的溶解性问题或延迟的药代动力学。

7. 发明申请

WO2010033678A2 NOVEL METHOD AND APPLICATION OF UNSYMMETRICALLY MESO-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PDT 审中-公开
标题翻译：用于PDT的非对称性取代的PORPHYRINS和CHLORIN的新方法和应用
公开(公告)号：WO2010033678A2
公开(公告)日：2010-03-25
申请号：PCT/US2009057283
申请日：2009-09-17
申请人： CERAMOPTEC IND INC , WIEHE ARNO , AICHER DANIEL , STARK CHRISTIAN B W , GRAFE SUSANNA
发明人： WIEHE ARNO , AICHER DANIEL , STARK CHRISTIAN B W , GRAFE SUSANNA
IPC分类号： C07D403/14 , A61K31/40 , A61K31/409 , A61P35/00 , C07D403/06
CPC分类号： C07D487/22 , C07H15/26
摘要： Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproiiferative diseases, fluorescence diagnosis and PDT treatment of a non- turaorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, opthamologica! or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso- substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT- efficacy. In another embodiment a method to reductsvely cleave the osmate(V?)ester avoiding the use of gaseous H2S is provided. In another embodiment substituents are identified that via their steric and/or electronic influence direct the dihydroxylation or reduction with diimine so that one isomer is favored. Another embodiment consists of formulate the desired isomer into a liposomal formulation to be injected avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems.
摘要翻译：可用作诊断和治疗应用的光敏剂的生物活性化合物，特别是用于癌症，感染和其它过度增生性疾病的PDT，荧光诊断和PDT治疗非变性指征如关节炎，炎性疾病，病毒或细菌感染，皮肤科，眼科学！或提供泌尿系统疾病，并提供以药物质量获得它们的方法。一个实施方案由合成具有定义的中间取代基排列的卟啉的方法组成，然后通过二羟基化或还原将该卟啉系统转化为二氢卟酚体系，并且如果形成多于一种异构体，则通过色谱法分离，或者在正常或反向相二氧化硅。在另一个实施方案中，选择卟啉上的取代基以指导还原或二羟基化为二氢卟酚，从而选择性地形成某种异构体。另一个实施方案是提供具有更高的膜亲和力和增加的PDT功效的两性化合物。在另一个实施方案中，提供了避免使用气态H 2 S的减少锇酸酯（V 2）酯的方法。在另一个实施方案中，鉴定了取代基，通过它们的空间和/或电子影响直接使二羟基化或还原与二亚胺，使得一种异构体是有利的。另一个实施方案包括将所需的异构体配制成待注射的脂质体制剂，避免不期望的作用，如四吡咯体系的溶解性问题或延迟的药代动力学。

8. 发明专利

DE10127544A1 Photodynamic therapy used for killing tumor cells in humans, by application of light in presence of carbonyl-substituted chlorin compound as oxidation stable photosensitizer 未知
公开(公告)号：DE10127544A1
公开(公告)日：2002-12-12
申请号：DE10127544
申请日：2001-06-05
申请人： ROEDER BEATE
发明人： WIEHE ARNO , ROEDER BEATE , SENGE MATHIAS O
IPC分类号： A61K31/409 , A61K41/00 , A61K45/06
摘要： In a photodynamic therapy method for killing tumor cells in humans by application of light to photosensitizers in, on or in the vicinity of the cells to be destroyed, the photosensitizer is a chlorin (I) carrying a carbonyl group in a beta -position of the tetrapyrrole ring system. A photodynamic therapy method for non-invasive reduction of tumor cells in the human organism involves directly or indirectly killing the cells by application of light to chlorin photosensitizers of formula (I) in, on or in the vicinity of the cells to be destroyed. M = 2H or metal; R -R = alkyl or aryl (both optionally substituted, specifically by alkoxy, OH, NH2 or COOH), and R = 1-7C alkyl. (N.B. These definitions of substituents are taken from the disclosure, since no definitions are given in the claims).

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