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1. 发明申请

US20110206613A1 METHOD AND APPLICATION OF UNSYMMETRICALLY meso-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PDT 有权
标题翻译：用于PDT的不对称中间取代的PORPHYRINS和CHLORIN的方法和应用
公开(公告)号：US20110206613A1
公开(公告)日：2011-08-25
申请号：US13119907
申请日：2009-09-17
申请人： Arno Wiehe , Daniel Aicher , Christian B .W. Stark , Volker Albrechi , Susanna Gräfe
发明人： Arno Wiehe , Daniel Aicher , Christian B .W. Stark , Volker Albrechi , Susanna Gräfe
IPC分类号： A61K49/00 , C07D487/22 , A61K31/409 , C07K16/00 , C07K2/00 , C07H15/26 , A61K31/7056 , A61P19/02 , A61P29/00 , A61P43/00
CPC分类号： C07D487/22 , C07H15/26
摘要： Biologically active compounds are provided 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 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 reductively cleave the osmate(VI)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：提供了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治疗非肿瘤适应症如关节炎，炎性疾病，病毒或细菌感染，皮肤病学，眼科学或泌尿系统疾病，以及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内消旋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体系转化为二氢卟酚体系，并且如果形成多于一种的异构体，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膜亲和力和增加的PDT功效的两亲化合物。在另一个实施方案中，提供了避免使用气态H 2 S的还原性裂解锇酸酯（VI）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。

2. 发明授权

US09315510B2 Method and application of unsymmetrically meso-substituted porphyrins and chlorins for PDT 有权
标题翻译：用于PDT的不对称内消旋卟啉和二氢卟酚的方法和应用
公开(公告)号：US09315510B2
公开(公告)日：2016-04-19
申请号：US13119907
申请日：2009-09-17
申请人： Arno Wiehe , Daniel Aicher , Christian B. W. Stark , Volker Albrecht , Susanna Gräfe
发明人： Arno Wiehe , Daniel Aicher , Christian B. W. Stark , Volker Albrecht , Susanna Gräfe
IPC分类号： A61K31/409 , C07D487/22 , C07H15/26
CPC分类号： C07D487/22 , C07H15/26
摘要： Biologically active compounds are provided 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 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 reductively cleave the osmate(VI)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：提供了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治疗非肿瘤适应症如关节炎，炎性疾病，病毒或细菌感染，皮肤病学，眼科学或泌尿系统疾病，以及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内消旋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体系转化为二氢卟酚体系，并且如果形成多于一种的异构体，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膜亲和力和增加的PDT功效的两亲化合物。在另一个实施方案中，提供了避免使用气态H 2 S的还原性裂解锇酸酯（VI）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。

3. 发明授权

US09156849B2 Application of β-functionalized dihydroxy-chlorins for PDT 有权
标题翻译：功能化二羟基二氢卟酚对PDT的应用
公开(公告)号：US09156849B2
公开(公告)日：2015-10-13
申请号：US13208917
申请日：2011-08-12
申请人： Daniel Aicher , Arno Wiehe , Christian B. W. Stark , Volker Albrecht , Susanna Gräfe
发明人： Daniel Aicher , Arno Wiehe , Christian B. W. Stark , Volker Albrecht , Susanna Gräfe
IPC分类号： C07D487/22 , A61K38/00 , A61K41/00 , A61K49/00
CPC分类号： C07D487/22 , A61K41/0071 , A61K49/0036
摘要： The present invention provides 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. The compounds are of the class of β-functionalized hydroxy- and dihydroxy-chlorins having the general formula
摘要翻译：本发明提供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治疗非肿瘤适应症如关节炎，炎性疾病，病毒或细菌感染，皮肤病学，眼科学或泌尿系统疾病。这些化合物是具有通式的具有通式的官能化羟基 - 和二羟基 - 二氢卟酚

4. 发明申请

US20130041307A1 APPLICATION OF BETA-FUNCTIONALIZED DIHYDROXY-CHLORINS FOR PDT 有权
标题翻译：用于PDT的功能化二羟基氯化物的应用
公开(公告)号：US20130041307A1
公开(公告)日：2013-02-14
申请号：US13208917
申请日：2011-08-12
申请人： Daniel Aicher , Arno Wiehe , Christian B. W. Stark , Volker Albrechr , Susanna Gräfe
发明人： Daniel Aicher , Arno Wiehe , Christian B. W. Stark , Volker Albrechr , Susanna Gräfe
IPC分类号： A61M37/00 , A61K39/395 , A61K31/407 , A61K9/127 , C07D487/22 , A61K38/00
CPC分类号： C07D487/22 , A61K41/0071 , A61K49/0036
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 β-functionalized 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诊断和治疗应用的光敏剂的生物活性化合物的方法，特别是用于癌症，感染和其它过度增殖性疾病的PDT，荧光诊断和PDT治疗非肿瘤适应症如关节炎，炎症疾病，病毒或细菌感染，皮肤病学，眼科学或泌尿系统疾病。本发明的一个实施方案由合成二酮二氢卟酚作为前体的方法组成。在另一个实施方案中，这些前体转化为官能化的羟基和二羟基二氢卟酚。另一个实施方案是提供具有更高膜亲和力和增加的PDT功效的两亲化合物。另一个实施方案包括将所需异构体配制成待注射的脂质体制剂，以避免不期望的作用，如注射部位的沉淀或四吡咯体系的延迟药代动力学。

5. 发明申请

US20120263625A1 GLYCO-SUBSTITUTED DIHYDROXY-CHLORINS AND ß-FUNCTIONALIZED CHLORINS FOR ANTI-MICROBIAL PHOTODYNAMIC THERAPY 有权
标题翻译：用于抗微生物光化学治疗的GLYCO取代的二羟基氯和ß-功能氯化物
公开(公告)号：US20120263625A1
公开(公告)日：2012-10-18
申请号：US13189113
申请日：2011-07-22
申请人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
发明人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
IPC分类号： C07H15/26 , A61L2/08
CPC分类号： A61K31/185 , A61K31/19 , A61K31/409 , A61K31/7056 , A61K41/0071 , A61K47/549 , C07H15/26
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 connecting dihydroxychlorins or β-functionalized chlorins to carbohydrate moieties. These conjugates are found to be very effective in combating bacterial infections caused by Gram-positive and Gram-negative bacteria, including their resistant strains. Significantly, they are also effective in complex environments, including blood, serum, and other body fluids which are present in patient's body. A method of use to control pathogenic microorganisms in human and animals 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二羟基二氢卟酚或二官能化的二氢卟酚连接到碳水化合物部分。发现这些缀合物对抗革兰氏阳性和革兰氏阴性细菌（包括其抗性菌株）引起的细菌感染是非常有效的。值得注意的是，它们在复杂的环境中也是有效的，包括血液，血清和患者体内存在的其他体液。还提供了用于控制人和动物中的病原微生物的方法。

6. 发明授权

US09308185B2 Glyco-substituted dihydroxy-chlorins and β-functionalized chlorins for anti-microbial photodynamic therapy 有权
标题翻译：糖基取代的二羟基二氢卟酚和用于抗微生物光动力治疗的功能性二氢卟酚
公开(公告)号：US09308185B2
公开(公告)日：2016-04-12
申请号：US13189113
申请日：2011-07-22
申请人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
发明人： Daniel Aicher , Volker Albrecht , Burkhard Gitter , Christian B. W. Stark , Arno Wiehe
IPC分类号： C07H15/26 , A61K31/409 , A61K31/185 , A61K31/19 , A61K31/7056 , A61K41/00 , A61K47/48
CPC分类号： A61K31/185 , A61K31/19 , A61K31/409 , A61K31/7056 , A61K41/0071 , A61K47/549 , C07H15/26
摘要： Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The conjugates are of the class of compounds of dihydroxychlorins or β-functionalized chlorins connected to carbohydrate moieties and having the general formula
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。缀合物是与碳水化合物部分连接的二羟基二氢卟酚或二官能化二氢卟酚的化合物，具有通式

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