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1. 发明申请

WO2012012809A2 APPLICATION OF β-FUNCTIONALIZED DIHYDROXY-CHLORINS FOR PDT 审中-公开
标题翻译：用于PDT的功能性二羟基氯化物的应用
公开(公告)号：WO2012012809A2
公开(公告)日：2012-01-26
申请号：PCT/US2011/047576
申请日：2011-08-12
申请人： CERAMOPTEC GMBH , CERAMOPTEC INDUSTRIES, 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 , A61P35/00 , A61P17/00
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 β -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β-无功羟基 - 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO2010033678A3 NOVEL METHOD AND APPLICATION OF UNSYMMETRICALLY MESO-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PDT 审中-公开
公开(公告)号：WO2010033678A3
公开(公告)日：2010-03-25
申请号：PCT/US2009/057283
申请日：2009-09-17
申请人： CERAMOPTEC INDUSTRIES, 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 , C07D403/06 , A61K31/40 , A61K31/409 , A61P35/00
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(VΪ)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.

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