公开(公告)号：EP2616065A1

公开(公告)日：2013-07-24

申请号：EP11869827.3

申请日：2011-07-22

申请人： Biolitec Pharma Marketing Ltd ,  CeramOptec GmbH

发明人： AICHER, Daniel ,  ALBRECHT, Volker ,  GITTER, Burkhard ,  STARK, Christian, B. W. ,  WIEHE, Arno

IPC分类号： A61K31/409 ,  A61K31/19 ,  A61K31/185 ,  A61P31/04 ,  A61P31/00

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 &bgr;-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类，并具有通式

公开(公告)号：EP2870159A2

公开(公告)日：2015-05-13

申请号：EP11810524.6

申请日：2011-08-12

申请人： CeramOptec GmbH ,  Biolitec Pharma Marketing Ltd.

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.

公开(公告)号：EP2350058A2

公开(公告)日：2011-08-03

申请号：EP09815180.6

申请日：2009-09-17

申请人： CeramOptec GmbH

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

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.