Biolitec Unternehmensbeteiligungs Iii Ag

Westfalische Wilhelms-universität Münster

Biolitec Unternehmensbeteiligungs Ii Ag

Universität Paderborn

Biolitec Research Gmbh

Biolitec Pharma Marketing Ltd

Freie Universitat Berlin

Biolitec Holding Gmbh & Co Kg

Volker Albrecht

Wolfgang Neuberger

Arno Wiehe

Rainer Haag

Burkhard Gitter

Susanna Gräfe

Dietrich Scheglmann

Gerhard Wieland

Danilo Castro

Benjamin Florian Hohlfeld

Dorika Steen

Susanna Graefe

Hartwig Richard Arthur Golf

Hagen Von Briesen

Klaus Langer

Hans-Ulrich Reißig

Sylvia Wagner

Gerhard Dieter Wieland

Wolfgang Birnbaum

Jingjiang Sun

Dirk Kuckling

Juliane Anderski

Dennis Mulac

Laura Mahlert

Beate Röder

Annegret Preuss

Michael Staegemann

Karin Löw

Thomas Knobloch

Hans-Ulrich Reissig

Claudia Simone Gutsche

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, opthamological 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 other embodiments the nucleophilic substitution on pentafluorophenyl-substituted tetrapyrroles is used to obtain compounds with a high PDT-efficacy. 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 formulating the desired tetrapyrrole photosensitizer into a pharmaceutical formulation to be injected into the body avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems.

Specifically meso-substituted porphyrins and chlorins for photodynamic therapy

Biologically active compounds and their methods of preparation are provided that may 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 non-tumorous indications such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, otorhinolaryngology disorders, ophthalmological or urological disorders. As the compounds exhibit also toxicity against targets (tumor cells, bacteria, inflammation-related cells) without light these biologically active compounds may also be used for the light-independent treatment of such indications. Embodiments also include methods to synthesize boron dipyrromethene complex structures incorporating a substituted 2,3,5,6-tetrafluorophenyl-dipyrromethene (2,3,5,6-tetrafluorophenyldipyrrin) unit or a substituted 3-nitrophenyl-dipyrromethene (3-nitrophenyl-dipyrrin) unit. Amphiphilic compounds with increased anti-tumour and anti-bacterial efficacy are also provided. Specifically, this is achieved by substitution with bromine atoms and sugar moieties.

Application of boron dipyrromethene derivatives in anti-tumor and anti-bacterial therapy

The present invention generally relates to the formation, chemistry and application of biologically active compositions. More particularly, the present invention relates to certain dyes, specifically porphyrin and chlorin derivatives, in combination with inventive polymers, i.e. light-cleavable polymers, that can be used as photosensitizer compositions for a wide range of light irradiation treatments such as photodynamic therapy of cancer, infections and other diseases. The dye derivatives may either be adsorbed on, or incorporated in, or attached to specific polymers, which as well form part of the invention.

Polymer-particle light-cleavable carrier systems for photodynamic therapy

Biologically active compounds and their methods of preparation are provided that may 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 non-tumorous indications such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, otorhinolaryngology disorders, ophthalmological or urological disorders. As the compounds exhibit also toxicity against targets (tumor cells, bacteria inflammation-related cells) without light these biologically active compounds may also be used for the light-independent treatment of such indications. Embodiments also include methods to synthesize iridium(III) complex structures incorporating a substituted 2,3,5,6-tetrafluorophenyl-dipyrromethene (2,3,5,6-tetratfluorophenyldipyrrin) unit or a substituted 3-nitrophenyl-dipyrromethene (3-nitrophenyl-dipyrrin) unit. Amphiphilic compounds with increased anti-tumour and anti-bacterial efficacy are also provided. Specifically, this is achieved by substitution with bromine atoms and sugar moieties.

Application of dipyrrinato-iridium complexes in anti-tumor and anti-bacterial therapy

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Nuthetal, Germany

Volker Albrecht