Biolitec Pharma Marketing Ltd

Biolitec Unternehmensbeteiligungs II Ag

Alfred E. Tiefenbacher Gmbh & Co. Kg

Biolitec Unternehmensberatungs II Ag

Daniel Aicher

Volker Albrecht

Arno Wiehe

Christian B W Stark

Susanna Gräfe

Burkhard Gitter

Ruslan Staver

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 HS 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.

[object Object]

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 &#x3b2;-functionalized chlorins connected to carbohydrate moieties and having the general formula 

Glyco-substituted dihydroxy-chlorins and &#x3b2;-functionalized chlorins for anti-microbial photodynamic therapy

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 &#x3b2;-functionalized hydroxy- and dihydroxy-chlorins having the general formula 

Application of &#x3b2;-functionalized dihydroxy-chlorins for PDT

Growing community of inventors

Berlin, Germany

Daniel Aicher