Ceramoptec Industries, Inc.

Biolitec Pharma Marketing Ltd

Dmitri V Yashunsky

Nikolay Nifantiev

Burkhard Gitter

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 a special spacer connecting at least one photosensitizer to a microorganism receptor (vector) which in turn binds selectively to the surface of a microorganism bringing about photo-destruction upon irradiation. Spacers having hydrophilic structure such as ethylene glycol units and amino carboxyl end capped ethylene glycol units must be used for linking the vector to the photosensitizer. In a preferred embodiment a spacer would have at least 3 ethylene glycol units and be end capped with a carboxyl group on one end and a amino group at the other end. The present invention effectively works to combat bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or at least nearby. Spacers of selected length and structure, in preferred embodiments, are used for linking the vector to the photosensitizer. These conjugate are found to be very effective in combating bacterial infection in the real patient-related environments where blood, serum and other body fluids are always present or a least nearby. A method of use is also provided.

Anti-microbial photodynamic therapy

Water-soluble mono-PEGylated tetrapyrrole derivatives are disclosed, having a formula given by formula 1, 2, or 3 in the specification. A method to produce the above water-soluble mono-PEGylated compounds is also disclosed, comprising an interaction of a tetrapyrrole with an aminopolyethylene glycol containing a functionalized terminal fragment, as well as their use as photosensitizers in photodynamic therapy.

Water-soluble mono-PEGylated tetrapyrrole derivatives for photodynamic therapy and method of production

High purity pharmaceutical-grade water-soluble porphyrin derivatives given by formula 1 or 2 in the specification, and new methods to prepare and use such porphyrin derivatives are disclosed. A preferred method comprises the steps of one- or two-step direct acidic alcoholysis of biological raw material producing a crystalline alkyl pheophorbide, conversion of the obtained alkyl pheophorbide into an acidic porphyrin, and reaction of the acidic porphyrin in water or in an aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises reaction of acidic porphyrins prepared in water or in aqueous organic solution with a hydrophilic organic amine. Another preferred method comprises the additional step of purification of the resultant water-soluble porphyrin derivative by reversed phase chromatography using volatile solvents. The disclosed compounds are useful as photosensitizers for the photodynamic therapy of cancer, infectious and other diseases as well as for light irradiation treatments in other cases.

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Moscow, Russia

Dmitri V Yashunsky