Process for preparing chlorins and their pharmaceutical uses

Details Process for preparing chlorins and their pharmaceutical uses Process for preparing chlorins and their pharmaceutical uses

C - Chemistry, Metallurgy

07

D

C07D 487/22 (2006.01) A61K 31/409 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2741429

The invention provides the methods of preparation, properties, pharmaceutical compositions and methods of thera-py of sulfonated chlorins and bacterioclorins designed for the photodynamic therapy (PDT) of hyperproliferative tissues such as tumors, hyperproliferative blood vessels and other disorders or abnormalies that are responsive to PDT. In particular, the econom-ical large-scale synthesis of stable chlorins and bacteriochlorins is described. Their properties were tailored to meet those of ideal photosensitizers for PDT. In another embodiment, pharmaceutical compositions and methods of therapy for systemic administra-tion are provided. In a further embodiment, pharmaceutical compositions and methods of therapy for topical administration are also provided. Further provided is a method of labeling a target tissue and providing an image of that tissue by fluorescence of magnetic resonance imaging.

La présente invention concerne les méthodes de synthèse, les propriétés, les compositions pharmaceutiques et les méthodes thérapeutiques liées aux bactériochlorines et aux chlorines sulfonées conçues pour la thérapie photodynamique (PDT) de tissus hyperprolifératifs comme les tumeurs, les vaisseaux sanguins hyperprolifératifs et autres pathologies ou anomalies sensibles à la PDT. En particulier, la présente invention concerne la synthèse peu onéreuse à grande échelle de bactériochlorines et de chlorines stables. Leurs propriétés sont conçues de manière à constituer des agents photosensibilisants idéaux en PDT. Dans un autre mode d'application, la présente invention concerne des compositions pharmaceutiques et des méthodes thérapeutiques pour administration systémique. Dans un mode d'application supplémentaire, la présente invention concerne des compositions pharmaceutiques et des méthodes thérapeutiques pour administration locale. La présente invention concerne également une méthode de marquage d'un tissu cible et d'obtention d'une image de ce tissu par fluorescence de résonance magnétique.

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