WATER-SOLUBLE PORPHYRINE DERIVATIVES FOR PHOTODYNAMIC THERAPY, THEIR USE AND MANUFACTURE

摘要

The invention relates to the chemistry of biologically active compounds, namely, to a new method to prepare water-soluble porphyrin derivatives, particularly chlorin derivatives having general formulae (1). The compounds of the present invention are useful as photosensitizers, as drug substances and optionally in suitable drug products, for the photodynamic therapy of cancer, of infectious and other diseases, as well as for light irradiation treatments in other cases. B is a ring having the structure: where: R1=-CH=CH2, -CH(OAlk)CH3, -CHO, -C(O)CH3; -CH2CH3; -CH(Alk)CH(COAlk)2, -CH2CH(COAlk)2, -CH(Alk)CH2COAlk, -CH(Alk)CH2CH(OH)CH3, -CH2CH2CH(OH)CH3 R2=-CH3, -CHO, -CH(OH)Alk, -CH=CHAlk, CH2OH, CH2OAlk; R3=H or lower alkyl; G=hydrophilic organic amine (f.ex. N-methyl-D-glucamine and other amino-group containing carbohydrate derivatives, TRIS, aminoacids, oligopeptides). Alk=alkyl substituent.