Water-soluble porphyrin derivatives and methods of their preparation
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United States of America Patent
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app pub date -
Nov 27, 2002
filing date -
Jun 1, 2001
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Abandoned
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Abstract
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: 1 where: R.sup.1=--CH.dbd.CH.sub.2, --CH(OAlk)CH.sub.3, --CHO, --C(O)CH.sub.3; --CH.sub.2CH.sub.3; --CH(Alk)CH(COAlk).sub.2, --CH.sub.2CH(COAlk).sub.2, --CH(Alk)CH.sub.2COAlk, --CH(Alk)CH.sub.2CH(OH)CH.sub.3, --CH.sub.2CH.sub.2CH(OH)CH.sub.3 R.sup.2=--CH.sub.3, --CHO, --CH(OH)Alk, --CH.dbd.CHAlk, CH.sub.2OH, CH.sub.2OAlk; R.sup.3=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.
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