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US 5,965,598 AGranted
Zinc-phthalocyanines and corresponding conjugates, their preparation and use in photodynamic therapy and as diagnostic agents
AssigneeMolteni L. & C. dei Fratelli Alitti Societa di esercizio S.p.A.
InventorsGabrio Roncucci, Donata Dei, Maria Paola De Filippis, Lia Fantetti, Ilaria Masini, Barbara Cosimelli, Giulio Jori
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Abstract
The present invention refers to zinc-phthalocyanines of general formula (I) ##STR1## to processes for their preparation and to their use as phototherapeutic and photodiagnostic agents as free molecules and as conjugates with macromolecular carrier molecules.
Claims20
Compounds of general formula (I) in which:
- R and R.sub.1 represent H or the group X-R.sub.5, where:
- X is chosen in the group consisting of --CH.sub.2 --, O, N, S, C.dbd.O, and ##STR10## where:
- Y is chosen in the group consisting of C.sub.1-10 -alkyl, phenyl possibly substituted, (CH.sub.2 CH.sub.2 O).sub.p, where p ranges from 1 to 4;
- Z is chosen in the group consisting of H, N, O, S, SO.sub.3, --CH--, --CH.sub.2 -- carbon atom, CH.sub.2 O, CONH, (CH.sub.2).sub.q CO.sub.2, where q ranges from 0 to 2;
- R.sub.2 is chosen in the group consisting of H, C.sub.1-12 -alkyl, PO(OEt).sub.2, CH.sub.2 CH.sub.2 NH.sub.2, aryl, and crown ether, or it forms, with the Z group to which it is bound, a saturated or unsaturated heterocycle, possibly substituted, which may contain up to two hetero-atoms chosen among N, O, and S;
- R.sub.3 and R.sub.4, which may be the same or different from one another, are chosen in the group consisting of H, CH.sub.3, and C.sub.2 H.sub.5, C.sub.3-12 alkyl m, n, w, t (independently from one another) are 0 or 1;
- V is an integer comprised between 1 and 5;
- with the proviso that at least one of R and R.sub.1 is always other than H.
5 more elements
Dependencies are inferred from the claim text.