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US 7,842,682 B2Granted
Boronated metal-phthalocyanines, process for their preparation, pharmaceutical compositions comprising them and use thereof
AssigneeL. Molteni & C. Dei Fratelli Alitti
InventorsGabrio Roncucci, Giulio Jori, Francesca Giuntini, Clara Fabris, Giacomo Chiti, Moira Municchi, Donata Dei
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Abstract
The present invention relates to meta 1-phthalocyanines bearing at least a group containing boron isotopes 11B or 10B, covalently bound to the peripheral positions of meta 1-phthalocyanine nucleus; moreover it refers to the processes for their preparation, the pharmaceutical compositions comprising them and their use for the treatment of neoplastic and dysplastic pathologies.
Claims10
A compound of general formula (I)
- in which:
- Me is selected from the group consisting of Zn, AlOR4 and Si(OR4), wherein R4 is selected from the group consisting of H and C1-C15 alkyl,
- R, R1, R2 and R3, equal or different from one other, are selected from H and groups (G)s-(X)t-(Y-Z)u wherein:
- G is selected from the group consisting of O, S, SO, CH2 and N;
- X is selected from the group consisting of phenyl, linear or branched C1-C10 alkyl, C1-C10 alkenyl and C1-C10 alkynyl;
- Y is selected from the group consisting of S, (CH2)n, phenyl, O—(CH2)n, (CH2)n—O—, (CH2CH2O)n, CONH, NHCO, COO, COS, and 3-mercapto-pyrrolidine-2,5-dione;
- Z is selected from the group consisting of 11B-(o,m,p-carborane), 11B-undecahydrododecaboromercaptyl, 11B-undecahydrododecaborate, 10B-(o,m,p-carborane), 10B-undecahydrododecaboromercaptyl and 10B-undecahydrododecaborate;
- n is an integer comprised between 1 and 10;
- s is 0, 1;
- t is 0, 1;
- u is an integer comprised between 1 and 3;
- with the proviso that at least one among R, R1, R2 and R3 is different from H, and when only one amongst R, R1, R2 and R3 is different from H, u is different from 1;
- and pharmaceutically acceptable salts thereof.
10 more elements
Dependencies are inferred from the claim text.