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US 2006/0040914 A1Published application
Meso-substituted porphyrins
AssigneeL. Molteni & C. dei Fratelli Alitti Societa di Esercizio S.p.A.
InventorsGabrio Roncucci, Donata Dei, Francesca Giuntini, Giacomo Chiti, Daniele Nistri, Lia Fantetti, Valentina Paschetta, Annalisa Cocchi
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Abstract
Meso-substituted porphyrins of general formula (I) suitable for the use as photosensitising agents, in particular in photodynamnic therapy, are herein described.
Claims20
Compounds of general formula (I)
- wherein
- R is the following group of formula (II)
- wherein
- X is selected from the group consisting of O, S, CH2, COO, CH2CO, O(CH2)2O, O(CH2)3O and N;
- Z is selected from between N and CH2N;
- Y is selected from aliphatic groups, linear or branched, saturated or unsaturated, having from 1 to 10 carbon atoms, and phenyl, possibly substituted, or Y forms with Z a saturated or unsaturated heterocycle, possibly substituted, comprising up to two heteroatoms selected from the group consisting of N, O and S;
- R4 and R5, equal or different from each other, are selected from H and alkyl groups having from 1 to 3 carbon atoms, or they form with the Z group a saturated or unsaturated heterocycle, possibly substituted, comprising up to two heteroatoms selected from the group consisting of N, O and S;
- R6 is selected from H and aliphatic groups, linear or branched, saturated or unsaturated, having from 1 to 5 carbon atoms, possibly substituted with alkylamine or alkylammonium groups having alkyl chains comprising from 1 to 5 carbon atoms, or forming a saturated heterocycle comprising up to two heteroatoms selected from between O and N;
- d, m, and n, equal of different from each other, are selected from 0 and 1;
- v and s, equal or different from each other, are integers comprised between 1 and 3;
- R1 is selected from H and a group of formula (III)
- wherein
- G is selected from H and P—(CH2)I—(W)f-J, wherein
- P is selected from the group consisting of O, CH2, CO2, NHCONH and CONH;
- I is an integer comprised between 0 and 5;
- W is selected from the group consisting of O, CO2, CONH and NHCONH;
- f is selected from between 0 and 1;
- J is H or an alkyl group (CH2)q—CH3, wherein q is an integer comprised between 0 and 20;
- R2 and R3, equal or different from each other, are selected from between R and R1, wherein R and R1 are defined as above,
- M is chosen from 2H and a metal selected from the group consisting of Zn, Mg, Pt, Pd, Si(OR7)2, Ge(OR7)2 and AlOR7, wherein R7 is chosen from between H and C1-C15 alkyl, and pharmaceutically acceptable salts thereof,
- with the exception of the following compounds:
- a) compound of formula (I) wherein M is 2H, R1═R3═H, R═R2 is a group of formula (II) in which s is 1,X is O, Y is (CH2)3, v is 1, Z is N, n=d=1, m is 0, and R4═R5═H;
- and
- b) compound of formula (I) wherein M is 2H, R1═R3═H, R1═R2 is a group of formula (II) in which s is 1, X is O, Y is (CH2)3, v is 1, Z is N, n=d=1, m is 0, R4 and R5 form with Z a phthalimido group.
21 more elements
11-14. (canceled)
17-18. (canceled)
Dependencies are inferred from the claim text.