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US 8,540,966 B2Granted
Contrast agents endowed with high relaxivity
AssigneeBracco Imaging S.P.A.
InventorsSilvio Aime, Matteo Galli, Luciano Lattuada, Pierfrancesco Morosini, Fulvio Uggeri, Kondareddiar Ramalingam
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Abstract
The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.
Claims17
A compound of formula (III)
- wherein:
- R is, independently, H or a C2-C70 aminopolyol moiety comprising a straight or branched alkyl chain substituted by from 2 to 30 hydroxyl groups, said chain being optionally interrupted by one or more groups selected from —O—, —NH—, —N<, —CO—, —CONH—, —NHCO—, —CON< or >NCO—;
- and optionally substituted by one or more C4-C10 cyclic units;
- L is, independently, a direct bond or a divalent straight or branched linker moiety between R and the rest of the molecule, comprising at most 20 carbon atoms;
- together with the corresponding protonated forms of the carboxy (—COOH) groups;
- or a physiologically acceptable salt of such ligand;
- with the proviso that at least one of the R groups is other than H.
4 more elements
A compound according to claim 2
- wherein:
- 1a) L1 is a direct bond, L2 is —CH2CO—, R1 is H, and R2 is group A2;
- 2a) L1 is a direct bond, L2 is —CH2CO—, R1 is H, and R2 is group B1;
- 3a) L1 is a direct bond, L2 is —CH2CO—, R1 is H, and R2 is group B2;
- 4a) L1 is —CH2CH2CO—, L2 is a direct bond, R1 is group B1, and R2 is H;
- 5a) L1 is —CH2CH2CO—, L2 is a direct bond, R1 is group B2, and R2 is H;
- 6a) L1 is —CH2CH2CO—, L2 is a direct bond, R1 is group G3, and R2 is H;
- 7a) L1 is —CH2CH2CO—, L2 is —CH2CO—, R1 is group B1, and R2 is group B1;
- 8a) L1 is —CH2CH2CO—, L2 is —CH2CO—, R1 is group G3, and R2 is group G3;
- 9a) L1 is —CH2CO—, L2 is a direct bond, R1 is group B1, and R2 is H;
- 10a) L1 is —CH2CO—, L2 is a direct bond, R1 is group B2, and R2 is H;
- 11a) L1 is —CH2CH2CO—, L2 is —CH2CO—, R1 is group B2, and R2 is group B2;
- 12a) L1 is a direct bond, L2 is —CH2CO—, R1 is H, and R2 is group C1;
- 13a) L1 is —CH2CH2CO—, L2 is a direct bond, R1 is group B2, and R2 is H;
- 14a) L1 is a direct bond, L2 is —CH2CO—, R1 is H, and R2 is group G7;
- 15a) L1 is —CH2CH2CO—, L2 is a direct bond, R1 is group C1, and R2 is H;
- and wherein any group A, B, C, G is as defined in claim 10;
- and the physiologically acceptable salts thereof.
15 more elements
Dependencies are inferred from the claim text.