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US 2009/0214441 A1Published application
Lipophilic Chelates and Their Use in Imaging
AssigneeGuerbet
InventorMarc Port
Life of this patent
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Abstract
The invention relates to chelate compounds which can be used in MRI, the chelates being intended to be conveyed by lipophilic transporters, such as lipid nanoparticles or liposomes. The invention also relates to compounds comprising, in association, these chelates and these transporters, if appropriate connected via chemical bonding groups, and to their use in diagnostic imaging, it being possible for this association additionally to comprise biological targeting markers, denoted biovectors.
Claims11
Compound of formula (I)
- in which:
- 1) represents a single or double bond;
- 2) Q represents a nitrogen atom or an NH radical;
- 3) X1, X2, X3, X4 and X5, which are identical or different, independently represent, provided that X1, X2, X3, X4 and X5 are not all H and that at least one of X1, X2, X3, X4 and X5 is a lipophilic group:
- 3.1) a hydrogen atom;
- 3.2) a —(CH2)a—CONR1R2, —(CH2)a—NR1COR2 or
- group, with;
- a=1, 2 or 3;
- each R1 or R2 group independently represents an H atom;
- a substituted or unsubstituted and linear, branched or cyclic C7-C30 alkyl or alkenyl chain optionally interrupted by O, NH, NR3 or S, where R3 is a C1-C3 alkyl;
- or a group
- with b=0, 1 or 2, Z represents O− or OH, R5 represents a saturated or unsaturated and optionally substituted group of at least 6 carbon atoms, and spacer represents a CH2CH2 or polyalkylene glycol group;
- 3.3) a group
- with:
- d between 0 and 3;
- Y chosen from O and S;
- R7 chosen from H, OH, CH3 or OCH3;
- R1 and R2 are as defined above;
- 4) A1, A2, B1, B2, C1, C2, D1, D2, E1, E2, F. and F2 represent, independently of one another, an H or CH3 or cyclohexyl group;
- 5) K represents C or N or CH or NH or N+R4 with R4 a C1-C6 group chosen from alkyl, benzyl or substituted benzyl;
- 6) G is not present or represents O or NHR4, with R4 as defined above;
- and its pharmaceutically acceptable salts.
19 more elements
Compound of formula (I)
- in which:
- 1) represents a single or double bond
- 2) Q represents a nitrogen atom or an NH radical;
- 3) X1 or X2, which are identical or different, independently represent a hydrogen atom, a —(CH2)a—CONR1R2, (CH2)a—NR1COR2 or
- group, with:
- a=1, 2 or 3;
- each R1 or R2 group independently represents an H atom, a substituted or unsubstituted and linear, branched or cyclic C7-C30 alkyl or alkenyl chain, or a group
- with b=0, 1 or 2, Z represents O− or OH, R5 represents a saturated or unsaturated and optionally substituted group of at least 6 carbon atoms, and spacer represents a CH2CH2 or polyalkylene glycol group;
- 4) X3, X4 and X5, which are identical or different, have the same meaning as X1 or X2 provided that X1, X2, X3, X4 and X5 are not all H and at least one of X1, X2, X3, X4 and X5 is a lipophilic group or X3, X4 and X5, which are identical or different, represent
- with:
- d between 0 and 3;
- Y chosen from O and S;
- R7 chosen from H, OH, CH3 or OCH3;
- R1 and R2 are as defined above;
- 5) A1, A2, B1, B2, C1, C2, D1, D2, E1, E2, F1 and F2 represent, independently of one another, an H or CH3 or cyclohexyl group;
- 6) K represents C or N or CH or NH or N+R4 with R4 a C1-C6 group chosen from alkyl, benzyl or substituted benzyl;
- 7) G is not present or represents O or NHR4, with R4 as defined above;
- and its pharmaceutically acceptable salts.
15 more elements
Dependencies are inferred from the claim text.