Metal chelates of polyamino macrocyclic derivatives and their use in diagnostic imaging.

摘要

Compound of formula (I) ** (See formula) ** 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, identical or different, represent, independently; 3.1) a hydrogen atom; 3.2) a - (CH2) a-CONR1R2, - (CH2) a-NR1COR2 or ** (See formula) ** with: each R1, R2 independently represents an H atom; alkyl or alkenyl chain C7-C30 substituted or unsubstituted, linear or branched or cyclic, optionally interrupted with O, NH, NR3 or S, wherein R3 is a C1-C3 alkyl; or a group ** (See formula) ** with b = 0, 1 or 2, Z represents O- or OH, R5 represents a saturated or unsaturated group of at least 6 carbon atoms, advantageously in C6 to C30 optionally substituted and "spacer" represents a CH2CH2 or polyalkylene glycol group; 3.3) a group ** (See formula) ** with: d comprised between 0 and 3; Y selected from O and S; R7 selected from H, OH, CH3, OCH3 R1 and R2 are as defined above with the proviso that X1, X2, X3, X4 and X5 are not all H and that at least one of X1, X2, X3, X4, X5 is a lipophilic group selected from: * a group - (CH2) a-CONR1R2, - (CH2) a-NR1COR2 or ** (See formula) with **; each R1, R2 independently represent an alkyl chain or alkenyl C7 to C30, linear or branched or cyclic, optionally interrupted by one or two atoms or groups O, S, NH or NR3 wherein R3 is alkyl C1-C3; or a group ** (See formula) ** with b = 0, 1 or 2, Z represents O- or OH, R5 represents a saturated or unsaturated group of at least 6 carbon atoms, C6 to C30 advantageously optionally substituted, and "spacer" represents a CH2CH2 or polyalkylene glycol group; * A group ** (See formula) ** with: d comprised between 0 and 3; Y selected from O and S; R7 selected from H, OH, CH3, OCH3; each R1, R2 independently represents an alkyl chain or alkenyl C7 to C30, linear or branched or cyclic, optionally interrupted by one or two atoms or groups O, S, NH, or NR3 wherein R3 is alkyl C1-C3 ; or a group ** (See formula) ** with b = 0, 1 or 2, Z represents O- or OH, R5 represents a saturated or unsaturated group of at least 6 carbon atoms, advantageously in C6 to C30 optionally substituted and "spacer" represents a CH2CH2 or polyalkylene glycol group; 4) A1, A2, B1, B2, C1, C2, D1, D2, E1, E2, F1, F2, independently of one another represent H or CH3 or cyclohexyl group; 5) K represents C or N or CH or NH or N + R4, R4 being a group C 1 -C 6 selected from alkyl, benzyl or substituted benzyl; 6) G represents nothing or O no or NHR 4, R 4 is as defined above and pharmaceutically acceptable salts thereof.