Patent ID: 8772446

Claim:
A bifunctional chelating agent of the formula (I): wherein: -M- is Q 1 , Q 2 and Q 4 are independently H or R; Q 5 is H, R or R 1 ″; Q 6 is H or R 1 ″; Q 7 is H or R; A 1 and A 2 form together with the atoms to which they are attached a C 6 -C 10 -aryl, C 6 —C 1-10 -heteroaryl, C 3 -C 5 -cycloalkyl, C 7 -C 10 -cycloalkyl or C 3 -C 10 -heterocyclyl group; R is —C(O)-L, —(CHR 2 ) p COR 3 or —(CHR 2 ) p PO 2 R 4 R 5 ; Q 3 is H, —(CHR 2 ) w COR 3 or —(CHR 2 ) w PO 2 R 4 R 5 ; R 1 , R 1 ′ and R 1 ″ are independently each R 2 is independently hydrogen; C 1 -C 4 alkyl or (C 1 -C 2 alkyl)phenyl; each R 3 , R 4 and R 5 are independently OH, an —O-protecting group or a leaving group; R 6 is H; OH; an alkyl-LG or alkoxy-LG, wherein LG is a leaving group; a boronate ester or a leaving group; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon—carbon bond; Z 1 and Z 2 are independently CH or N; m is an integer from 0 to 10 inclusive; n is 0 or 1; p is 1 or 2; r is 0 or 1; w is 0 or 1; z is 1 or 2; L is a linker/spacer group covalently bonded to, and replacing one hydrogen atom of the carbon atom to which it is joined, said linker/spacer group being represented by the formula (II): wherein: s is an integer of 0 or 1; t is an integer of 0 to 20 inclusive; R 7 , R 8 and R 9 are independently H; an electrophilic, nucleophilic or electron-rich moiety that allows for covalent attachment to a carrier comprising a biotargeting group, a lipophilic moiety or a biosensor; a protected form or a precursor of the electrophilic, nucleophilic or electron-rich moiety; or a synthetic linker having an electrophilic, nucleophilic or electron-rich moiety that allows for covalent attachment to the carrier comprising a biotargeting group, a lipophilic moiety or a biosensor, or a protected form or a precursor of the electrophilic, nucleophilic or electron-rich moiety of the synthetic linker, and Cyc represents a cyclic aliphatic moiety, aromatic moiety, aliphatic heterocyclic moiety, or aromatic heterocyclic moiety, each of said moieties optionally substituted with one or more groups, which do not interfere with binding to a carrier comprising a biotargeting group, a lipophilic moiety or a biosensor; or a pharmaceutically acceptable salt thereof, provided that the chelating agent is not 6,6′,6″,6′″-((ethane-1,2-diylbis(azanetriyl))tetrakis(methylene))tetrapicolinic acid, 6,6′-((ethane-1,2-diylbis((phosphonomethyl)azanediyl))bis(methylene))dipicolinic acid, 6,6′-((ethane-1,2-diylbis((carboxymethyl)azanediyl))bis(methylene))dipicolinic acid or 6,6′-((ethane-1,2-diylbis((pyridin-2-ylmethyl)azanediyl))bis(methylene))dipicolinic acid, and provided that the bifunctional chelating agent comprises at least one covalently attached moiety that allows for covalent attachment to the carrier comprising a biotargeting group, a lipophilic moiety or a biosensor.