Patent ID: 8518715

Claim:
A bifunctional polyazamacrocyclic chelating agent of the formula (VIb) or (VIe): wherein: each Q is independently (CHR 5 ) p CO 2 R or (CHR 5 ) p PO 3 R 6 R 7 ; Q 1 is hydrogen, (CHR 5 ) w CO 2 R or (CHR 5 ) w PO 3 R 6 R 7 ; each R is independently hydrogen, benzyl or C 1 -C 4 alkyl; R 6 and R 7 are independently H, C 1 -C 6 alkyl or (C 1 -C 2 alkyl) phenyl; each R 5 is independently hydrogen; C 1 -C 4 alkyl or (C 1 -C 2 alkyl) phenyl; A is CH, N, C—Br, C—Cl, C—SO 3 H, C—OR 8 , C—OR 9 , N + —R 10 X − , or Z and Z 1 independently are CH, N, C—SO 3 H, N + —R 10 X − , C—CH 2 —OR 8 or C—C(O)—R 11 ; R 8 is H, C 1 -C 5 alkyl, benzyl, or benzyl substituted with at least one R 12 ; R 9 is C 1 -C 16 alkylamino; R 10 is C 1 -C 16 alkyl, benzyl, or benzyl substituted with at least one R 12 ; R 11 is —O—(C 1 -C 3 alkyl), OH or NHR—; R 12 is H, NO 2 , NH 2 , isothiocyanato, semicarbazido, thiosemicarbazido, maleimido, bromoacetamido or carboxyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon-carbon bond; n is 0 or 1; m is an integer from 0 to 10 inclusive; p is 1 or 2; r is 0 or 1; w is 0 or 1; L is a linker/spacer group covalently bonded to, and replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula: wherein: s is 1; t is an integer from 0 to 20 inclusive; R 1 is an electrophilic or nucleophilic moiety which allows for covalent attachment to a biological carrier, or synthetic linker which can be attached to a biological carrier, or precursor thereof; 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 biological carrier; or a pharmaceutically acceptable salt thereof.