| 摘要 |
The invention relates to octadentate ligands of a general formula R1-D-X-D-X-D-X-D-E-R2, wherein D is C(O)N(OH) or N(OH)C(O), pyrimidinone or pyridinone, each X independently of any other X is a saturated or partially unsaturated, substituted or unsubstituted linker comprising 8-11 atoms selected from any of N, C, O; R1 is alkyl, cycloalkyl, arene, or heteroarene, E is a saturated or partially unsaturated, substituted or unsubstituted chain comprising 1-50 atoms and R2 is a moiety capable of selectively binding to a biomolecule, or a nanoparticle. The invention further relates to complexes of the ligand, particularly radionuclides and their use in radioimmunotherapy and imaging. |
| 主权项 |
1. A ligand characterized by a general formula I:
R1-D-X-D-X-D-X-D-E-R2 (I),wherein
D is C(O)N(OH) or N(OH)C(O), or each X independently of any other X is a linker defined by the structure —(CH2)k—Ya—(CH2)m—Yb—(CH2)n—Yc—(CH2)p—
wherein each Y independently of any other Y can be —O—, —NH—, —CO—NH—, —HN—CO—, —COO— or —OCO—,k, m, n, and p can have values from 0 to 11, and a, b and c can be 0 or 1, and wherein each pair of D moieties is separated by 8, 9, 10 or 11 covalent bonds in the linker moiety X between them; R1 is a C1-C5 alkyl, in particular a CH3 or CH2CH3, or a C3-C6 cycloalkyl, an arene, and/or a heteroarene, wherein the arene or heteroarene consists of between five and fifteen carbon or hetero atoms, E is a linear linker and, R2 is a) an OH, SH, COOH, SCN, an activated ester, or an ene-one-system or b) a polypeptide, particularly an antibody, that specifically binds to a target site on cells and/or tissues with an association constant of lower than (<) 10−6 mol/l, <10−7 mol/l, <10−8 mol/l or <10−9 mol/l. |
