초록 ▼

Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for dia

Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

대표청구항 ▼

1. A method for radiodiagnosis and/or radiotherapy of a patient, comprising conducting radiodiagnosis and/or radiotherapy of a patient who has been administered a cascade polymer complex having complex-forming ligands complexing at least five ions of an element of atomic numbers 27, 29, 31, 32, 37-3

1. A method for radiodiagnosis and/or radiotherapy of a patient, comprising conducting radiodiagnosis and/or radiotherapy of a patient who has been administered a cascade polymer complex having complex-forming ligands complexing at least five ions of an element of atomic numbers 27, 29, 31, 32, 37-39, 43, 49, 62, 64, 70, 75 or 77, as well as, optionally, cations of inorganic and/or organic bases, amino acids or amino acid amides.2. A method of claim 1, wherein the complex is administered in a dose of 0.0001-5 mmol/kg weight of the patient.3. A method of claim 1, wherein the cascade polymer complex contains more than 15% by weight of the elements of atomic numbers 27, 29, 31, 32, 37-39, 43, 49, 62, 64, 70, 75 or 77.4. A method of claim 1, wherein at least one complex-forming ligand is a macrocyclic ligand.5. A method of claim 4, wherein the at least one macrocyclic complex-forming ligand is a tetraazacyclododecane macrocyclic ring ligand.6. The method of claim 1, wherein the cascade polymer complex is of the formula I whereinA represents a nitrogen-containing cascade nucleus of basis multiplicity b, S represents a reproduction unit, independently for each generation, N represents a nitrogen atom, Z1 and Z2 for the first to penultimate generation, independently each represent, but for the last generation,Z1 represents a hydrogen atom, a C1-C10-alkyl, C2-C10-acyl or C1-C10-alkylsulfonyl radical optionally containing 1 to 3 carboxy groups, from 1 to 3 sulfonic acid groups, from 1 to 5 hydroxy groups and/or 1 to 3 oxygen atoms, or represents the radical of a complex former or complex K and Z2 represents the radical of a complex K, b represents a number 1 to 50, and s represents a number 1 to 3. 7. The method of claim 6, wherein in formula (I), K represents a radical of the formula IA, IB or IC bonded to the terminal nitrogen atoms of the last generation via V: whereinn and m in each case independently are 0, 1, 2, 3 or 4; n and m adding up to no more than 4, k represents the numbers 1, 2, 3, 4 or 5, l represents the numbers 0, 1, 2, 3, 4 or 5, q represents the numbers 0, 1 or 2, U represents CH2X or V, X represents the radicals ?COOH, optionally in the form of an ester or an amide thereof, B, D and E which are identical or different represents the group ?(CH2)a wherein a represents the numbers 2, 3, 4 or 5, R1 represents V or a hydrogen atom, with the proviso that R1 represents V only when U at the same time represents CH2X, and that U represents V only when R1 at the same time represents a hydrogen atom, V representing a straight-chain, branched, saturated or unsaturated C1-C20-alkenylene group optionally containing imino, phenylene, phenyleneoxy, phenyleneimino, amide, hydrazide, ureido, thioureido, carbonyl ester groups(s) and oxygen, sulphur and/or nitrogen atom(s), and optionally substituted by hydroxy, mercapto, imino, epoxy, oxo, thioxo and/or by amino group(s). 8. A method for detecting tumors in a patient, comprising conducting MRI-, x-ray- or radio-diagnosis of a patient who has been administered a cascade polymer complex having complex-fanning ligands complexing at least five ions of an element of atomic numbers 21-29, 31, 32, 37-39, 42,43, 44,49 or 57-83, as well as, optionally, cations of inorganic and/or organic bases, amino acids or amino acid amides.9. The method of claim 8, wherein the method comprises conducting MRI-diagnosis, the cascade polymer complex is complexed with at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83 and the cascade polymer complex is administered in a dose of below 1 mg per kg body weight of the patient.10. A method of claim 8, wherein the cascade polymer complex contains more than 15% by weight of the elements of atomic numbers 21-29,31, 32, 37-39, 42, 43, 44, 49 or 57-83.11. A method of claim 8, wherein the cascade polymer complex contains at least one complexed gadolinium ion.12. A method of claim 8, wherein all of the complexed paramagnetic ions are gadolinium ions.13. A method of claim 8, wherein at least one complex-forming ligand is a macrocyclic ligand.14. A method of claim 13, wherein the at least one macrocyclic complex-forming ligand is a tetraazacyclododecane macrocyclic ring ligand.15. A method for susceptibility imaging comprising imaging a patient by in vivo NMR spectroscopy to whom a susceptibility reagent has been administered, wherein said susceptibility reagent is a cascade polymer complex having complex-forming ligands complexing at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, optionally, cations of inorganic and/or organic bases, amino acids or amino acid amides.16. A method of claim 15, wherein the cascade polymer complex contains more than 15% by weight of the elements of atomic numbers 21-29, 39, 42, 44 and 57-83.17. A method of claim 15, wherein the cascade polymer complex contains at least one complexed gadolinium ion.18. A method of claim 15, wherein all of the complexed paramagnetic ions are gadolinium ions.19. A method of claim 15, wherein at least one complex-forming ligand is a macrocyclic ligand.20. A method of claim 19, wherein the at least one macrocyclic complex-forming ligand is a tetraazacyclododecane macrocyclic ring ligand.21. The method of claim 8, wherein the cascade polymer complex is of the formula I whereinA represents a nitrogen-containing cascade nucleus of basis multiplicity b, S represents a reproduction unit, independently for each generation, N represents a nitrogen atom, Z1 and Z2 for the first to penultimate generation, independently each represent, but for the last generation,Z1 represents a hydrogen atom, a C1-C10-alkyl, C2-C10-acyl or C1-C10-alkylsulfonyl radical optionally containing 1 to 3 carboxy groups, from 1 to 3 sulfonic acid groups, from 1 to 5 hydroxy groups and/or 1 to 3 oxygen atoms, or represents the radical of a complex former or complex K and Z2 represents the of a complex K, b represents a number 1 to 50, and s represents a number 1 to 3. 22. The method of claim 21, wherein in formula (I), K represents a radical of the formula IA, LB or IC bonded to the terminal nitrogen atoms of the last generation via V: whereinn and m in each case independently are 0, 1, 2, 3 or 4; n and m adding up to no more than 4, k represents the numbers 1, 2, 3, 4 or 5, l represents the numbers 0, 1, 2, 3, 4 or 5, q represents the numbers 0, 1 or 2, U represents CH2X or V, X represents the radicals ?COOH, optionally in the form of an ester or an amide thereof, B, D and E which are identical or different represents the group ?(CH2)a wherein a represents the numbers 2, 3, 4 or 5, R1 represents V or a hydrogen atom, with the proviso that R1 represents V only when U at the same time represents CH2X, and that U represents V only when R1 at the same time represents a hydrogen atom, V representing a straight-chain, branched, saturated or unsaturated C1-C20-alkenylene group optionally containing imino, phenylene, phenyleneoxy, phenyleneimino, amide, hydrazide, ureido, thioureido, carbonyl ester groups(s) and oxygen, sulphur and/or nitrogen atom(s), and optionally substituted by hydroxy, mercapto, imino, epoxy, oxo, thioxo and/or by amino group(s). 23. The method of claim 15, wherein the cascade polymer complex is of the formula I whereinA represents a nitrogen-containing cascade nucleus of basis multiplicity b, S represents a reproduction unit, independently for each generation, N represents a nitrogen atom, Z1 and Z2 for the first to penultimate generation, independently each represent, but for the last generation,Z1 represents a hydrogen atom, a C1-C10-alkyl, C2-C10-acyl or C1-C10-alkylsulfonyl radical optionally containing 1 to 3 carboxy groups, from 1 to 3 sulfonic acid groups, from 1 to 5 hydroxy groups and/or 1 to 3 oxygen atoms, or represents the radical of a complex former or complex K and Z2 represents the radical of a complex K, b represents a number 1 to 50, and s represents a number 1 to 3. 24. The method of claim 23, wherein in formula (I), K represents a radical of the formula IA, IB or IC bonded to the terminal nitrogen atoms of the last generation via V: whereinn and m in each case independently are 0, 1, 2, 3 or 4; n and m adding up to no more than 4, k represents the numbers 1, 2, 3, 4 or 5, l represents the numbers 0, 1, 2, 3, 4 or 5, q represents the numbers 0, 1 or 2, U represents CH2X or V, X represents the radicals ?COOH, optionally in the form of an ester or an amide thereof, B, D and E which are identical or different represents the group ?(CH2)a wherein a represents the numbers 2, 3, 4 or 5, R1 represents V or a hydrogen atom, with the proviso that R1 represents V only when U at the same time represents CH2X, and that U represents V only when R1 at the same time represents a hydrogen atom, V representing a straight-chain, branched, saturated or unsaturated C1-C20-alkenylene group optionally containing imino, phenylene, phenyleneoxy, phenyleneimino, amide, hydrazide, ureido, thioureido, carbonyl ester groups(s) and oxygen, sulphur and/or nitrogen atom(s), and optionally substituted by hydroxy, mercapto, imino, epoxy, oxo, thioxo and/or by amino group(s).