Cascade polymer bound complexing compounds, their complexes and conjugates, processes for their production, and pharmaceutical agents containing them

• US 7,208,139 B2
• Filed: 09/30/2004
• Issued: 04/24/2007
• Est. Priority Date: 11/21/1989
• Status: Expired due to Fees

• Current Assignee: Bayer Schering Pharma AG (Bayer AG)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Schmitt-Willich, Heribert, Platzek, Johannes, Bauer, Hans, Weinmann, Hanns-Joachim, Gries, Heinz, Schuhmann-Giampieri, Gabriele, Vogler, Hubert
• Primary Examiner(s): Jones; Dameron L.
• Application Number:
  US10/953,582
• Publication Number:
  US 20050118105A1
• Time in Patent Office: 936 Days
• Field of Search: 424/1.11, 424/1.37, 424/1.65, 424/9.1, 424/9.3, 424/9.36, 424/9.361, 424/9.362, 424/9.363, 424/9.364
• US Class Current: 424/9.36
• CPC Class Codes: A61K 49/0002 General or multifunctional contrast agents, e.g. chelated agents
• CPC Class Codes: A61K 49/04 X-ray contrast preparations
• CPC Class Codes: A61K 49/06 Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
• CPC Class Codes: A61K 49/085 conjugated systems
• CPC Class Codes: A61K 49/124 dendrimers, dendrons, hyperbranched compounds
• CPC Class Codes: A61K 51/04 Organic compounds
• CPC Class Codes: A61K 51/065 conjugates with carriers being macromolecules
• CPC Class Codes: C08G 83/003 Dendrimers
• CPC Class Codes: C08G 85/00 General processes for preparing compounds provided for in this subclass
• CPC Class Codes: Y10T 436/24 Nuclear magnetic resonance, electron spin resonance or other spin effects or mass spectrometry

Abstract

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.

Claims

1. A method for imaging of inflammation and/or tumors in the brain of a patient by nuclear spin tomography, comprising conducting nuclear spin tomography on 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 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.

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 21–

29, 39, 42, 44 or 57–

83.

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.

7. The method of claim 6, 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:

8. A method of claim 1, wherein the cascade polymer complex contains at least one complexed gadolinium ion.

9. A method of claim 1, wherein all of the complexed paramagnetic ions are gadolinium ions.

10. A method of claim 1, wherein the cascade polymer complex is a complex of a nitrogen-containing cascade polymer.