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

• US 20050118105A1
• Filed: 09/30/2004
• Published: 06/02/2005
• Est. Priority Date: 11/21/1989
• Status: Active Grant

• Current Assignee: Bayer Schering Pharma AG (Bayer AG)
• Original Assignee: Bayer Schering Pharma AG (Bayer AG)
• Inventors: Schmitt-Willich, Heribert, Platzek, Johannes, Bauer, Hans, Weinmann, Hanns-Joachim, Gries, Heinz, Schuhmann-Giampieri, Gabriele, Vogler, Hubert
• Granted Patent: US 7,208,139 B2
• Time in Patent Office: Days
• US Class Current: 424/9.322
• 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

1-20. -20. (canceled)

21. 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.

22. A method of claim 21, wherein the complex is administered in a dose of 0.0001-5 mmol/kg weight of the patient.

23. A method of claim 21, 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.

24. A method of claim 21, wherein at least one complex-forming ligand is a macrocyclic ligand.

25. A method of claim 24, wherein the at least one macrocyclic complex-forming ligand is a tetraazacyclododecane macrocyclic ring ligand.

26. The method of claim 21, wherein the cascade polymer complex is of the formula I

27. The method of claim 26, 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:

28. A method of claim 21, wherein the cascade polymer complex contains at least one complexed gadolinium ion.

29. A method of claim 21, wherein all of the complexed paramagnetic ions are gadolinium ions.