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

• US 6,576,222 B2
• Filed: 10/11/2001
• Issued: 06/10/2003
• 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 LEVEST
• Application Number:
  US09/973,836
• Publication Number:
  US 20020068037A1
• Time in Patent Office: 607 Days
• Field of Search: 424/1.11, 424/1.65, 424/9.1, 424/78.01, 424/9.3, 424/9.361, 424/9.362, 424/9.363, 424/9.364, 534/7, 534/10-16, 266/168, 514/492, 514/502, 514/501, 514/499, 514/496, 514/495
• 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 purifying a cascade polymer complex having complex-forming 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, which comprises subjecting a composition containing the cascade polymer complex to purification by ultrafiltration through a membrane having a pore size suitable to the size of the cascade polymer complex.

2. The method of claim 1, wherein the membrane has a pore size suitable to provide a cut-off of about 5,000 dalton.

3. The method of claim 1, wherein the membrane has a pore size suitable to provide a cut-off of about 10,000 dalton.

4. The method of claim 1, wherein the cascade polymer complex contains paramagnetic complexed ions and is suitable as a contrast agent for MRI diagnosis.

5. 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 and 57-83.

6. A method of claim 1, wherein at least one complex-forming ligand is a macrocyclic ligand.

7. A method of claim 6, wherein the at least one macrocyclic complex-forming ligand is a tetraazacyclododecane macrocyclic ring ligand.