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Metal complexes having vitamin B12 as a ligand

A technology of metal complexes and B12, which is applied in pharmaceutical formulations, preparations for in vivo tests, organic chemistry, etc., can solve problems such as inability to be cut and affect the biological behavior of vitamin B, and achieve the effect of simple synthesis

Inactive Publication Date: 2007-02-07
UNIV ZURICH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Derivatization at the position of the ribose or corrin backbone has the disadvantage of not being able to be cleaved, thus significantly affecting vitamin B 12 biological behavior

Method used

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  • Metal complexes having vitamin B12 as a ligand
  • Metal complexes having vitamin B12 as a ligand
  • Metal complexes having vitamin B12 as a ligand

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Embodiment Construction

[0060] Materials and methods

[0061] All chemicals were of the highest commercial grade purchased from the companies Merck, Dietikon (CH), Aldrich or Fluka, Buchs (CH) and were used without further purification unless otherwise stated.

[0062] All reactions were performed under nitrogen or argon atmosphere. The reaction was monitored by HPLC.

[0063] HPLC analysis was performed on a Merck-Hitachi L-7000 system equipped with a diode array UV / Vis detector and an EG&G Berthold LB508 radiometric detector. Macherey Nagel Nucleosil C-18ec RP columns (5 μm particle size, 100 Å pore size, 250×3 mm) and Merck C-18e RP Supersphere® columns (100 Å pore size, 250×4 mm) and Waters XTerra RP8 columns (5 μM particle size diameter, 3.0×100mm) for separation. Different HPLC solvent systems and gradients were used: Solvent system 1: 0.1% AcOH and 10% CH in water 3 CN, pH 3 (A) and methanol (B). Solvent system 2: 0.1% triethylammonium acetate and 10% CH in water 3 CN, pH 8. Solvent sys...

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Abstract

The present invention relates to a metal complex of the general formula M(L)n, wherein each L is independently selected and represents a ligand and at least one L is vitamin B12 (cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC-[Co] moiety with [Co] representing vitamin B12 without cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B12. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy.

Description

field of invention [0001] The present invention relates to vitamin B 12 Metal complexes as ligands. The invention also relates to the use of these complexes in radiodiagnosis, radionuclide therapy, chemotherapy or as catalysts. Background technique [0002] Existing cancer drugs, such as cisplatin, are also toxic to normal, healthy cells. Relatively high doses need to be administered to patients, which can lead to serious side effects. Enhanced selectivity by targeting cancer cells is beneficial to patients' therapeutic index and quality of life. [0003] In radionuclide therapy, the metabolic accumulation of radiopharmaceuticals is used to deliver therapeutic radiation doses to tissues. A critical factor for the success of radionuclide therapy is the accumulation of target tissue relative to normal tissue, which is in the range of 5-100 in all known methods. The highly successful iodine metabolism treatment of thyroid disease is a special case relative to this. The ra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F19/00C07D487/22A61K49/00
Inventor 苏珊尼·B·孔兹罗杰·艾伯托赫克托·H·奈特卡斯特罗斯蒂芬·芒德韦勒
Owner UNIV ZURICH
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