Meso-tetraphenylporphyrin complex compounds, process for their p

Details Meso-tetraphenylporphyrin complex compounds, process for their p Meso-tetraphenylporphyrin complex compounds, process for their p

1995-09-26

1997-10-07

Hollinden, Gary E.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

In an organic compound

424 9362, 540145, 534 10, 534 15, 534 16, 514185, A61K 5104, A61B 5055, C07B 4700, C07F 500

Patent

active

056744676

DESCRIPTION:

BRIEF SUMMARY
The invention relates to new meso-tetraphenylporphyrin complex compounds, new pharmaceutical agents containing these compounds, their use in diagnosis and therapy as well as process for the production of these compounds and agents.
The use of complexing agents or complexes or their salts has long been known in medicine. As examples, there can be mentioned: complexing agents are known as stabilizers of pharmaceutical preparations; complexes and their salts are known as additives for the administration of poorly soluble ions (e.g., iron); complexing agents and complexes (preferably calcium or zinc) optionally as salts with inorganic and/or organic bases, are known as antidote for detoxification in the case of inadvertent incorporation of heavy metals or their radioactive isotopes; and complexing agents are known as additives in nuclear medicine with use of radioactive isotopes such as .sup.99m Tc for scintiscanning. In Patents EP 71564, EP 130934 and DE-OS 3401052, complexes and complex salts have been presented as diagnostic agents, mainly as NMR diagnostic agents. These complexes and complex salts are quite well-tolerated and assure a separation of the ions that is complete to the greatest extent possible. Their parameters determining the effectiveness of an NMR contrast medium are not yet optimized, of which there are mentioned:
an advantageous relaxivity, so that the contrast medium in the smallest possible concentration reduces in vivo the relaxation time of the protons in the tissue water and other nuclei, such as P, F and Na, and thus makes possible, for example, the locating of tumors by increasing the signal intensity of the image obtained with the help of the nuclear spin tomograph; as selective as possible a concentration and/or retention of the contrast medium in the target organ; sufficient water solubility; low toxicity; good compatibility; good chemical and biochemical stability.
The complexes and complex salts of the mentioned patents are affected by the drawback that they are dispersed only relatively unspecifically in the extracellular space and therefore do not always make possible an identification of pathologically altered tissue. There is therefore a need particularly for selectively-bonding, tumor-specific compounds.
Relative to their compatibility, they should exhibit as great a safety margin as possible. As a measurement for it, the product from toxicity and relaxivity can be considered.
It has been known for several years now that porphyrin derivatives can accumulate selectively in human and animal tumors (D. Kessel and T. H. Chou, Cancer Res. 43, pp. 1994-1999, 1983, P. Hambright, Bioinorg. Chem. 5, pp. 87-92, 1975; R. Lipson et al., Cancer 20, pp. 2250-2257, 1967; D. Sanderson et al., Cancer 30, pp. 1368-1372, 1972). First attempts to use this family of compounds also as diagnostic agents have also been described (J. Winkelmann et al., Cancer Research 27, pp. 2060-2064, 1967; European Patent Application Publication No. 133603; N. J. Patronas et al., Cancer Treatment Reports 70, pp. 391-395, (1986).
The previously described compounds, however, are far from meeting the above-mentioned criteria in a satisfactory manner; their deficient concentration in the target organs increasingly calls for special attention. An improvement of this property should simultaneously help to reduce the existing problems with the toxicity and compatibility of the previously known compounds.
In Patent Application EP 0336879, substituted meso-tetraphenylporphyrin complex compounds for use in diagnosis and therapy are described. These compounds show a good concentration behavior in various target organs, but the described compounds in use as NMR diagnostic agents exhibit a ratio between the dose necessary for optimum imaging and the lethal dose that is not yet completely satisfactory.
Therefore, for varied purposes, there is further a need for stable, readily soluble but also better compatible and selectively-bonding complex compounds, which are suitable for the diagnosis and/or also treatment, for example,

REFERENCES:
patent: 5262532 (1993-11-01), Tweedle et al.
patent: 5284647 (1994-02-01), Niedballa et al.
Keinan et al., "Catalytic Antibodies, Circular Dichroism and UV-Vis Studies of Antibody-Metalloporphyrin Interactions", Inorg. Chem., 31, 5433-5438, (1992).

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