Pharmaceutical composition for the treatment of malignant neopla

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514416, A01N 4354, A61K 31515

Patent

active

061437530

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention refers to a pharmaceutical composition for the treatment of malignant neoplasms and immunosuppressive deficiencies, by re-establishing the biochemical balance within the cells, mainly those cells undergoing a disordered reproduction, and to a method for producing said pharmaceutical composition.


BACKGROUND OF THE INVENTION

Nowadays, the existence of several types of cancer control by means of conventional treatments has conducted, after studies based on cellular biochemistry, to the provision of a pharmaceutical composition formed by an essential aminoacid of the benzoic genesis and by a genetic derivative of a pyrimidinic nitrogenized base. The experiment has clinically proved its efficiency on the neoplastic cells, avoiding their disordered reproduction.


DISCLOSURE OF THE INVENTION

Thus, it is a first objective of the present invention to use the efficiency of the active ingredients of an essential aminoacid of the benzoic genesis with a pyrimidinic nitrogenized base in a biologically acceptable pharmaceutical formula in the following compositions: DL-kinurenine, [2-amine-3-(2-aminebenzene)propionic acid] and tymine, [2,1 dihydroxy-5-methyl-pyrimidine;5-methyluracil].
A further objective of the present invention is to provide a method for producing a pharmaceutical composition, which is formulated for the dissolution of 1.5-6.0 grams, preferably 3-4 grams of DL-kinurenine and 1.2-7.0 grams, preferably 2.5-3.5 grams of tymine in 50 ml of distilled water, preferably at about 50.degree. C., resulting in a stabilized solution with a neutral pH of about 5.6 to 9.0, preferably from 6.8 to 7.3 by adding an adequate amount of potassium or sodium hydroxide.
Taking into account that DL-kinurenine is the final product of anthranil transformation in the biochemical reactions, in which is included tryptophan, which precedes kinurenine, it has been verified that it is possible to substitute kinurenine by tryptophan in the desired pharmaceutical composition, without modifying the effects. Tryptophan [(R)-2-amine-3-(indole-propionic acid) associated with tymine has become viable for the pharmaceutical composition in the originally suggested proportions.
The substances mentioned in the described pharmaceutical composition have their active ingredients diluted in distilled water or in the form of encapsulated powder and are intended for oral administration. They result in a new drug for treating the biochemical disorders found in all neoplastic cells and with immunosuppressive deficiencies.
The observation of the biochemical reactions that occur within the cells, in terms of DNA and RNA, between the aminoacids and the functions of the nitrogenized bases in the presence of the enzymatic systems, has allowed the correction of several forms of lesions in the chromossomal structures caused by hydrolysis or external mutagenic agents, deaminating agents and alkylating agents (Ames, 1979,204:587-593; Cairns, 1975,233:64-78; and Goodman and Gilman, 1987). It has been developed a pharmaceutical formulation, obtaining a product formed by the association of an aminoacid of the benzoic genesis with a pyrimidinic nitrogenized base which, inside the cell, in terms of DNA and RNA in the presence of carboxylase, produces a double effect, i.e., neutralizes the formylic radicals which appear during the irregular mitosis of the chromosomal structures and eliminates the energy produced with oxygen release for the formation of the neoplastic cells.
This process, called catacholase, stops the liberation of energy by oxygen and completes the neutralization of the formylic radicals, re-establishing the bridge with the deoxyribonucleoside of the DNA chromosomes (Lawitscka, Dados Informativos de Pesquisa (Research Informative Data), 1960). The neoplastic cells during the cellular mitosis have a defect in the ribonucleosidase of the purines. Failure in this purine formation makes the cell become cancerous.
Knowing that the nucleic acids are informative molecules which control the basic processes o

REFERENCES:
Kruglyakova et al., "Investigation of the effect of UV light of varying wavelength on DNA with different protein content in the presence of endogenous sensitizers", Stud. Biophys. 85(1), 55-56, 1981.
Tarui et al., "Thermodynamic effect of complementary hydrogen bond base paring on aromatic stacking interaction in the guanine-X-Trp complex (X=adenosin, guanine, ctosine, thymine)", Chem. Pharm. Bull., 44(11), 1998-2002, 1996.
Koshima et al, "Photochemical behavior of crystals and mixed crystals composed of nucleic acid bases", Photomed. Photobiol. 17, 109-110, 1995.

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