Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-03-17
2000-06-06
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544 14, A61K 31549, C07D51314
Patent
active
060719052
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to medicine, and more specifically to pharmacology, veterinary, cosmetology, and in particular to synthetic biological active compound of heterocycle series, which possess antimicrobial, antiviral, antichlamydia and immune stimulating activities: derivatives of 5-oxo-5H-[1]-benzopyrano-[5,6-b]-4-oxo-4H-[1,2]-pyrimido-1,4,5,6-tetrahydr o-1,3-thiazine. The derivatives mentioned above have high antimicrobial activity to various mycobacteria, substantial antiviral activity relative to Herpes simplex virus, high antichlamydial activity, and also activity as inducers of interferon. The substances compounds are intended, mainly, for the use in medical practice for treating tuberculosis, mycobacteriosis, viral diseases, infections caused by chlamydia, and also diseases which are accompanied by immunodeficiency, in particular malignant neoplasm. In addition, the above mentioned compound can be used for the same purposes in veterinary and cosmetology.
As known, there are many unsolved problems in modern chemotherapy of infectious diseases. Among bacterial infections one of the most serious problems is caused by tuberculosis, whose treatment is especially complicated due to high resistivity of tuberculosis mycobacteria to the action of chemotherapeutical agents [1]. Moreover, existing compounds possess substantial disadvantage-wide spread of mycobacteria which are resistant to them.
Historically first antituberculosis compounds were derivatives of phenols, benzioc acids (2), mercaptobenzimidizols (3), p-aminosalicyclic acid (4). The most active antituberculosis agents were derivatives of isonicotine acid discovered at the end of 40.sup.s of our century, such as isoniazide and its analogs, which are used at present, ethionamide, ethambutole, aminoglycosides, rifampicin, fluoroquinols (1). During therapy of tuberculosis and mycobateriosis usually 2-3 compounds are simultaneously prescribed, which slow appearance of resistant forms of mycobacteria, but do not solve the problems of getting used and resistance completely. Therefore search for new active antituberculosis agents, including those which act on forms of mycobacteria which are resistant to isoniazide, is still actual. Viral diseases pose for modern medicine problems which are not less serious. As a rule, viral infections, such as those caused by viruses of herpes group, are very difficult to be treated, which is connected with insufficient efficiency of existing compounds as well as fast changes of viruses, whose mutations cause appearance of resistant forms (5-7). Synthetic compounds for treatment of diseases caused by viruses of herpes group include acylovir, gancyclovir, retrovir (5) and others whose efficiency is not always sufficient.
Many problems exist during treatment of diseases caused by chlamydia, including widely spread urogenital infections (8). Chlamydia of which are intracellular parasites, are little accessible for the majority of existing compounds and, in addition to this, widespread resistance to the latter caused an appearance of a great number of chronic forms of diseases. To treat chlamydia infections, usually there are used compounds of tetracycline series, macrolids and fluoroquinolones, for example ciprophoxacin (8).
Frequently diseases of viral and bacterial nature occur on the background of reduction of activity of organism immune system, and therefore the problem of development of efficient compounds for treatment of immune deficient states of various origin is also one of the most actual problems. In addition, stimulation of activity of immune system contributes to fight of organism against tumoral processes during which multiple resistance to existing treatment compounds is observed (9).
It is necessary to note that at present intense search of biologically active compounds among derivatives of pyrimidine series is conducted. In particular, in the pyrimidine series a lot of derivatives are known which are used as medicinal compounds (10). Monocyclic derivatives of pyrimidin
REFERENCES:
patent: 4297355 (1981-10-01), Schering
Ashkinazi Rimma Iliinichna
Krasnov Konstantin Andreevich
Natural Drug Sciences LLC
Raymond Richard L.
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