Uses of indolo-(2,3b)-quinoxalines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

active

06248742

ABSTRACT:

The present invention relates to new uses of indolo-[2,3b]-quinoxalines of the general formula I
wherein R
1
represents hydrogen or one or several, preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, preferably Br, lower alkyl/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group; and in one of the positions 7-10 R
1
can be a hydroxyl group;
X is a group —(CH
2
)
n
—R
2
wherein R
2
represents a nitrogen containing basic residue such as NH
2
, NHR
4
or NR
5
R
6
wherein R
4
, R
5
and R
6
independently are lower alkyl or cycloalkyl and n is an integer of from 1 to 4 and R
3
represents hydrogen, lower alkyl/-cycloalkyl group having not more than 4 carbon atoms, and the physiologically acceptable addition products of the compounds with acids and halogen adducts, preferably adducts with iodine, iodine monochloride or iodine monobromide,
as DNA protecting agent both in the initial phase and in the promoting phase of carcinogenesis and which agent also reduces or eliminates the effect of promoters and which agent has effects which protect for oxidative stress and effects of gamma-irradiation. Thus, the compounds used according to the present invention activates the defence of the body against carcinogenesis, oxidative stress and gamma-irradiation.
It is known that free radicals (oxidative stress) of different types are associated with a range of diseases such as ischemic or reperfusion injury, thrombosis and embolism, atherosclerosis, allergic/inflammatory conditions such as bronchial asthma and rheumatoid arthritis, diseases caused by ionizing radiation or ultra violet light, conditions related to neurodegenerative diseases for instance Parkinson's disease and Alzheimer's disease, ageing, apoptosis, necrosis and cirrhosis, cataract, physical stress, diabetes, autoimmune diseases, intoxications, colitis, hematocrosis, neoplasms and toxicity of antineoplastic or immuno suppressive agents diseases, premature aging or consequences of viral or bacterial infections and endogeneous or exogeneous chemicals present in air, food, general environmental contamination or lifestyle related exposure. An explanation for these conditions and diseases can be that the endogeneous protecting capacity are not sufficiently active to protect the tissue against radical damage. Lipid peroxidation or DNA-oxidation caused by excess generation of radicals can constitute significant damaging pathways in the above conditions and diseases. The compounds used according to the present invention probably enter into the cell where it activates parts of the genome.
Oxidative stress can be chemically, physically or biologically induced. Chemically induced oxidative stress is caused by a compound which gives rise to a tissue damage. Physically induced stress is caused by e.g. 1) radiation, such as radioactive or ionizing radiation or UV radiation; 2) by physical blockage of blood flow; biologically induced oxidative stress is the defence by the body itself, with over-reaction of oxidases in phagocytes, extra and intra cellular, one example is HIV patients. Other examples are asthma, rheumatoid arthritis, diabetes etc, cf. above.
Different conditions such as inflammations, infections, gamma-radiation, UV radiation and deficiency of vitamins/antioxidants give rise to oxidative stress which leads to the different conditions and diseases stated above. Use of the compounds according to the present invention in preparations to be administrated via different carriers will thus protect the body against oxidative stress and prevent the outburst of different diseases caused by such oxidative stress.


REFERENCES:
patent: 4990510 (1991-02-01), Bergman et al.
patent: 5866575 (1999-02-01), Bergman

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