Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1990-11-29
1993-08-03
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549280, A61K 3135, C07D31192
Patent
active
052329429
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to Q-2819 substance and a process for production thereof as well as bacterial strains capable of producing the same.
Q-2819 substance removes active oxygen seeds in the living body and exhibits an action of preventing or reducing the formation of lipid peroxides and is thus useful as a drug for the treatment of various diseases supposed to be induced by these active oxygen seeds. (Background)
Oxygen is necessary and indispensable for maintaining life such as energy production, metabolism, etc. in the living body. Oxygen becomes a so-called active oxygen seed such as a hydrogen anion radical, hydrogen peroxide, a hydroxy radical, etc. in energy-producing reactions, enzyme reactions or reactions with ultraviolet rays or radiations. The active oxygen seed is useful for the living body in oxygen-added enzyme, a sterilizing action of leucocytes, etc. on one hand but on the other hand, accelerates conversion into peroxides of unsaturated fatty acids constructing phospholipids of biomembrane such as oleic acid, linoleic acid, linolenic acid, arachidoic acid, etc. which are abundantly present in the living body. The lipid peroxides induce alkoxy radicals or hydroxy radical, attack biomembrane and cause impairment of membrane or inactivation of various useful enzymes (Metabolism, 15 (10), special 1978 edition featuring active oxygen).
However, enzymes such as superoxide dismutase (SOD), catalase, glutathione peroxidase, etc. participate in metabolic inactivation of the active oxygen seeds described above, and a variety of vitamins having an antioxidizing activity including .alpha.-tocopherol (vitamin E) and the like, in the living body. By these actions, the living body is normally maintained. However, it is often recognized that, by some reason, defects are caused in adequate protection mechanisms by these substances, active oxygenseeds beyond the ability of these protection mechanisms generate, or formation and accumulation of lipid peroxides occur. Where defects or the like are caused in such protection mechanisms, peroxidation proceeds like a chain reaction to induce various serious disturbances in the living body. Representative examples of these disturbances are various diseases caused by platelet coagulation, inflammation, hepatic disturbances, arteriosclerosis, hemolysis, senility or senile diseases, retinal diseases, cardiac and pulmonary disturbances induced by certain drugs, ischemic vascular diseases, ischemic cardiac diseases, organ disturbances in ischemia-recycling, etc. Experimental Medicine, 4 (12), special 1986 edition featuring in vivo free radical and disease.
In general, drugs having an antioxidizing action have been developed for purposes of preventing and treating the diseases described above.
For example, in Japanese patent application laid-open No. 63-152374, hydroxybutenolide derivatives having an action of eliminating active oxygen seeds and organic radicalseeds are disclosed and it is described there that the derivatives have an effect of treating, preventing and improving various disturbances such as ischemic cardiac function disturbances, ischemic cerebral function disturbances, ischemic renal disturbances, etc.
The compound of the present invention has an action of inhibiting formation of lipid peroxides and an action of scavenging superoxide anion radicals and is useful as a prophylactic and therapeutic drug for the aforesaid various diseases.
Specific examples of diseases to which the compound is applied include an agent for improving organs of the circulatory system such as an anti-arrhythmic agent, an anti-myocardiac infarction agent, an agent for preventing from growing senile or senile dementia, treatment or improvement after subarachnoid hemorrhage, etc.; an agent for improving renal function, an agent for treating stress-induced digestive ulcer, an anti-arteriosclerotic agent, an antiinflammatory agent, an agent for preventing platelet coagulation, an agent for treating autoimmune diseases, an anti-rheumatoid agent, an anti
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patent: 4547579 (1985-10-01), Mockli
patent: 4939274 (1990-07-01), Terao et al.
patent: 4963581 (1990-10-01), Kanamaru et al.
Imai, II et al "Substance Q-2819 and its Preparation from Chrysosporium" CA 113:57452e,
Leeper, F. J. et al "Biomimetic Syntheses of Polyketide Aromatics from Reaction of an Orsellinate Anion with Pyrones and Pyrylium Salt" J. Chem. Soc. Perkin Trans (1984) pp. 1053-1059.
Imai Harumitsu
Liang Shu F.
Nagai Koji
Saito Takeshi
Yazawa Hidenori
Ivy C. Warren
Owens A. A.
Yamanouchi Pharmaceutical Co. Ltd.
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