Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-05-20
1993-03-16
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549315, A61K 43455, C07D30762
Patent
active
051944456
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an ascorbic acid derivative useful as a preparation for preventing and curing an organ dysfunction, particularly as a preparation having a preventive and curing effect on organ dysfunctions caused by active oxygen species and/or active organic radical species which are induced by ischemia, etc.
TECHNICAL BACKGROUND
Recently increasing organ dysfunctions in the heart, brain, kidney, liver, etc., have been found to be caused as follows. An ischemic state (bloodstream malcirculation) causes a failure in supply of an energy source and a metabolic change. Various tissue-disordering factors, which are caused by reperfusion with a bloodstream, destroy or injure cells and tissues of which the resistive strength has been lowered due to the above metabolic change.
In recent years, a study of the above tissue-disordering factors has advanced and showed that active oxygen species or active organic radical species have a large share as a factor for the tissue disorder [I. Fridovich, Archives of Biochemistry and Biophysics, Vol. 247, p. 1 (1968); B. Halliwell, Biochemical Journal, Vol. 219, p. 1 (1984); J. M. McCord, Advance in Free Radical Biology and Medicine, Vo. 2, p. 325 (1986)].
Development of these active oxygen species or active organic radical species during the ischemia-reperfusion and a decrease in endogenous resistive factors are considered to have an essential effect on organ dysfunctions.
SOD (superoxide dismutase) and compounds such as .alpha.-tocopherol, ascorbic acid, etc., are considered to eliminate these active oxygen species or active organic radical species, and studies of a therapy using these enzyme and compounds are now under way.
However, SOD shows a short half-life in vivo. Being an enzyme, SOD poses an antigenicity problem having regard to an acquisition method and source. And, .alpha.-tocopherol has a defect in that its activity in vivo is low. Ascorbic acid has a defect in that it is easily decomposed and inferior in stability.
JP-A-61-263969 discloses that 2-O-substituted ascorbic ascorbic acid is able to eliminate the above active species and useful as a preparation for preventing and curing the dysfunction of a circulatory system which is one of organ dysfunctions. However, this 2-O-substituted ascorbic acid also has a defect in that it is easily decomposed and poor in stability.
Therefore, the first object of the present invention is to provide a novel ascorbic acid derivative which has the activity to prevent and cure organic dysfunctions caused by active oxygen species and/or active organic radical species induced by ischemia, etc.
The second object of the present invention is to provide a process for the preparation of the above novel ascorbic acid derivative.
Further, the third object of the present invention is to provide a preparation for preventing and curing organic dysfunctions, which contains, as an active component, the above novel ascorbic acid derivative and/or other known ascorbic acid derivative.
DISCLOSURE OF THE INVENTION
That is, the ascorbic acid derivative of the present invention is a novel ascorbic acid derivative of the general formula (Ia), ##STR2## wherein R.sub.1 is an alkylcarbonyl lower alkyl group of which the terminal alkyl group has 7 inclusive to 15 inclusive carbon atoms.
The present process for the preparation of an ascorbic acid derivative is a process for the preparation of an ascorbic acid derivative of the general formula (Ia), ##STR3## wherein R.sub.1 is an alkylcarbonyl lower alkyl group of which the terminal alkyl group has 7 inclusive to 15 inclusive carbon atoms, which comprises treating a compound of the general formula (II), ##STR4## wherein R.sub.1 is as defined in the formula (Ia), with an acid thereby to convert the acetal group of said compound to a vic-glycol group.
Further, the present preparation for preventing and curing organ dysfunctions contains, as an active component, an ascorbic acid derivative of the general formula (IA), ##STR5## wherein R.sub.2 is a group selected from t
REFERENCES:
patent: 4780549 (1988-10-01), Terao et al.
patent: 5034543 (1991-07-01), Satoh et al.
patent: 5061812 (1991-10-01), Satoh et al.
Kakegawa Hisao
Matsumoto Hitoshi
Niiro Yasunori
Satoh Toshio
Covington Raymond
Ivy C. Warren
Nippon Hypox Laboratories Incorporated
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