Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai
Reexamination Certificate
1999-08-27
2001-09-04
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ketone doai
C426S531000, C426S590000, C426S625000, C426S653000
Reexamination Certificate
active
06284801
ABSTRACT:
TECHNICAL FIELD OF THE INVENTION
The present invention relates to pharmaceuticals, foods and beverages useful for therapy and prevention of inflammatory diseases such as chronic articular rheumatism.
PRIOR ART
Inflammation is believed to be a result where living body defensively acts against the invasion from outside and produces intrinsic active substance to adapt the state of the body thereto. There are many cases, however, that the reaction induced thereby is harmful and induces a diseased state. In addition, inflammation in autoimmune diseases is resulted from the fact that immunocytes regard themselves as foreign matters and act in an interceptive manner even to normal cells.
It has been reported that, in helper T (Th) cells, there are Th1 cells which produce interleukin-2 and interferon &ggr; (IFN-&ggr;) which are cytokines promoting the activation of cellular immunity such as macrophage (Mø) and also Th2 cells which produce interleukin-4, interleukin-5 and interleukin-10 activating the humoral immunity participated in antibody production.
It has been also shown that Th1 cells and Th2 cells are controlled each other by cytokines produced by each of them. Thus, IFN-&ggr; produced by Th1 cells controls the activation of Th2 cells and induces the activation of Th1 cells. On the other hand, interleukin-10 produced by Th2 cells controls the activation of Th1 cells and interleukin-4 induces the activation of Th2 cells.
Autoimmune diseases are roughly classified into organ-specific and systemic ones. It is believed that, in systemic autoimmune disease and allergic disease, the symptom is caused by Th2-dominant immune response while, in organ-specific autoimmune disease and inflammatory disease, the symptom is caused by Th1-dominant immune response.
Chronic articular rheumatism which is one of autoimmune diseases is believed to be inflammation specific in articular site and is suggested probably to be an organ-specific disease or, in other words, Th1-mediated autoimmune. Actually, in inflammation sites of patients suffering from rheumatism, invasion of Mø and neutrophils which are believed to be induced and activated by cytokines derived from Th1 and significant increase in tumor necrosis factor-&agr; produced by Mø are noted. In other organ-specific autoimmune diseases and inflammatory diseases, the same histologic patterns are observed as well and it is believed that inflammation is exacerbated by those inflammatory cells and inflammatory cytokines which are induced by Th1.
From those facts, it is believed that, in the therapy of inflammatory diseases and organ-specific autoimmune diseases such as chronic articular rheumatism, suppression of tumor necrosis factor produced from Mø and induction of interleukin-10 which is a Th1-inhibiting cytokine are important [Igaku no Ayumi, published by Ishiyaku Shuppan KK, volume 182, pages 523-528 and 661-665 (1997)].
As a drug therapy for chronic articular rheumatism, an internal therapy by steroids, non-steroidal anti-inflammatory agents and remission-inducing agents such as gold and D-penicillamine have been conducted.
PROBLEMS TO BE SOLVED BY THE INVENTION
An object of the present invention is to develop a compound which is useful for the therapy of inflammatory diseases such as chronic articular rheumatism and to offer pharmaceuticals, foods and beverages containing said compound.
MEANS TO SOLVE THE PROBLEM
In order to achieve the above-mentioned object, the present inventors have conducted an intensive investigation and found that 4,5-dihydroxy-2-cyclopenten-1-one which is represented by the formula [I] (hereinafter, just referred to as “the cyclopentenone”) is useful for therapy or prevention of inflammatory diseases such as chronic articular rheumatism and immune diseases whereupon the present invention has been accomplished.
Outline of the present invention is that the first feature of the present invention relates to an antirheumatic agent which is characterized in containing at least one compound selected from a group consisting of 4,5-dihydroxy-2-cyclopenten-1-one represented by the following formula [I] and an optically active substance and a salt thereof as an effective component.
The second feature of the present invention relates to food or beverage for the improvement or prevention of chronic articular rheumatism which is characterized in containing at least one compound selected from a group consisting of 4,5-dihydroxy-2-cyclopenten-1-one represented by the formula [I] and an optically active substance and a salt thereof as an effective component.
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Enoki Tatsuji
Hagiya Michio
Kato Ikunoshin
Koyama Nobuto
Nishiyama Eiji
Kennedy Covington Lobdell & Hickman LLP
Krass Frederick
Takara Shuzo Co. Ltd.
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