Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-01-23
1998-05-12
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514383, 514384, 5462724, 5482638, 5482648, 5482652, 5482656, C07D24914, C07D48704, A61K 3141, A61K 3153
Patent
active
057505454
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/01215, filed Jul. 22, 1994.
1. Technical Field
The present invention relates to novel pharmaceutical use of a series of triazole derivatives and to novel triazole derivatives. More particularly, the present invention relates to an agent for the prophylaxis and treatment of immune-related diseases, which has eosinophilia-inhibitory action, lymphocytes activation-inhibitory action and the like, and to novel triazole derivatives.
2. Background Art
A typical condition of immune-related diseases is immune sthenia such as allergic diseases, and for the prevention and treatment thereof, there have been widely used bronchodilators and antiallergic agents.
An allergic disease is associated with, besides the reactions mainly of mastocytes and basocytes, increase and activation of eosinophil and activation of lymphocytes, by which, it has been clarified, inflammation is induced which causes chronic conditions of the disease. Accordingly, suppression of the disease upon development of an eosinophilia inhibitor and immunosuppressant has been considered.
In a typical allergic reaction, chemical transmitters such as histamin, leukotriene and PAF (platelet activating factor) and various enzymes are released from mastocytes and basocytes by the degranulation due to the invasion of an extraneous factor (allergen). At the same time, the lymphocytes, upon recognition of the allergen, produce various lymphokines which cause wandering, activation and growth of inflammatory cells (mainly eosinophil). These induce an inflammation which gives damages to the tissues, thus causing allergic diseases. The patients with such allergic diseases have been rapidly increasing in number, attracting much social attention, and various methods have been applied for the prophylaxis and treatment of the diseases. However, they are hardly sufficient in terms of effects and side-effects. Meanwhile, the action mechanism of the allergic reaction has been intensively studied, and the reports in recent years have clarified the deep involvement of the activation of, in the main, eosinophil and lymphocytes, and various factors released therefrom, in the onset of the disease. For example, it has been gradually clarified that type III and type IV allergies cause, besides type I allergic reaction, symptoms of bronchial asthma, and that inflammation of respiratory tract is present as a basic symptom. In fact, humectation and activation of eosinophil and lymphocytes have been observed on the air duct mucosa in bronchial asthma, thus suggesting the deep involvement of eosinophil and lymphocytes in the mechanism that makes the disease chronic.
Eosinocytes generally occupy 1-3% of the leukocytes in peripheral blood. An allergic disease such as allergic rhinitis and bronchial asthma, or vermination causes numerous emergence of eosinophil in the topical lesion and blood. Eosinophilia is a hematological pathic phenomenon found when allergic diseases and verminous diseases are contracted, wherein eosinophil occupies 6% or more of peripheral blood leukocytes. Eosinophilia is known to occur in various diseases, besides the above-mentioned allergic diseases and vermination, such as dermal diseases (e.g. herpes zoster, hives, psoriasis and eczema), haematopoietic diseases (e.g. myelocytic leukemia and pernicious anemia), various epidemic (e.g. cholera and malaria) and various osteopathic diseases (e.g. sarcoma, rachitis and myelitis). In allergic diseases such as asthma, moreover, the activation of lymphocytes has been found to play an important role prior to eosinophilia. That is, lymphokines produced by lymphocytes act on various inflammatory cells and cause wandering, activation and growth of inflammatory cells. In addition, lymphocytes exert important actions in various immune diseases as well, besides eosinophil.
Accordingly, a substance having inhibitory actions on eosinophilia and lymphocyte activation is expected to be effective in the treatment of accumulation and activation of eosinophil and lymphocytes caused by allergen,
REFERENCES:
patent: 5135928 (1992-08-01), Reiter et al.
Akahoshi Fumihiko
Fukaya Chikara
Kajii Masahiko
Kuwahara Shigeki
Naito Youichiro
Raymond Richard L.
The Green Cross Corporation
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