Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-08-15
1999-11-09
Stockton, Laura L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514340, 514342, 514365, 514369, 514374, 514375, 514376, 5462697, 5462714, 5462717, 5463701, 548152, 548171, 548178, 548179, 548181, 548202, 548203, 548204, 548221, 548217, 548229, 548235, A61K 31425, A61K 3144, C07D27726, C07D27764
Patent
active
059815590
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a medicament, particularly to a novel azole derivative or a salt thereof which has both leukotriene (LTs) antagonizing activity and thromboxane (TX) A.sub.2 antagonizing activity and is useful as an agent for the prevention or treatment of diseases in which these mediators are concerned, as well as to a pharmaceutical composition comprising said derivative and to an intermediate useful in producing said derivative.
BACKGROUND ART
Various cases are known in relation to asthma, which include dyspeptic asthma, allergic asthma, atopic asthma, bronchial asthma, bacterial asthma, cardiac asthma and the like. Particularly, there are a great number of patients of bronchial asthma among these cases, so that studies have been made on agents or methods for its prevention and treatment. The action mechanism of anti-bronchial asthmatic agents is considered from two viewpoints, i.e. bronchiectasis and anti-inflammation, and many therapeutic and preventive agents has been developed. As the aforementioned bronchodilators, .beta..sub.2 -stimulators, methylxanthine and cholinolytic agents may be exemplified, and steroids and mediator inhibitors may be exemplified as the anti-inflammatory agents. However, since the current antiasthmatic agents have disadvantages in that the bronchodilators have strong side effects and the anti-inflammatory agents have low efficacy in therapeutic and preventive effects in comparison with other agents, great concern has been directed toward the development of excellent asthma-preventing and treating agents which can supplement both of these disadvantages.
In recent years, among these anti-inflammatory agents, mediator inhibitors such as PAF antagonists, thromboxane A.sub.2 (TXA.sub.2) antagonists/synthesis inhibitors and leukotriene (LTs) antagonists have been applied to asthma and their efficacy is being recognized. However, it has been reported that the therapeutic effect of these agents on asthma (medium or more improvement of the efficacy of agents) is approximately around 50% when used alone (Igakuno Ayumi 168 (4), 295 (1994) and Igakuno Ayumi 164 (4), 225 (1993)), suggesting that the efficacy is not sufficient because of the difference in the type of mediator which takes the main role in each patient of asthma.
Recently, some compounds capable of inhibiting a plurality of mediators have been reported (for example, an unexamined published Japanese patent application (Kokai) No. 4-154766). However, their effects are not sufficient from the viewpoint of oral absorbability, so that great concern has been directed toward the creation of clinically useful agents which can effect well-balanced inhibition of a plurality of mediators and also are excellent in oral absorbability.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide a compound which can achieve well-balanced inhibition of two or more mediators (hereinafter, to be referred to as "multiple mediator inhibitor") and a pharmaceutical agent comprising said compound. The inventors of the present invention have conducted extensive studies based on an assumption that a multiple mediator inhibitor could be used as an agent effective for a broad range of allergic diseases such as asthma and the like, and, particularly, excellent effects could be expected as an antiasthmatic agent in the case of an inhibitor having both TXA.sub.2 antagonism and LTs antagonism. As the results, it was found that a derivative represented by the following general formula (I) or a salt thereof, which is characterized in that it has a monocyclic or condensed ring azole ring and which is different from the structures of the known compounds, has the aforementioned two functions in a well-balanced manner and is also possessed of excellent oral absorbability and that it can be an antiasthmatic agent which is broadly useful as a multiple mediator inhibitor, thereby resulting in the accomplishment of the present invention.
Accordingly, the present invention relates to an azole derivative repr
REFERENCES:
patent: 5273986 (1993-12-01), Holland et al.
Akane Hiroaki
Arakida Yasuhito
Isomura Yasuo
Nagaoka Noriko
Yokota Masaki
Stockton Laura L.
Yamanouchi Pharmaceutical Co. Ltd.
LandOfFree
Azole derivative with leukotriene (LTs) antagonizing activity an does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Azole derivative with leukotriene (LTs) antagonizing activity an, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Azole derivative with leukotriene (LTs) antagonizing activity an will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1456508