Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1994-12-30
1996-12-31
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
558402, A61K 31275, C07C25534
Patent
active
055895069
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP44/00370.
TECHNICAL FIELD
The present invention relates to novel compounds of a stilbene derivative, a stilbene homologue derivative and an .alpha.,.beta.-diarylacrylonitrile derivative inhibiting 12-lipoxygenase selectively, and medicines containing the above compounds as effective components; more specifically, the present invention relates to a stilbene derivative, a stilbene homologue derivative and an .alpha.,.beta.-diarylacrylonitrile derivative having an effect of inhibiting the activities of 12-lipoxygenase on the 12-lipoxygenase route selectively, and medicines containing said compounds as effective components and inhibiting 12-lipoxgenase selectively useful as medicine for the prevention and remedies of various circulatory diseases such as arteriosclerosis and vasospasm and the prevention of the metastasis of some cancers (e.g., Lewis lung cancer).
In addition, the present invention relates to novel compounds of a stilbene derivative and a stilbene homologue derivative capable of forming a substance whose modified part is cleaved in vivo and which inhibits 12-lipoxygenase selectively, and medicines containing the above compounds as effective components; more specifically, the present invention relates to a stilbene derivative and a stilbene homologue derivative (hereinafter may be described as precursors) capable of being converted to compounds whose modified parts are cleaved in vivo and which inhibit 12-lipoxgenase on the 12-lipoxgenase route selectively, and medicines containing said precursors as effective components and inhibiting 12-lipoxgenase selectively useful as medicine for the prevention and remedies of various circulatory diseases such as arteriosclerosis and vasospasm and the prevention of the metastasis of some cancers.
The indication of percentage in the present specification means values by weight unless otherwise noted.
TECHNICAL BACKGROUND
It is known that a metabolic route called the 5-lipoxygenase route exists in arachidonate cascade and that arachidonate is converted to 5-hydroperoxyeicosatetraenoic acid (hereinafter may be described as 5-HPETE) by the function of 5-lipoxygenase ("Prostaglandin and Morbid States", edited by Seiitsu Murota, Tokyo Kagaku Dojin, 1984).
It is known that various leukotrienes are biosynthesized with this compound as an intermediate ("Prostaglandin and Morbid States", edited by Seiitsu Murota, Tokyo Kagaku Dojin, 1984), and it is also known that, for example, leukotriene B4 of these leukotrienes has a strong leukocyte migration effect and is a mediator of inflammations and that leukotriene C4 and D4 are mediators of asthma ("Prostaglandin and Morbid States", edited by Seiitsu Murota, Tokyo Kagaku Dojin, 1984).
Hence, searches for medicines having an inhibitory effect to 5-lipoxgenase have been performed broadly, from the viewpoint that if there is a medicine capable of inhibiting 5-lipoxgenase, an incipient enzyme of the biosynthesis system of these leukotrienes, effectively, the prevention and remedy effects of various diseases caused by the excess occurrence of leukotrienes (e.g., allergic diseases, bronchial asthma, dropsical swellings, various inflammatory diseases) may be anticipated.
On the other hand, a metabolic route called the 12-lipoxygenase route exists in arachidonate cascade. 12-lipoxygenase is an enzyme existing mainly in platelets and forms 12-hydroperoxyeicosatetraenoic acid (hereinafter may be described as 12-HPETE) according to a reaction with arachidonate, and the compound becomes 12-hydroxyeicosatetraenoic acid (hereinafter may be described as 12-HETE) according to reduction.
The physiological meaning of metabolic products on the 12-lipoygenase route has not been clear compared with that of the 5-lipoxgenase route; however, various physiological activities of the metabolic products have been made clear recently with 12-HPETE and 12-HETE of the main metabolic products at the center.
These physiological activities can be exemplified as below. Namely, regarding the metabolic product of 12-l
REFERENCES:
patent: 2681359 (1954-06-01), Rorig
patent: 2740806 (1956-04-01), Rorig
patent: 4015017 (1977-03-01), Gazave et al.
patent: 4326055 (1982-04-01), Loeliger
patent: 4996237 (1991-02-01), Pettit et al.
patent: 5091569 (1992-02-01), Matsumoto et al.
patent: 5430062 (1995-07-01), Cushman et al.
Takatoshi et al, "Lipoxygenase inhibitors and their use as anti-allergy and anti-inflammatory agents", CA 122:29906, (1995).
Hamano Hirokazu
Hashimoto Koichi
Mori Shigehiro
Moriuchi Hisako
Yamada Akio
Dees Jos,e G.
Lambkin Deborah
Morinaga Milk Industry Co. Ltd.
LandOfFree
Stilbene derivative and stilbene analog derivative, and use ther does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Stilbene derivative and stilbene analog derivative, and use ther, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Stilbene derivative and stilbene analog derivative, and use ther will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1142503