Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-03-05
1998-07-28
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546153, 546157, 546158, A61K 3147, C07D215227
Patent
active
057863679
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INDUSTRIAL UTILIZATION
The present invention relates to novel cyclic amide derivatives and salts thereof.
BACKGROUND ART
The sunlight is indispensable environmental factor to the living body, while at the same time the sunlight is harmful to the living body. The skin and eyes are contacted continuously with oxygen in the air, additionally these organs are unavoidably encountered in the environment where active oxygen species and lipid peroxides are formed easily by physical reactions caused by direct effect of the ultraviolet rays and radiations, and by chemical reactions in the presence of the sebum and other chemical substances. (Cf. Pharma. Medica., 1990, Vol. 8, No. 4, pp. 67-71). Harmful effects caused by the sunlight to the living body are mostly made on the basis of actions of ultraviolet rays. Among the ultraviolet rays, ultraviolet ray-C has the highest energy level and shows strong germicidal activity, and is also known that it accelerates the cancerization. Ultraviolet ray-C is absorbed in the ozonosphere in the stratosphere surrounding the earth, so that very little amount of ultraviolet ray-C only reaches the earth ground. Ultraviolet ray-A causes pigmentation of the skin due to increase of melanin formation in the skin. Ultraviolet ray-B causes sunburn, such as "feel hot" and varicella, and it has been known that the skin cancerization may be caused by long hour-exposure to the ultraviolet ray-B. (Cf. Active oxygen . Free radicals, 1993, Vol. 4, pp. 20-22).
In recent years, it has been well known as the fact that the cancerization tends to upward by increasing of irradiated amount of ultraviolet ray-B due to destruction of the ozonosphere. These disturbances and injuries of the living body caused by ultraviolet rays are presumed on the basis of various active oxygen radicals which are formed by exposure to the ultraviolet rays.
Formation of the active oxygen species caused by exposure to the ultraviolet rays is proposed as two types of mechanisms as follows. That is, one type of the mechanism is that the substrate (e.g., lipid) is oxidized and/or reduced by reacting with excited state of sensitized materials which are excited by action of the ultraviolet rays or lights. Then, oxygen is added to the substrate, which is changed to radical state, to form peroxide (lipid peroxide). Further, oxygen anion radicals are formed by transformation of electrons from the radical to oxygen. Another type of formation mechanism is that the sensitized materials in excited state are first reacted with oxygen, so that energy or electron transfer causes the formation of singlet oxygen or oxygen anion radical. Furthermore, hydrogen peroxide is formed from oxygen anion radical by disproportionation, and hydroxy radicals are also formed by Fenton reaction (Cf. Active Oxygen . Free Radicals, 1993, Vol. 4, pp. 6-19).
Pharmaceutical chemicals which possess activities for scavenging these oxygen radicals can be used as agents for prevention and treatment of various injuries and diseases caused by the ultraviolet rays. In addition to the above, superoxide dismutases (SOD), which act disproportionation against oxygen anion radicals, present in the living bodies (Cf. Journal of Investigative Dermatology, 1984, Vol. 83, pp. 166-168), and there are known some agents for preventing and treating dermatological injuries which are caused by active oxygen species present in the living bodies pp. 179-182!. Glutathione is known that it possesses activity for scavenging alkoxy radicals, so that it is used as treating agent of cataract. Vitamin E possesses skin protection activity (Cf. Fragrance Journal, 1991, No. 8, pp. 28-33). Vitamin C possesses anti-oxidation activity, and is known that it is effective to prevention of pigmentation (Cf. Fragrance Journal and Biophysics, 1992, Vol. 296, No. 2, pp. 575-582; Journal of Dermatology, 1990, Vol. 17, pp. 595-598). However, it should be noted the fact that, because SOD and glutathione are endgenous substances, they have some problems in stabilities thereof and raw mater
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Fujisawa Shigeki
Kuwahara Keiichi
Nishi Takao
Oshiro Yasuo
Takasu Keiko
Gupta Yogendra N.
Otsuka Pharmaceutical Co. Ltd.
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