Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1997-05-30
1998-09-01
Burn, Brian M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
564507, 564487, 564445, 564453, 564462, 564504, 514668, 514669, 549551, A01K 3113
Patent
active
058012028
DESCRIPTION:
BRIEF SUMMARY
This application is a 35 USC 371 of PCT/JP95/02284, filed Nov. 8, 1995.
TECHNICAL FIELD
The present invention relates to novel amine derivatives, acid addition salts thereof, and novel glycidyl ether derivatives which are intermediates in the process of preparing the amine derivatives and acid addition salts. The compounds encompassed by the present invention dramatically improve keratinization, prevent or improve pigmentation of skin, and solve skin problems caused by dyskeratosis.
DESCRIPTION OF THE RELATED ART
The outermost layer of the skin called the epidermis prevents water loss and loss of a variety of components from living bodies and controls the homeostasis of living bodies. Moreover, the epidermis functions as a barrier and protects the body from outside physical and chemical stimulation (heat, humidity, etc.) and also from various bacteria. Thus, its physiological functions are very important for the activities of living bodies. Keratinocytes, which constitute the epidermis, form healthy epidermis having the above-mentioned physiological functions when cell proliferation and keratinization (differentiation) are well balanced. However, if this balance is lost due to the presence of intra- or extra- corporeal factors that affect living bodies including excessive stimulation (for example, UV-rays) from the environment and degradation of physiological functions (for example, aging of skin accompanying senility, diseases, etc.), healthy epidermination cannot occur. Particularly, the face and hands which are usually exposed to stimulation by UV rays, etc. are generally in a condition where proliferation is excessive and keratinization is insufficient. This induces acanthosis and parakeratosis, and as a result, ordinary skin complaints such as dry skin, fatty skin, and dandruff are caused. Furthermore, formation of keratinous plugs is considered to cause various troubles in the skin including generation of acne, and delay in melanin metabolism to cause pigmentation of skin.
Approaches to restore such abnormal skin conditions and to keep the skin healthy include removal or suppression of causal substances or conditions and addition or application of a certain components. Previously, a primary care for preventing and solving skin problems employed synthetic or natural moisture-retainable components which prevent the skin from drying and enhance the moisture-retention ability of the skin, thereby compensating the decrease in moisture-retaining ability of the skin. Alternatively, circulation promoters were applied to the skin to accelerate blood circulation in the skin. Moreover, spots, freckles, and pigmentation caused by sunburns and suntans tend to easily occur or increase in number as the skin ages, and in addition, they do not disappear easily, so they are a source of complaints to middle aged to elderly persons. The onset mechanism of these pigmentations of the skin has not yet been elucidated. However, it is considered that sunlight, particularly UV rays, and melanocyte stimulating hormones act to stimulate the melanin-synthesizing mechanism in epidermal melanocytes. Conventionally, in order to blanch acquired pigmentation of melanin described above to a normal skin color, vitamin C (ascorbic acid) derivatives and isoflavon derivatives (Japanese Patent Application Laid-open (kokai) No. 58-225004) have been used as well as p-hydroxycinnamic acid derivatives (Japanese Patent Application Laid-open (kokai) No. 59-196813).
However, the above-mentioned conventional approaches have various problems with respect to the ability of preventing skin problems, efficacy in improvement, sustainability of the effect, and stability/safety of the composition. That is, since the conventional methods are intended to supply water or to supplement part of moisture-retaining components to the epidermis, particularly the surface of the horny layer, they produce only temporary effects, and accordingly, long-lasting and radical alleviation of skin problems were not expected. Moreover, as regards the pigmentation, subs
Fujimori Taketoshi
Higuchi Kazuhiko
Imokawa Genji
Kondo Naoki
Kusuoku Hiroshi
Burn Brian M.
Kao Coproration
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