Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
2000-02-10
2000-10-17
Ramsuer, Robert W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544 586, 544128, 544363, 546157, 546158, A61K 315377, A61D 1700, C07D40102
Patent
active
06133264&
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to carbostyril derivatives and agents for inhibiting skin erythema and/or skin pigmentation containing, as the effective ingredient, said carbostyril derivative.
BACKGROUND ART
JP-A-4-234386 discloses carbostyril derivatives represented by the general formula (A), ##STR2## (wherein R.sup.A is a hydrogen atom or a lower alkyl group; R.sup.B is a hydrogen atom, a lower alkyl group or a lower alkoxy group; and R.sup.C is a lower alkyl group respectively) which can be used as intermediates for preparing other carbostyril derivatives used for treating cardiovascular diseases.
Additionally, WO 93/22317 discloses carbostyril derivatives represented by the general formula (B), ##STR3## (wherein R.sup.D and R.sup.E are each the same or different from each other and are hydrogen atoms, lower alkyl groups or lower alkoxy groups; and the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond) which can be used as intermediates for preparing quinoline derivatives used for remedy for cardiac diseases.
However, these prior art references disclose only that the above-mentioned carbostyril derivatives can be used as intermediates for preparing blocking agents of adrenaline .beta.-receptor or antiarrhythmic drugs. Thus, above-mentioned prior art references do not disclose at all that these carbostyril derivatives per se possess whatever pharmacological activities.
Furthermore, WO 97/44037 and WO 97/44321 disclose quinoline compounds as antagonists of gonadotropin-releasing hormone, and WO 97/03066 discloses substituted benzolactam compounds as substance P antagonist. In fact that these quinoline compounds and substituted benzolactam compounds involve carbostyril skeleton in their molecular structures. However, these compounds are quite different from the carbostyril derivatives of the present invention in both chemical stractures and usages.
DISCLOSURE OF THE INVENTION
The present inventors have found the fact that at least one of the compound selected from the group consisting of carbostyril derivatives represented by the general formula (1) and salts thereof including the above-mentioned known compounds possesses activities for inhibiting skin erythema (sunburn) and/or skin pigmentation. Such pharmacological activities could not been anticipated from the usefulnesses being disclosed in these prior art references. Thus the present invention has been successfully established on the basis of said finding.
The present invention relates to agents for inhibiting skin erythema (sunburn) and/or skin pigmentation containing, as the effective ingredient, at least one selected from the group consisting of carbostyril derivatives and salts thereof represented by the general formula (1), ##STR4## (wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a lower alkenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkenyloxy group, a lower alkenyl group or a tetrahydropyranyloxy group; R.sup.3 and R.sup.4 are the same or different from each other, and each is a lower alkyl group which may have hydroxyl groups as substituents; further R.sup.3 and R.sup.4 may form, together with the adjacent nitrogen atom, further with or without additional nitrogen atom, sulfur atom or oxygen atom, a 5- or 6-membered saturated heterocyclic group which may have substituents selected from the group consisting of a lower alkyl group and a lower alkanoy group; the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond).
Nowadays, vitamins such as vitamin E, ascorbic acid and the like; natural substances such as arbutin, kojic acid and the like are used as the effective ingredients in cosmetics for preventing sunburn and suntan being caused by exposure to UV rays and the sun light, as well as for the purpose to effect bleaching the skin pigmentation such as spots and ephelides. However, these vitamins and natural substances are difficult to handle becaued they a
REFERENCES:
D. Blondet et al., "Convenient Synthesis of 6-Methyl, 8-Methyl and 6,8-Dimethyl Derivatives of 5-Hydroxy-1,2,3,4-Tetrahydro-2-Quinolinone", Chemical Abstracts, vol. 119, No. 9, Abstract No. 95292j, (1993).
Kuwahara Keiichi
Nishi Takao
Oshiro Yasuo
Watanabe Kozo
Otsuka Pharmaceutical Co. Ltd.
Ramsuer Robert W.
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