Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-11-20
2000-10-24
Weddington, Kevin E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514306, 514859, A61K 3150, A61K 3144
Patent
active
061368067
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a treating agent for rosacea.
BACKGROUND ART
Rosacea is, while rare among colored races, common among races with a light-colored skin, especially white races, and many cases occur among them. It is divided according to the symptoms into the first degree (telangiectatic rosacea on the forehead, cheeks, dorsum nasi), the second degree (acne rosacea, coexistence of follicular papules and pustules), and the third degree (rhinophyma, dark red tumor and dilated pore on apex nasi). It starts with facial flush (redness) and eventually involves serious impairment of appearance, developing papules, pustules, rhinophyma and tumor on apex nasi, It is also accompanied by seborrhea or enhancement of feeling of heat on the face due to emotional stress or change of environmental temperature. Thus, these symptoms give a patient mental and physical suffering.
For the time being, the real cause of rosacea is unknown (Hifuka Chirya Handbook, pp. 380-381, Nanzando (1987) and Gerd Plewing, Albert M. Kligman, ACNE and ROSACEA, 2nd, Completely Revised and Enlarged Edition, pp. 431-454, Springer-Verlag (1993)). Rosacea is apt to be confused with acne, what is called pimple, classificationally. Rosacea, which can coexist with acne, essentially differs from acne. It is characterized by facial flush due to vascularization and proceeds with acne rosacea and tumor on apex nasi. A digestive disease, hypertension, Demodex folliculorum, emotional stress, hereditary predisposition, etc. have been pointed out as a conceivable cause of rosacea, which has not been ascertained yet.
Therefore, there is no drug established as a remedy for rosacea, and the only method available now is symptomatic treatment, such as administration of minocycline or tetracycline antibiotics for the treatment of delayed skin diseases, use of metronidazole (anthelmintic), removal of mental stress, dietetic treatment, and supplemental concomitant use of vitamin B.sub.2 or B.sub.6.
Accordingly, it has been keenly demanded to study and develop more useful treating agents for rosacea.
An object of the present invention is to provide a useful rosacea treating agent.
DISCLOSURE OF THE INVENTION
The inventor of the present invention has conducted extensive study to develop a rosacea treating agent in the light of the above circumstances, and found as a result that at least one compound selected from the group consisting of benzoheterocyclic derivatives represented by the following formula (1): ##STR2## wherein R represents a lower alkyl group; and X represents a halogen atom, and salts thereof is suitable as an active ingredient of a rosacea treating agent, The present invention has been completed based on this finding.
That is, the present invention relates to a rosacea treating agent comprising at least one selected from the group consisting of the above benzoheterocyclic derivatives represented by formula (1) and salts thereof as an active ingredient; use of at least one selected from the above compounds for preparing a rosacea treating agent; and a method for treating rosacea comprising using at least one selected from the above compounds.
The benzoheterocyclic derivatives represented by formula (1) or salts thereof are known from, e.g., Japanese Patent Publication No. 41127/89, which teaches details of a method for preparing these compounds and usefulness of the compounds as antimicrobial agents.
However, it is unpredictable even for one skilled in the art whether or not these benzoheterocyclic derivatives and their salts are effective for treating rosacea that has been considered baffling and difficult to cure.
The rosacea treating agent according to the present invention is effective even for treating intractable rosacea on which conventional antibiotics such as minocycline do not work, healing rosacea active papules, active pustules, erythema, and active efflorescence, and suppressing telangiectasia. It has low toxicity, causing little side effect, and is of long duration.
BEST EMBODIMENTS FOR CARRYING OUT TH
REFERENCES:
patent: 4399134 (1983-08-01), Ishikawa et al.
patent: 4552879 (1985-11-01), Ishikawa et al.
patent: 5179096 (1993-01-01), Gentilini et al.
Nishijima et al., Activity of Eight Fluoroquinolones Against Both Methicillin-Susceptible and -Resistant Staphylococcus, arues Isolated from Skin Infections, Journal of Dermatology vol. 22, 153-155, 1995.
Acne and Rosacea, 2.sup.nd, Completely Revised and Enlarged Edition, G. Plewig, Springer-Verlag, pp. 431, 433-455.
Otsuka Pharmaceutical Co. Ltd.
Weddington Kevin E.
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