Cytokine potentiator and pharmaceutical formulation for cytokine

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

514561, 514667, 514669, 514673, 562567, 564503, 424 851, 424 852, 424 854, A01N 3718, A01N 3712

Patent

active

060081880

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a cytokine potentiator and a medicine for diseases with lowered cytokine activity. In particular, the present invention relates to a cytokine activity enhancer and a medicine for diseases associated with lowered cytokine activity, which can enhance the cellular response to cytokines. The present invention enhances the reactivity of cytokines lowered by aging or the like, and can treat disorders caused by a decrease in cytokine activity.


BACKGROUND OF THE INVENTION

It is known that the restoration of aged skin tissue or chapped skin tissue to its original condition is closely associated with cytokine activity. In addition, it is known that changes in cytokine activities are closely correlated with certain diseases. Various attempts to use cytokines to treat these diseases have been and are being actively pursued.
Cytokines may be administered to patients orally or by parenteral administration, such as by injection or endermic application. However, these methods require continuous administration of a large amount of expensive cytokines to the patient until complete recovery is achieved. These methods are therefore costly and time-consuming.
Alternatively, a substance that promotes the production of cytokines may be administered. Like direct administration of cytokines, the substance may be administered to the patient orally or by parenteral administration such as injection or endermic application. However, like the administration of cytokines, the administration of cytokine production enhancers are costly and time-consuming.
The administration of large amounts of cytokines for extended periods of time is further problematic in that the treatment often disrupts the patient's overall metabolism. In addition, external application of cytokines are ineffective in achieving a local effect, due to decomposition or poor absorbability of the compound. Therefore, a safer method for treating aged or chapped skin is desirable.


OBJECTS AND SUMMARY OF THE INVENTION

For the purposes of this specification, cytokine potentiator is defined as a substance which augments the efficacy of a cytokine, accelerates the activity of a cytokine, acts as a carrier for a cytokine, increases a cytokine's affinity or avidity for its receptor, improves the cellular response to a cytokine in vivo or in vitro, acts in the manner of an adjuvant, directs the localization of a cytokine, or in any manner improves the way in which a cytokine exerts its function on the target.
Accordingly, an object of the present invention is to provide a cytokine activity enhancer or a medicine for treating diseases characterized by lowered cytokine activity which, when administered to an individual, can increase cellular response to endogenous cytokines.
Another object of the present invention is to provide a cytokine activity enhancer or a medicine for treating diseases characterized by lowered cytokine activity which, when administered along with exogenous cytokines, can reduce the amount of cytokines to be administered.
The present invention provides a cytokine activity enhancer comprising an ethanolamine derivative of the following general formula (I) or a salt thereof. ##STR2## wherein R.sub.1 represents H, --CH.sub.3, --CH.sub.2 CH(CH.sub.3)OH or --CH.sub.2 CH.sub.2 OH; R.sub.2 represents H, --CH.sub.3, --CH.sub.2 CH.sub.3 or --COOH; and R.sub.3 represents H, --CH.sub.3, --CH.sub.2 CH.sub.3 or --CH.sub.2 NH.sub.2.
The present invention also provides a medicine to treat diseases characterized by lowered cytokine activities, which comprises the above-mentioned cytokine activity enhancer.


BRIEF DESCRIPTION OF THE DRAWINGS

FIG. 1 shows a vertical diffusion cell device used in Test Example 15.
FIG. 2 shows the results of the skin-through permeability of N-methyl-L-serine as obtained in Test Example 15.


BEST MODES OF CARRYING OUT THE INVENTION

Of the ethanolamine derivatives of formula (I) intended for use in the present invention, the preferred forms are those wherein R.sub.1 is H, R.sub.2 is H, --CH

REFERENCES:
patent: 4423223 (1983-12-01), Huggins et al.
patent: 4469684 (1984-09-01), Hall et al.
patent: 5189166 (1993-02-01), Hull
patent: 5332758 (1994-07-01), Nakata et al.
patent: 5543394 (1996-08-01), Wozney et al.
patent: 5591709 (1997-01-01), Lindenbaum
Zhang et al., Immunology, vol. 79:528-534, Dec., 1993.
Zwierzina et al., Stem Cells, vol. 11:144-153, Nov. 1993.

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