Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-07-09
1994-08-02
Waddell, Frederick E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31505
Patent
active
053345932
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to anxiolytic drugs containing a 1-amino-5-halogenouracil as an active ingredient.
BACKGROUND ART
An anxiolytic drug (minor tranquilizer) is a therapeutic agent which is effective in treating anxiety and which can eliminate anxiety or psychentonia in a dose that will not induce excessive sedation. A typical therapeutic agent which is presently used as an anxiolytic drug is a benzodiazepine-type anxiolytic.
Heretofore, (1) bromacil (see Japanese Patent Laid-Open Publication No. 42624/1982), and (2) N.sup.3 -substituted (e.g., benzyl-substituted) uridine derivatives (see Japanese Patent Laid-Open Publication No. 207218/1987) have been known as uracil derivatives having anxiolytic activity or being expected to have the same.
We previously found that 1-amino-5-halogenouracil has sedative effects on central nervous system, and filed therefore an application for a patent (PCT/JP89/00708). As a 1-amino-5-halogenouracil, 1-amino-5-fluorouracil is so far known. However, it has not yet been reported that the compound has anxiolytic activity (see Sci. Pharm., 52, 46 (1984); and Japanese Patent Laid-Open Publication No. 93281/1987).
Benzodiazepine-type anxiolytic drugs which are now widely used as anxiolytic drugs, typically diazepam, give rise to various side effects (e.g-, muscle relaxation, sedation, and elicitation of amnesia). The use of the anxiolytic drugs of this type therefore brings about clinical problems. Since the above side effects are common to compounds having a benzodiazepine skeleton, there exists a demand for finding out a compound which has a skeleton other than the benzodiazepine and which can be used as an anxiolytic drug.
Further, among the above-described uracil derivatives having anxiolytic activity, the bromacil referenced as (1) exhibits low anxiolytic activity when it is orally administered, and the minimum effective dose thereof for single administration is as high as 100 mg/kg. Therefore, the expected effects cannot be fully obtained unless a large amount of the bromacil is administered. With respect to the N.sup.3 -substituted uridine derivatives referenced as (2), although the aforementioned patent publication discloses their hypnotic effects, their anxiolytic activity and particular data regarding the same are not disclosed therein.
An object of the present invention is to provide an anxiolytic drug which comprises as an active ingredient a compound which has a uracil skeleton and low side effects such as those mentioned above.
DISCLOSURE OF THE INVENTION
We have conducted extensive research in order to find out a compound which has anxiolytic activity. As a result, we have found that 1-amino-5-halogenouracil has excellent anxiolytic activity.
The present invention therefore provides an anxiolytic drug (hereinafter often referred to simply as "the drug of the present invention") which comprises as an active ingredient a 1-amino-5-halogenouracil represented by formula [I]: ##STR2## wherein X represents a halogen atom, or a pharmaceutically acceptable salt thereof.
The present invention also provides a method of treating anxiety in mammal, which comprises administering an effective dose of a compound represented by the above formula [I] or a pharmaceutically acceptable salt thereof to a mammal in a state of anxiety.
Furthermore, the present invention provides the use of a compound represented by the above formula [I] or a pharmaceutically acceptable salt thereof for the manufacture of an anxiolytic drug.
As is apparent from the results of Test Example 1 which will be described later, the compound having the above formula [I] or its pharmaceutically acceptable salt (hereinafter often referred to as "the compound of the present invention "), which is an active ingredient of the drug of the present invention, shows potent anti-conflict activity comparable to that of diazepam when it is orally administered in a dose of 50 mg/kg or less. Moreover, when the compound of the present invention is administered, the decrease in the number of leve
REFERENCES:
Japanese Abstract: JP-A-57-042624 (Mar. 10, 1982) "Antianxiety Agent with Antidepressant Activity".
Japanese Abstract: JP-A-207218 (Sept. 11, 1987) "Central Nervous System Depressant".
JP 62-93281 (A), Kyowo Hakko Kogyo Co., Ltd. Japan, Apr. 28, 1987, (abstract).
Imaizumi Masahiro
Sakata Shinji
Moezie M.
Waddell Frederick E.
Yamasa Shoyu Kabushiki Kaisha
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