Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-25
1998-08-04
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142332, 5142342, 5142345, A61K 31535
Patent
active
057894078
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an antidepressant.
BACKGROUND ART
It is known that compounds represented by the following formula (II): ##STR2## in which R.sup.1a represents hydrogen, substituted or unsubstituted lower alkyl, or lower alkanoyl, R.sup.2a represents hydrogen, lower alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group, R.sup.3a represents a substituted or unsubstituted 5-membered heterocyclic group, X.sup.a represents O, S, S(O), S(O).sub.2, or NR.sup.4a (in which R.sup.4a represents hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.2a and NR.sup.4a are combined to form a substituted or unsubstituted 4 to 6-membered saturated heterocyclic group), and A.sup.a represents N or CR.sup.5a (in which R.sup.5a represents hydrogen, or substituted or unsubstituted lower alkyl), and compounds represented by the following formula (III): ##STR3## in which R.sup.1b represents hydrogen, substituted or unsubstituted lower alkyl, or lower alkanoyl, R.sup.2b represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted phenyl, or a substituted or unsubstituted 5- or 6-membered heterocyclic group, and A.sup.b represents N or CR.sup.5b (in which R.sup.5b represents hydrogen, or substituted or unsubstituted lower alkyl), have an selective adenosine A.sub.2 antagonistic activity (Japanese Published Unexamined Patent Application Nos. 97855/93 and 155887/93).
It is clinically well known that the conventional antidepressant exhibits little effect in a single administration, and the effect is observed after at least about two weeks' consecutive administration.
With the conventional antidepressant, the enhancement of clonidine-induced aggressive behavior in mice is observed after at least ten days'
DISCLOSURE OF THE INVENTION
The present invention relates to an antidepressant containing as an active ingredient a triazine derivative, or a pharmaceutically acceptable salt thereof, the derivative being represented by the following Formula (I): ##STR4## in which, R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower alkanoyl; R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a substituted or unsubstituted heterocyclic group; X represents a single bond, O, S, S(O), S(O).sub.2, or NR.sup.4 (in which R.sup.4 represents hydrogen, or substituted or unsubstituted lower alkyl; or R.sup.2 and NR.sup.4 are combined to form a substituted or unsubstituted 4 to 6-membered saturated heterocyclic group); and A represents N or CR.sup.5 (in which R.sup.5 represents hydrogen, or substituted or unsubstituted lower alkyl).
The present invention also relates to a method of treating depression comprising administration of an effective amount of a triazine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof.
The present invention further relates to the use of a triazine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition which is useful for treating depression.
The present invention further relates to the use of a triazine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof for treating depression.
Furthermore, the present invention relates to a composition for treating depression comprising, in a pharmaceutically acceptable dosage form, an effective amount of a triazine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
The compounds represented by Formula (I
REFERENCES:
patent: 4780464 (1988-10-01), Trivedi
patent: 5356894 (1994-10-01), Rodney et al.
Pharmacol. Biochem. Behav., 16 (1982) 449.
Drug Dev. Res., 29 (1983) 38-55.
Chemical Abstracts AN 1990:191746, Nikodijevic et al., 1990.
Griebel et al, Psychopharmacology, 103(4) 541-4, Nov. 9, 1990.
Medline Abstract AN 86066118, Marenyo et al. Sep. 1995.
Ichikawa Shunji
Kitamura Shigeto
Koike Nobuaki
Nakamura Joji
Shimada Jun'ichi
Kyowa Hakko Kogyo Co. Ltd.
MacMillan Keith D.
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