Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-25
1996-08-06
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514267, A61K 3152, A61K 31505
Patent
active
055434150
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/00931 filed Jul. 7, 1993.
TECHNICAL FIELD
The present invention relates to an antidepressant containing a xanthine derivative or a pharmaceutically acceptable salt thereof as an active ingredient.
BACKGROUND ART
##STR4##
It is known that adenosine antagonistic action is found in compounds represented by Formula (A) in which R.sup.1a and R.sup.2a represent propyl, R.sup.3a represents hydrogen, and R.sup.4a represents substituted or unsubstituted phenyl, aromatic heterocyclic group, cycloalkyl, styryl, or phenylethyl [J. Med. Chem., 34, 1431 (1991)]. Further, Japanese Published Unexamined Patent Application No. 26516/72, as cerebral stimulants, compounds represented by Formula (B) in which R.sup.1b and R.sup.2b independently represent methyl or ethyl, R.sup.3b represents methyl, Y.sup.1b and Y.sup.2b represent hydrogen, and Z.sup.b represents phenyl or 3,4,5-trimethoxyphenyl WO92/06976 discloses, as compounds having an adenosine A.sub.2 receptor antagonistic activity and therapeutic effects on asthma and osteoporosis, compounds represented by Formula (B) in which R.sup.1b and R.sup.2b independently represent hydrogen, propyl, butyl, or allyl, R.sup.3b represents hydrogen or lower alkyl, Y.sup.1b and Y.sup.2b independently represent hydrogen or methyl, and Z.sup.b represents phenyl, pyridyl, imidazolyl, furyl, or thienyl unsubstituted or substituted by 1 to 3 substituents such as lower alkyl, hydroxy, lower alkoxy, halogen, amino, and nitro. Furthermore, other compounds represented by Formula (B) are known. One is 8-styryl caffeine which is a compound of Formula (B) in which R.sup.1b, R.sup.2b, and R.sup.3b represent methyl, Y.sup.1b and Y2b represent hydrogen, and Z.sup.b represents phenyl [Chem. Ber., 119, 1525 (1986)]. Another is a compound of Formula (B) in which R.sup.1b, R.sup.2b, and R.sup.3b represent methyl, Y.sup.1b and Y.sup.2b represent hydrogen, and Z.sup.b represents pyridyl, quinolyl, or methoxy-substituted or unsubstituted benzothiazolyl [Chem. Abst., 60, 1741h (1964)]. However, there is no description with regard to the pharmacologic action of any of these compounds.
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' consecutive administration [J. Neural Transmission, 52, 189 (1981)].
DISCLOSURE OF THE INVENTION
The present invention relates to an antidepressant containing as an active ingredient a xanthine derivative or a pharmaceutically acceptable salt thereof, the xanthine derivative being represented by Formula (I): ##STR5## in which R.sup.1, R.sup.2, and R.sup.3 represent independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR6## (in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR7## (in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 3), or a substituted or unsubstituted heterocyclic group);
In the definitions of Compound (I), the lower alkyl means a straight-chain or branched alkyl group having 1 to 6 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, neopentyl, and hexyl. The lower alkenyl means a straight-chain or branched alkenyl group having 2 to 6 carbon atoms such as vinyl, allyl, methacryl, crotyl, 3-butenyl, 2-pentenyl, 4 -pentenyl, 2-hexenyl, 5-hexenyl. The lower alkynyl means a straight-chain or branched alkynyl group having 2 to 6 carbon atoms such as ethynyl, propargyl, 2-butynyl, 3-butynyl, 2-pentynyl, 4-pentynyl, 2-hexynyl, 5-hexynyl, 4-methyl-2-pentyn
REFERENCES:
patent: 3641010 (1972-02-01), Schweiss et al.
patent: 4472387 (1984-09-01), Laruelle et al.
Sarges et al, J. Med. Chem., vol. 33, 1990, pp. 2240-2254.
Sarges et al., Chemical Abstracts, vol. 113, No. 7, abstract No. 59110r, 1990.
Erickson et al., J. Med. Chem., vol. 34, No. 4 (1991) 1431-1435.
Kaupp et al., Chem. Ber., vol. 119 (1986) 1525-39.
Chem. Abstracts, 60 (1964) 1741h.
Maj. et al., J. Neural Transmission 52 (1981) 189-197.
Ichikawa Shunji
Ishii Akio
Kitamura Shigeto
Koike Nobuaki
Nakamura Joji
Cintins Marianne M.
Jarvis William R. A.
Kyowa Hakko Kogyo Co. Ltd.
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