Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-01-26
1997-07-29
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514255, A61K 31445, A61K 31495
Patent
active
056522495
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This is a 371 of PCT/JP94/01235 filed Jul. 27, 1994. This invention relates to an antidepressant composition.
BACKGROUND TECHNOLOGY
With the increasing complexity of the society, more and more people are succumbing to depression or presenting with depressive-like symptoms. The therapeutic regimen in use today is centered around tricyclic antidepressants (e.g. imipramine hydrochloride, desipramine hydrochloride, etc.). However, these drugs exert various side effects on the cardiovascular system, neuropsychological system, blood, liver, etc. and cannot be considered to be therapeutically satisfactory drugs. Accordingly there has been a standing demand for a new therapeutic agent.
Among the antidepressant drugs under development these days are 1) selective serotonin reuptake inhibitors, 2) specific monoamine reuptake inhibitors, and 3) 5-HT.sub.1A receptor partial agonists.
Meanwhile, aniracetam which is a recently launched nootropic drug is expected to have ameliorative effects on emotional disturbances (anxiety, impatience, depressed mood) after brain infarct.
The cholinergic neurons in the central neurons system are deeply involved in learning and memory and reportedly many nootroic drugs have activity to stimulate neuronal system. On the other hand, it is known that anticholinergic drugs have inhibitory actions on both learning and memory.
Though neither the etiology of depression nor the detailed mechanisms of action of antidepressants have been elucidated as yet, many workers negate the idea that stimulation of the cholinergic nervous system elicits antidepressive effect. Rather, drugs having anticholinergic activity are known to produce antidepressant effects in animal experiments (F. Borsini and A. Meli: Psychopharmacology 94, 147-160, 1988).
The pyroglutamide derivatives to be utilized in accordance with the present invention have been investigated extensively by the present inventors as substances capable of remarkably alleviating learning and memory disabilities(Japanese Kokoku Tokkyo Koho Hei 04-55405; Japanese Kokai Tokkyo Koho Sho 62-252762).
DISCLOSURE OF THE INVENTION
It is an object of the present invention to provide a novel pharmaceutical composition differing in type from the known antidepressants and having a decreased potential for side effects.
The invention is thus directed to an antidepressant composition which comprises, as an active ingredient, a pyroglutamide derivative of the general formula [I] ##STR2## wherein Y is CH.sub.2 or N--R (in which R is an alkoxycarbonyl group, a substituted or unsubstituted aralkyl group or a morpholinocarbonylalkyl group), or a pharmaceutically acceptable salt thereof.
It has now been found that such a known compound having alleviating effects on learning disabilities and disorders of memory has antidepressant activity which is quite irrelevant to said alleviating effects on learning disabilities and disorders of memory.
At present the mechanism by which the compound of the present invention acts as an antidepressant is unknown. Presumably, however, it is considered not to act on the serotonin or noradrenaline system.
In the following, the invention is described in more detail.
Referring to general formula [I], the alkoxy group is preferably a straight or branched lower alkoxy group containing 1 to 4 carbon atoms, such as methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy or tert-butoxy. The aralkyl group preferably contains 7 to 11 carbon atoms and includes, among others, benzyl, phenethyl, phenylpropyl, phenylbutyl and phenylpentyl. The alkyl moiety of the aralkyl group may be branched. The alkyl as a substituent or substituents on the aryl moiety may be straight or branched and preferably contain 1 to 4 carbon atoms, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl being preferred examples. As the alkyl moiety of the morpholinocarbonylalkyl group, there may be mentioned those examples that are given above.
Among the compounds of general formula [I], that compound in which Y
REFERENCES:
patent: 5102882 (1992-04-01), Kimura et al.
Kimura Kiyoshi
Ukai Yojiro
Henley III Raymond
Nippon Shinyaku Co., Inc.
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