Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-12-03
1993-12-14
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514422, 514423, 514424, 514425, 514429, 548400, 548517, 548524, 548531, 548538, 548539, 548540, 548542, 548543, 548545, 548550, 548551, C07D20708, C07D20706, C07D20720, C07D20724
Patent
active
052703398
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention is useful in the medicinal field. The present invention relates to a novel phenoxybenzene derivative and a salt thereof, which has cognition enhancing activity and antidepressive activity, and a cognition enhancer comprising the same as an effective ingredient and an antidepressant comprising the same as an effective ingredient.
BACKGROUND ART
With increasing a population of aged generation, dementia is occupying large weight in care of the aged. Although many medicines have been developed in order to improve various types of dementia such as dysmnesia, they are not fully enough in the points of efficacy, persistence and side effect.
For example, the function of cholinergic nervous system in hippocampus, amygdala and cerebral cortex is depressed in brains of patients of Alzheimer's disease (Pope et al., Trans. Am. Neurol. Assoc., 89, 15 (1964), Bowen et al., Brain, 266, 558 (1976) and Davies et al., Lancet, ii, 1043 (1976)). The above-mentioned is considered to be firmly concerned with nosogenesis of the impairment of memorization or memory which is main symptom of Alzheimer's disease (Whitehouse et al., Science, 215, 1237 (1982)). Therefore, there is a possibility that these disturbances are improved by potentiating cholinergic nervous system. However, agonists of muscarinic cholinergic receptor which have been used up to date have high toxicity in spite of showing efficacy and therefore have not been practically used (Wettsein et al., Psychopharmacology, 84, 572 (1984) and Hollander et al., Biol. Psychiatry, 22, 1067 (1987)).
On the other hand, in a highly information-oriented society, there increase diseases due to mental repression. As one of such diseases, depression can be exemplified. Although there are many medicaments for depression, they are not fully satisfiable in the points of fast-acting property and side effect.
So, more effective and safe medicaments are required for the above-mentioned diseases.
DISCLOSURE OF THE INVENTION
As a result of continuous effort and detailed investigation of the present inventors in view of the above-mentioned actual circumstances, it has now been found that a novel phenoxybenzene derivative and a salt thereof show anti-amnesic activity by oral administration in animal experiments such as experimental amnesic mice, that the above-mentioned compounds potentiate central chlolinergic neural function as a characteristic of anti-amnesic activity by acting on muscarinic chlorinergic receptors, that the above-mentioned compounds show potent antidepressive activity by both oral and parenteral administeration in a forced swimming test with rats and that toxicity of the above-mentioned compounds is low. Therefore the above-mentioned compounds have been found to be useful as a cognition enhancer and an antidepressant, and thus the present invention has been accomplished.
That is, the present invention relates to
1 a phenoxybenzene derivative having the formula (I): ##STR3## wherein R.sup.1 is hydrogen atom; an alkyl group having 1 to 3 carbon atoms; --OR.sup.6 wherein R.sup.6 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; or a halogen atom, cycloalkyl group having 3 to 5 carbon atoms, allyl group, vinyl group or carbon atoms or tetrahydropyranyl group, a halogen atom, 3 carbon atoms, ##STR4## wherein R.sup.10 and R.sup.11 are independently hydrogen atom; an alkyl group having 1-3 carbon atoms; ##STR5## wherein R.sup.12 is hydrogen atom or --OR.sup.13 wherein R.sup.13 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; or ##STR6## wherein R.sup.14 and R.sup.15 are independently hydrogen atom or an alkyl group having 1 to 3 carbon atoms and n.sup.2 is an integer of 1 to 3, cyano group, ##STR7## wherein R.sup.16 and R.sup.17 are independently hydrogen atom or an alkyl group having 1 to 3 carbon atoms, ##STR8## wherein R.sup.19 is hydrogen atom or --OR.sup.20 wherein R.sup.20 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; or ##STR9## or a phenyl group having the formula ##STR10## wherein R.s
REFERENCES:
patent: 3732247 (1970-05-01), Helsley et al.
Vosmer et al, E. M. "Action of the Antidepressant Pridefine (AHR-1118) on Biogenic Amines in the Rat Brain", Biochemical Pharmacology, vol. 29, pp. 2557-2562 (1980).
Fuse Yoshihide
Hidaka Takayoshi
Katsumi Ikuo
Kishida Hideyuki
Miwa Toshiaki
Kanagafuchi Kagaku Kogyo Kabushiki Kaisha
Lee Mary C.
McKane Joseph K.
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