Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-12-27
1993-01-26
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544 52, A61K 3154, C07D27916
Patent
active
051822768
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a nootropic agent which comprises a derivative of 2-phenyl-3-oxo-2H-1,4-benzothiazine, for instance, a nootropic agent which is effective in treating or presenting diseases accompanied by a lowering of cerebral functions such as cerebral infarction and transitory cerebral ischemic attack.
BACKGROUND ART
In Japan, the average span of human life has been increased and correspondingly patients suffering from diseases accompanied by a lowering of cerebral functions such as dementia, mental disorder, neurosis or the like associated with after-effects of cerebral infarction, cerebral arterial sclerosis or the like have been rapidly increased. This has become a serious social problem.
There have been compelling demands for the development of a medicine which shows excellent effect of treating or improving these diseases accompanied by the lowering of cerebral functions, but there has not yet been proposed any medicine exhibiting a satisfied effect for these diseases.
On the other hand, Japanese Patent Unexamined Publication (hereinafter referred to as "J.P. KOKAI") No. Sho 62-123181 discloses that a derivative of 2-phenyl-3-oxo-2H-1,4-benzothiazine represented by the following general formula (I) exhibits a platelet aggregation inhibiting effect and calcium antagonism and is useful as an agent for treating circulatory diseases, but does not disclose or suggest, at all, that the derivative be effective as a nootropic agent.
DISCLOSURE OF THE INVENTION
The inventors of this invention have conducted various studies to solve the foregoing problems, have found out that the compound represented by the general formula (I) disclosed in J.P. KOKAI No. Sho 62-123181 has an excellent effect as nootropic agent and thus have completed the present invention.
Accordingly, the present invention provides a nootropic agent which comprises, as an effective component, a compound represented by the following general formula (I) or salts thereof ##STR1## wherein R.sub.1 represents one or more of groups selected from the group consisting of a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, a hydroxyl group, a lower alkoxy group, a lower alkanoyloxy group, an amino group, a lower alkylamino group and a lower alkoxycarbonyloxy group; R.sub.2 represents a hydrogen atom, a lower alkyl group or a cycloalkyl group having 3 to 6 carbon atoms; R.sub.3 represents one or more groups selected from the group consisting of a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, a hydroxyl groups a lower alkoxy group, a lower alkylenedioxy group, a lower alkanoyl group, a lower alkanoyloxy group, an amino group, a lower alkylamino group, a lower alkanoylamino group and a lower alkoxycarbonyloxy group, or a group: ##STR2## R.sub.4 represents a hydrogen atom or a lower alkyl group; A and B may be the same or different and each represents a lower alkylene group having 1 to 6 carbon atoms; and n is 3 or 4].
BEST MODE FOR CARRYING OUT THE INVENTION
In Formula (I), the term "a lower alkyl group" means an alkyl group having 1 to 6 carbon atoms such as a methyl, ethyl, propyl and hexyl groups; the term "a halogen atom" means a fluorine, chlorine, bromine atom or the like; the term "a lower alkoxy group" means an alkoxy group having 1 to 6 carbon atoms such as methoxy, ethoxy, propoxy and hexyloxy groups; and the term "a lower alkanoyloxy group" means alkanoyloxy group having 1 to 6 carbon atoms such as acetyloxy, propionyloxy and hexanoyloxy groups. Examples of the cycloalkyl groups having 3 to 6 carbon atoms are cyclopropyl group, cyclohexyl groups and the like. The term "a lower alkylenedioxy group" means a group formed by bonding each of two oxygen atoms to the terminal carbon atoms of an alkylene group having 1 to 6 carbon atoms such as methylenedioxy and ethylenedioxy groups; and the term "a lower alkanoyl group" means an alkanoyl group having 1 to 6 carbon atoms such as an acetyl, propionyl and hexanoyl groups.
Examples of the salts of the compounds of Formula (
REFERENCES:
patent: 3166554 (1965-01-01), Krapcho
patent: 4640916 (1987-02-01), Meguro et al.
patent: 4654372 (1987-03-01), Marcoux
Hata, Medical Pharmacy, 1991, 25:33(85)-39(92).
Wauquier et al, The Japanese Journal of Pharmacology, vol. 38, No. 1, (1985) 1-7, "`Calcium Entry Blockers`" as Cerebral Protecting Agents: Comparative Activity in Tests of Hypoxia and Hyperexcitability.
Reynolds, Martindale--The Extra Pharmacopoeia, 29th Edition, p. 1492 "Vasodilators".
Yoshitomi Seiyaku K.K., Patent Abstracts of Japan, vol. 5, No. 111, (1981), "Benzothiazine Derivative".
Ashida Shinichiro
Shirasaki Yasufumi
Daiichi Pharmaceutical Co. Ltd.
Ford John M.
Santen Pharmaceutical Co. Ltd.
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