Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-10-01
1993-02-09
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514421, 546183, 548512, A61K 31435, C07D 2204
Patent
active
051853442
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel bicyclolactam derivative. The present compound has cerebral function improving effect, cerebral metabolism activating or anoxic brain damage protecting effect and effect against senile dementia.
BACKGROUND ART
With an increase in the population of advanced ages in recent years, patients with senile dementia increase in number, posing a serious problem medically and socially. Although various antidementia drugs have been investigated and developed in view of the situation, no compounds have been provided with satisfactory efficacy. It has been strongly desired to develop medicaments for treating the disease.
An object of the present invention is to provide novel bicyclolactam derivatives which are very useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives.
DISCLOSURE OF THE INVENTION
The present invention provides a bicyclolactam derivative represented by the formula ##STR2## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.
The above bicyclolactam derivative of the formula (1) includes stereoisomers due to the presence of bicyclo ring and optical isomers derived from asymmetric carbon atom and all of the isomers are included in the present invention.
In the invention, examples of halogen atoms which are a substituent of benzoyl group represented by R are fluorine, chlorine, bromine and iodine atom. Examples of lower alkyl groups are preferably a straight-chain or branched-chain alkyl group having 1 to 6 carbon atoms such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl and hexyl group. Examples of lower alkoxyl groups are preferably a straight-chain or branched-chain alkoxyl group having 1 to 6 carbon atoms such as methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, pentyloxy, isopentyloxy and hexyloxy group. The benzoyl group preferably has 1 to 3 substituents.
Among the compounds of the formula (1), preferable are those wherein R is benzoyl group which is substituted with lower alkoxyl group or amino group, l is 1 or 2, m is 0 or 1, and n is 0 or 2. Further, more preferable are those wherein R is benzoyl group which is substituted with lower alkoxyl group, when l is 1, m is 0, and n is 2, or when l is 2, m is 1, and n is 0.
Further, we have found that the present compound of the formula (1) has an excellent cerebral function improving effect, cerebral metabolism activating or anoxic brain damage protecting effect and effect against senile dementia.
Accordingly, the present invention provides a cerebral function improving composition and a cerebral metabolism activating or anoxic brain damage protecting composition each comprising an effective amount of a compound of the formula (1) and a pharmacologically acceptable carrier.
The present invention further provides a method of improving cerebral functions and activating cerebral metabolism or protecting anoxic brain damage characterized by administering an effective amount of a compound of the formula (1).
The compounds of the formula (1) have pharmacological activities to ameliorate: response.
These pharmacological properties are useful for activating injured nervous cells and ameliorate memory and learning disturbances.
Accordingly, the compounds of the present invention are usable not only as medicaments for use in treating deterioration of intelligence or neurasthenia, amnesia, senile dementia or intellectual fatigue, cerebrovascular dementia, aftereffects of encephalopathy and Alzheimer's disease but also as medicaments for improving other cerebral functions or for activating cerebral metabolism or protecting anoxic brain damage.
The bicyclolactam derivative (1) of the present invention can be prepared
REFERENCES:
Kennewell et al., J. Chem. Soc. Perkin Trans. I, pp. 2563-2570 (1982).
Kajitani Makoto
Kawaguchi Akihiro
Satoh Atsushi
Yamamoto Junji
Yasumoto Mitsugi
Dentz Bernard
Taiho Pharmaceutical Company Ltd.
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