Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1990-08-16
1991-11-26
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514300, 514387, 544282, 546121, 548302, A61K 31505, A61K 3144, A61K 31415, C07D51502
Patent
active
050682350
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a diazabicycloalkane derivative which is novel compound and is not disclosed in the literature. The present compound has a cerebral function improving effect, a cerebral metabolism activating effect and is effective 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.
An object of the present invention is to provide novel diazabicycloalkane 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 diazabicycloalkane derivative represented by the formula ##STR2## wherein R.sup.1 is phenyl group, thienyl group or furyl group, the phenyl group may have lower alkoxyl, lower alkyl or halogen atom as a substituent, R.sup.2 is oxygen atom or sulfur atom, m is 3 or 4, n is 1 or 2.
In the invention, examples of lower alkoxyl groups, which are a substituent for the phenyl group represented by R.sup.1, are 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, t-butoxy, n-pentyloxy, isopentyloxy and hexyloxy group. Lower alkyl group means 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, t-butyl, n-pentyl, isopentyl and hexyl group. Examples of halogen atoms are fluorine, chlorine, bromine and iodine. When R.sup.1 represents a substituted phenyl group, the group preferably has 1 to 3 substituents.
Among the compounds of the formula (1), preferable are those wherein R.sup.1 is a phenyl group having or not having 1 to 3 substituents selected from among lower alkoxyl, lower alkyl and halogen atom. More preferable are compounds of the formula (1) wherein R.sup.1 is a phenyl group having one lower alkoxyl as a substituent, m is 3 and n is 2.
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 is effective 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:
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, ammnesia, 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 diazabicycloalkane derivative (1) of the present invention can be prepared, for example, by the following reaction processes.
a) Diazabicycloalkanone ##STR3##
b) Diazabicycloalkanethione ##STR4## wherein R.sup.1, m and n are same as above, R.sup.3 is methyl or ethyl.
Namely, the present compound is prepared by reacting a diazabicycloalkanone or diazabicycloalkanethione of
REFERENCES:
Arch. Pharm., vol. 294 (1961), K. Winterfeld et al., [Reactivity of 2-Aza-3-Oxoindolizidine], pp. 404-410.
Chem. Letter, No. 6 (1975), M. Watanabe et al., [Azafulvenes. 1. Novel Generative Method of 6-Amino-1-Azafulvene and its Cycloaddition Reaction with Isothiocycanate], pp. 607-610.
Hasegawa Etsuo
Kajitani Makoto
Kasahara Nobuo
Kawaguchi Akihiro
Yamamoto Junji
Grumbling Matthew V.
Shah Mukund J.
Taiho Pharmaceutical Company Limited
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