Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-03-20
1993-04-27
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514339, 546273, 548486, C07D20934, A01K 3140
Patent
active
052062619
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel oxindole 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 oxindole 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 an oxindole derivative represented by the formula ##STR2## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, cyano group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.4 is 1-propylbutyl group; pyridyl group; or phenyl group which may be substituted by lower alkoxyl group, halogen atom, diethylamino group, benzyloxy group, trifluoromethyl group, cyano group, nitro group or lower alkyl group.
In the invention, examples of lower alkyl groups represented by R.sup.1, R.sup.2, R.sup.4 and R.sup.5 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 halogen atoms represented by R.sup.1, R.sup.4 and R.sup.5 are fluorine, chlorine, bromine and iodine. Examples of lower alkoxyl groups represented by R.sup.1, R.sup.4 and R.sup.5 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. Examples of alkyl groups which may form a ring and represented by R.sup.5 are preferably the above lower alkyl groups and cycloalkyl groups having 3 to 6 carbon atoms such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl group.
When R.sup.5 of the above formula (1) is 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 hydrogen atom or lower alkoxyl group, R.sup.2 is hydrogen atom, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group and diethylamino group), R.sup.4 is 1-propylbutyl group, pyridyl group or phenyl group which may have plural lower alkoxyl groups as substituents. More preferable are those wherein R.sup.1 and R.sup.2 are each hydrogen atom, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being phenyl group substituted by 1 to 3 methoxy groups), R.sup.4 is 4-methoxyphenyl group or phenyl group.
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 c
REFERENCES:
Coda, J. Chem. Res. Synop (3) 84 (1986).
Kajitani Makoto
Kawaguchi Akihiro
Sato Atsushi
Yamamoto Junji
Yasumoto Mitsugi
Gerstl Robert
Taiho Pharmaceutical Company Limited
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