1,2-benzoisoxazole derivative or its salt and brain-protecting a

Details 1,2-benzoisoxazole derivative or its salt and brain-protecting a 1,2-benzoisoxazole derivative or its salt and brain-protecting a

1995-04-12

1996-11-26

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548241, A61K 31405, C07D20910

Patent

active

055786278

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP93/01549 filed Oct. 27, 1993.


TECHNICAL FIELD

This invention relates to a novel 1,2-benzoisoxazole derivative or its salt or a brain-protecting agent comprising the same.


BACKGROUND ART

In the acute phase of cerebral circulatory disturbance, the principal object has heretofore been put in the treatment of which the primary purpose is life-saving, and substantially no treatment for relieving sequelae has been effected. On the other hand, in the chronic phase, various cerebral circulation and metabolism ameliorants have been used. However, since the symptomatology has already been fixed, an improvement of neurological symptoms and activities of daily living which improvement has been most desired has not been observed with these cerebral circulation and metabolism ameliorants.
Therefore, it has now become considered that an adequate treatment in the acute phase can relieve the sequelae, particularly neurological sequelae.
Accordingly, there has been desired a development of a compound which has a brain-protecting action by which cell death in the cerebral ischemia is depressed, is weak in such central depressant action as to make the whole body control of patient difficult, and is further chemically stable.


DISCLOSURE OF THE INVENTION

Under such circumstances, the present inventors have made extensive research and have consequently found that a compound obtained by introducing a group represented by the following formula: ##STR2## wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R.sub.6 have the same meanings as mentioned hereinafter, 1,2-benzoisoxazole derivative represented by the general formula (I) mentioned hereinafter or its salt, is a compound which has an excellent brain-protecting action by which cell death in the cerebral ischemic state is depressed, further is weak in central depressant action and hence, is useful as a curing agent for cerebral circulatory disturbance not only in the acute phase but also in the chronic phase, head injury sequelae and epilepsy, and is chemically stable, and further that it is useful as their precursor, whereby this invention has been completed.
An object of this invention is to provide a novel 1,2-benzoisoxazole derivative or its salt.
Also, another object of this invention is to provide a novel, chemically stable 1,2-benzoisoxazole derivative or its salt which has a brain-protecting action but is weak in central depressant action.
Moreover, a still another object of this invention is to provide a novel 1,2-benzoisoxazole derivative or its salt which is useful as a curing agent for cerebral circulatory disorder not only in the acute phase but also in the chronic phase, head injury sequelae and epilepsy.
According to this invention, there is provided a 1,2-benzoisoxazole derivative represented by the following general formula (I) or its salt: ##STR3## wherein R represents at least one member selected from hydrogen atom, halogen atoms, nitro group, cyano group, hydroxyl group and substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, aralkyl, aryl, lower alkyloxy, cycloalkyl, aralkyloxy, aryloxy, amino, lower acyl, arylcarbonyl, lower alkanesulfonyl, arenesulfonyl, lower alkylthio, carbamoyl, lower alkylene, lower alkenylene and heterocyclic groups; R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen atoms or substituted or unsubstituted lower alkyl groups; R.sub.3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl, aryl, aralkyl or heterocyclic group; R.sub.4 represents a substituted or unsubstituted lower alkyl, aryl or heterocyclic group, or alternatively R.sub.3 and R.sub.4, when taken together, represent a lower alkylene group; R.sub.5 and R.sub.6, which may be the same or different, represent hydrogen atoms or substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, lower acyl, lower alkyloxycarbonyl or aralkyl groups.
This invention is described in detail below.
In the present specification, unless otherwise specified, each term has the follo

REFERENCES:
CA 70:37702b Biological . . . 3-alkylaminoalkoxybenzisothiazoles., Vitali et al., p. 341, 1969.
CA 71:49831b Biological . . . 3-(alkylaminoalkoxy)-benzisothiazoles., Vitali et al., p. 383, 1969.
CA 72:31781w 1,2-Benzisothiazole . . . ethers. Vitali et al., p. 337, 1970.

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