Novel 1,2-benzoisoxazole derivative or its salt and...

C - Chemistry – Metallurgy – 07 – D

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C07D 261/20 (2006.01) A61K 31/395 (2006.01) C07D 413/00 (2006.01) C07D 413/04 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2146755

This invention relates to a 1,2-benzoisoxazole derivative represented by the following general formula (I) or its salt: Image (I) 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, heterocyclic, lower alkylene and lower alkenylene groups; R1 and R2, which may be the same or different, represent hydrogen atoms or substituted or unsubstituted lower alkyl groups; R3 represents a hydrogen atom or a substituted or unsubstituted lower alkyl, aryl, aralkyl or heterocyclic group; R4 represents a substituted or unsubstituted lower alkyl, aryl or heterocyclic group, or alternatively R3 and R4, when taken together, represent a lower alkylene group; R5 and R6, 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, and the above compound (I) of the invention has excellent cerebral hypoxia-protecting action, action of the prolongation of life of cerebral ischemic animal and anticonvulsive action and also is weak in central nervous system depressant action and high in safety, and hence, is effective for treating various diseases such as cerebral circulatory disorder not only in the acute phase but also in the chronic phase, head injury sequelae and epilepsy.

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