N4-SUBSTITUTED TETRAHYDRO-1,2,4-OXADIAZIN-5-ONE DERIVATIVES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

The invention relates to new tetrahydro-1,2,4-oxadiazin-5-one derivatives having a CNS activity. More particularly, the invention concerns new N4-substituted tetrahydro-1,2,4-oxadiazin-5-ones of the formula (1) IMAGE (1) wherein R2 is benzyloxycarbonyl or alkylcarbonyl containing 1 to 4 carbon atoms in the alkyl moiety, preferably acetyl; R3 is phenyl optionally substituted with 1 to 3 lower alkoxy groups; and R4 is an aliphatic or cyclic alkyl group having 1 to 11 carbon atoms, hydroxymethyl, halomethyl or acyloxymethyl. According to another aspect of the invention there are provided processes for the preparation of compounds of formula (1). Still another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a compound of formula (1).