ANTI-ISCHAEMIC HYDROXYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS

摘要

The invention relates to novel hydroxylamine derivatives represented by general formula (I), the pharmaceutically acceptable acid addition salts thereof as well as the pharmaceutical compositions containing the same as active ingredient. Another object of the invention is the preparation of the hydroxylamine derivatives and salts thereof. The compounds according to the invention possess anti--ischaemic effect. In the above formula (I) X is O, -NH or a group of the formula -NR'-, wherein R and R', independently from each other, are alkyl, cycloalkyl, phenylalkyl; a phenyl group optionally substituted with halo, haloalkyl, alkyl, alkoxy or nitro; or an N-containing hetero ring; R1 is H or alkanoyl; R2 is H or hydroxy optionally acylated with alkanoyl; and R3 is a group of the formula -N(R4)R5 wherein R4 and R5, independently from each other, may be H, alkyl or a group of the formula -C(O)-NH-R wherein R is as defined above, or R4 and R5, when taken together with the adjacent nitrogen attached theret o, form a 5 to 7-membered hetero ring which may contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which i s optionally substituted with alkyl of phenylalkyl.