NOVEL HIDROXYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS

Hidroksilamin derivati predstavljeni opštom formulom (I), i njihove farmaceutski prihvatljive kiselinske adicione soli, u kojoj X je O, -NH ili grupa formule -NR'-, u kojoj R i R', nezavisno jedan od drugog su alkil, cikloalkil, fenilalkil; fenil grupa u datom slučaju supstituisana sa halo, haloalkil, alkil, alkoksi ili nitro; R1 je H ili alkanoil, R2 je H ili hidroksi u datom slučaju acilovan sa alkanoilom, i R3 je grupa formule -N(R4)R5 u kojoj R4 i R5, nezavisno jedan od drugog mogu biti H, alkil ili grupa formule -C(O)-NH-R u kojoj R je kao što je u prethodnom definisano, ili, R4 i R5, kada su uzeti zajedno sa susednim azotom sa kojim su povezani, obrazuju 5- do 7-člani hetero prsten koji može da sadrži jedan dodatni hetero atom odabran izmedju azota, kiseonika ili sumpora i koji je u datom slučaju supstituisan sa alkilom ili fenilalkilom. Prijava sadrži 5 zavisna patentna zahteva i 3 nezavisna patentna zahteva. PCT No. PCT/HU96/00033 Sec. 371 Date May 13, 1998 Sec. 102(e) Date May 13, 1998 PCT Filed Jun. 14, 1996 PCT Pub. No. WO97/00251 PCT Pub. Date Jan. 3, 1997The present invention provides novel hydroxylamine derivatives represented by the general formula: wherein: X is O, -NH, or a group of formula NR', wherein R and R' are independently selected from alkyl, cycloalkyl, phenylalkyl, phenyl optionally substituted with halo, haloalkyl, alkyl, alkoxy or nitro; and a N-containing heterocyclic ring; R1 is H or alkanoyl, R2 is H or hydroxy optionally acylated with alkanoyl, and R3 is a group of the formula -NR4R5 wherein R4 and R5 are independently selected from H, alkyl, and a group of the formula -CO-NH-R wherein R is as defined above, or wherein R4 and R5 when taken together form a 5- to 7-membered heterocyclic ring which may optionally contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl or phenylalkyl. Also provided are pharmaceutically acceptable acid addition salts of the compounds defined above, as well as pharmaceutical compositions containing the compounds or their acid addition salts as active ingredients. The compounds of the invention have been shown to have anti-ischemic effects.