公开(公告)号：US4748175A

公开(公告)日：1988-05-31

申请号：US947700

申请日：1986-12-30

申请人： Endre Kasztreiner ,  Gyorgy Rabloczky ,  Nandor Makk ,  Gyorgy Cseh ,  Maria Kuhar nee Kurthy ,  Eszter Diesler ,  Laszlo Jaszlits ,  Laszlo Sebestyen ,  Janos Wellmann ,  Aniko Tegdes ,  Judit Sarossy nee Kincsesy ,  Peter Matyus ,  Andras Varro ,  Laszlo Szam ,  Sarolta Vegvari nee Gyurki

发明人： Endre Kasztreiner ,  Gyorgy Rabloczky ,  Nandor Makk ,  Gyorgy Cseh ,  Maria Kuhar nee Kurthy ,  Eszter Diesler ,  Laszlo Jaszlits ,  Laszlo Sebestyen ,  Janos Wellmann ,  Aniko Tegdes ,  Judit Sarossy nee Kincsesy ,  Peter Matyus ,  Andras Varro ,  Laszlo Szam ,  Sarolta Vegvari nee Gyurki

IPC分类号： A61K31/535 ,  A61K31/5383 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D498/04

CPC分类号： C07D498/04

摘要： The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.1-4 alkyl or benzyl group; furtherNR.sup.5 R.sup.6 may also represents a 6-membered, saturated, nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.2-4 alkoxycarbonyl or C.sub.1-4 hydroxyalkyl group;R.sup.3 and R.sup.4 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group;R.sup.9 stands for hydrogen or a C.sub.1-4 alkyl group unsubstituted or monosubstituted by an oxo, cyano, aminocarbonyl, C.sub.2-5 alkoxycarbonyl, pyridiyl, morpholinocarbonyl, or phenyl group or mono- or polysubstituted by OH group(s), with the proviso that R.sup.2 is different from chlorine, 4-morpholinyl and piperidyl group when R.sup.9 stands for hydrogen; orR.sup.2 is different from chlorine and 4-morpholinyl group when R.sup.9 stands for a methyl or benzyl group.The compounds of the formula (I) are capable to increase the myocardial contractile force (the performance of the failing heart) and the coronary blood flow, thus they can therapeutically be used for the treatment of the chronic heart failure and coronary disturbances.