Triazine derivatives, processes for preparation thereof and pharmaceutical compositions comprising the same
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0122627A2
公开(公告)日:1984-10-24
New traizine derivatives represented by the formula:
wherein R1 is hydrogen; halogen or hydrazinocarbonyl
(lower) alkyl;
R2 is hydrazino;
azido;
halosulfonyl;
mono- or di(lower)alkylamino;
mono- or di-(lower)alkynylamino;
pyridylamino;
lower alkylideneamino substituted by furyl pyridyl or
aryl;
mono- or di-(lower) alkylamino substituted by amino, carboxy, hydroxy, ureido, lower alkoxy, lower alkoxycarbonyl, lower alkoxy (lower) alkoxy, aryl, furyl, pyridyl, phthalimido, or succinimido;
N-methyl (lower) alkanoylamino;
N-containing, 5- or 6-membered heterocyclic group
optionally substituted by oxo, lower alkyl and/or lower alkoxycalbonyl;
lower alkoxy substituted by hydroxy and lower alkvlamino: or
a group of the formula
in which R' is hydrogen; lower alkyl or ar (lower) alkyl;
R4 is pyridyl; aryl; styryl;
alkynyl; lower alkoxycarbonyl;
a-hydroxybenzyl; lower alkanoyl; carboxy; or lower alkyl
substituted by halogen, amino, hydroxy, carboxy, lower alkanoyl, lower alkanoyloxy, lower alkoxycarbonyl, morpholino, lower alkoxycarbonylamino, 1-methyl-2-oxo-1, 2, 3, 4-tetrahydroquinolyloxy, mono- or di(lower)alkylamino, piperazinyl being substituted with hydroxy(lower)alkyl or furoyl, or pyrrolidino; and pharmaceutically acceptable salt thereof, which are useful in the treatment of hypertension, thrombosis and ulcer in human beings and animals.
由以下式子表示的新的曲嗪衍生物
其中 R1 为氢、卤素或肼基羰基
(低级)烷基;
R2 是肼基
叠氮
卤磺酰基
单-或二-(低级)烷基氨基
单-或二-(低级)炔基氨基
吡啶氨基
被呋喃基吡啶或芳基取代的低级亚烷基氨基
芳基;
被氨基、羧基、羟基、脲基、低级烷氧基、低级烷氧羰基、低级烷氧基(低级)烷氧基、芳基、呋喃基、吡啶基、邻苯二甲酰亚胺或琥珀酰亚胺取代的单-或二-(低级)烷基氨基;
N-甲基(低级)烷酰氨基;
含 N 的 5 或 6 元杂环基团
可选择被氧代、低级烷基和/或低级烷氧基羰基取代的低级烷氧基;
被羟基和低级烷氨取代的低级烷氧基:或
式中的基团
其中 R' 是氢;低级烷基或 ar(低级)烷基;
R4 是吡啶基;芳基;苯乙烯基;
炔基;低级烷氧羰基;
a-羟基苄基;低级烷酰基;羧基;或低级烷基
被卤素、氨基、羟基、羧基、低级烷酰基、低级烷酰氧基、低级烷氧羰基、吗啉基、低级烷氧羰基氨基、1-甲基-2-氧代-1,2,3,4-四氢喹啉基氧基、单-或二(低级)烷基氨基、被羟基(低级)烷基或呋喃基取代的哌嗪基或吡咯烷基取代;及其药学上可接受的盐,可用于治疗人类和动物的高血压、血栓和溃疡。