申请人:Toyo Jozo Kabushiki Kaisha
公开号:US04837319A1
公开(公告)日:1989-06-06
1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.
式子如下:##STR1## 其中A是低碳基;R.sub.1选自烷基、苯基-低碳基、取代苯基-低碳基;R.sub.2和R.sub.3分别是低碳基,或者一起形成四亚甲基,R选自羟基、卤素、低碳酰氧基、R.sub.4-氨基甲酰氧基、芳基硫醇、1-甲基四唑-5-基硫醇、1-咪唑、吗啉基、##STR2## 其中R.sub.4是低碳基或芳基,R.sub.5是氢、低碳基或芳基,R.sub.6是氢、低碳基、羟基-低碳基、芳基、芳基-低碳酰基、芳基羰基、芳基磺酰基或噻吩基-低碳酰基,Ar是苯基或取代了C.sub.1-3烷基、卤素、硝基或低碳氧基的苯基,其中A、R.sub.1、R.sub.2和R.sub.3如上所定义,m是4-6的整数,n为2或3;以及其药学上可接受的盐。这些化合物可用作抑制血小板聚集、扩张血管和抗脂质过氧化物生成的药物。