申请人:Akzona Incorporated
公开号:US04028380A1
公开(公告)日:1977-06-07
The invention relates to novel amidino-hydrazone derivatives of the general formula: ##STR1## in which the dotted lines mean one extra bond starting from the (guanidine-)carbon atom to one of the adjacent nitrogen atoms, and A stands for methylene, ethylene, propylene or butylene, which groups may optionally be substituted with alkyl (1-4 C), R stands for hydroxy, alkyl (1-4 C), alkylthio or alkoxy (1-4 C), halogen, trifluoromethyl, nitro, amino, hydroxymethyl, acyloxy or an alkylenedioxy group, n is the number 0, 1, 2, 3 or 4, R.sub.1, r.sub.4 and R.sub.5 represent hydrogen or alkyl (1-4 C), with the proviso that one of them is absent in view of the presence of the double bond, R.sub.2 and R.sub.3 stand for hydrogen, alkyl (1-4 C), aralkyl, aryl, hydroxy or amino, with the proviso that R.sub.2 + r.sub.3 together may also represent a saturated or unsaturated alkylene group with 2 or 3 carbon atoms, or R.sub.3 + r.sub.4 together with the nitrogen atom may also stand for a heterocyclic five- or six-membered ring, As well as the pharmaceutically acceptable acid addition salts thereof, having valuable, antihypertensive and antithrombosis activities.
本发明涉及新的一般式为:##STR1## 的酰胺肼衍生物,其中虚线表示从(胍基)-碳原子到相邻氮原子之一的额外键,A代表亚甲基,乙烯基,丙烯基或丁烷基,这些基团可以选择性地被取代为烷基(1-4C),R代表羟基,烷基(1-4C),烷基硫醚或烷氧基(1-4C),卤素,三氟甲基,硝基,氨基,羟甲基,酰氧基或烷基二氧基基团,n为数字0、1、2、3或4,R1、r4和R5代表氢或烷基(1-4C),但其中一个因存在双键而不存在,R2和R3代表氢、烷基(1-4C)、芳基烷基、芳基、羟基或氨基,但R2 + r3也可以表示饱和或不饱和的2或3碳原子的烷基,或者R3 + r4连同氮原子也可以表示杂环五元或六元环,以及其药学上可接受的酸加合盐,具有有价值的降压和抗血栓活性。