Amidines, preparation process and therapeutical application thereof
    1.
    发明授权
    Amidines, preparation process and therapeutical application thereof 失效
    脒,其制备方法及其治疗应用

    公开(公告)号:US4665085A

    公开(公告)日:1987-05-12

    申请号:US717185

    申请日:1985-03-12

    摘要: Compounds having the formula (I) wherein R.sub.1 and R.sub.2 are a hydrogen atom, an alkyl group or a hydroxy group, or else R.sub.1 and R.sub.2 form together a bivalent ethylene or trimethylene radical; R.sub.3 is a halogen atom, an alkyl group, an alkoxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or di-alkyl amino group, an acetamido or sulfonamido group; R.sub.1 is a hydroxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or dialkyl amino group, an acetamido or sulfonamido group; R.sub.4 being in the position 3, 4 or 5 and A is a bridge having from 1 to 3 links selected among the groups having the formula (II), --NH--,--N.dbd.--O-- and --S--. R.sub.5 represents an hydrogen atom, an alkyl group, a hydroxy group or an alkoxy group as well as the addition salts thereof with pharmaceutically acceptable acids. Said compound may be used in therapeutical treatment as antihypertensive agents, particularly in the ocular field. ##STR1##

    摘要翻译: PCT No.PCT / FR84 / 00170 Sec。 371日期1985年3月12日 102(e)1985年3月12日PCT PCT。1984年7月6日PCT公布。 公开号WO85 / 00366 1985年1月31日。具有式(I)的化合物,其中R 1和R 2是氢原子,烷基或羟基,或者R 1和R 2一起形成二价乙烯或三亚甲基; R3是卤素原子,烷基,烷氧基,单羟基或多羟基化烷基,氨基,一或二烷基氨基,乙酰氨基或亚磺酰氨基; R1是羟基,单羟基烷基或多羟基化烷基,氨基,一或二烷基氨基,乙酰氨基或亚磺酰氨基; R4为位置3,4或5,A为选自具有式(II)的基团,-NH - , - N = -O-和-S-的1至3个连接的桥。 R5表示氢原子,烷基,羟基或烷氧基,以及其与药学上可接受的酸的加成盐。 所述化合物可用作治疗性治疗作为抗高血压药,特别是在眼部。 (I)(II)