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New amines and their application to the treatment of cardiovascular disease

机译:新胺及其在心血管疾病治疗中的应用

摘要

For the preparation of novel hydroxyamines of the formula (I) IMAGE with the radicals as in Patent Claim 1, and of therapeutically acceptable acid addition salts of these compounds, a starting compound of the formula (II) IMAGE is used. This is reacted with an amine of the formula (III) IMAGE The resulting isomeric mixtures are separated into the pure isomers and the resulting racemates into the optical antipodes. The resulting free bases can be converted into their salts and the resulting salts converted into the corresponding free bases. Preferred compounds prepared are: 1) 1-[2-(4-carbamylphenoxy)ethylamino]-3-(2-allylphenoxy)propan-2-ol, 2) 1-[2-(4-carbamylphenoxy)ethylamino]-3-(2-methoxyethyl)phenoxy-propan-2 -ol, 3) 1-[1-methyl-2-(4-carbamylphenoxy)ethylamino]-3-(2-allyl-phenoxy)propan -2-ol, 4) 1-[1-methyl-2-(2-methylphenoxy)ethylamino]-3-(2-allylphenoxy)-propan-2 -ol, 5) 1-[1-methyl-2-(4-methylphenoxy)ethylamino]-3-(2-allylphenoxy)-propan-2 -ol, 6) 1-[1-methyl-2-(4-carbamylphenoxy)ethylamino]-3-(2-methylisonitrosometh ylphenoxy)propan-2-ol, 7) 1-[2-(4-carbamylphenoxy)ethylamino]-3-(3-allylphenoxy)-propan-2-ol. The compounds have a blocking effect on beta -receptors and can be employed for the treatment of cardiovascular disorders.
机译:为了制备如权利要求1所述的具有自由基的式(I)的新的羟基胺,以及这些化合物的治疗上可接受的酸加成盐,使用式(II)的起始化合物。将其与式(III)的胺反应。<图像>将所得异构体混合物分离为纯异构体,并将所得外消旋体分离为旋光对映体。可以将所得的游离碱转化成它们的盐,并且将所得的盐转化成相应的游离碱。制备的优选化合物是:1)1- [2-(4-氨基甲酰基苯氧基)乙氨基] -3-(2-烯丙基苯氧基)丙-2-醇,2)1- [2-(4-氨基甲酰基苯氧基)乙氨基] -3- (2-甲氧基乙基)苯氧基丙烷-2-醇,3)1- [1-甲基-2-(4-氨基甲酰基苯氧基)乙氨基] -3-(2-烯丙基-苯氧基)丙烷-2-醇,4)1 -[1-甲基-2-(2-甲基苯氧基)乙基氨基] -3-(2-烯丙基苯氧基)-丙烷-2-醇,5)1- [1-甲基-2-(4-甲基苯氧基)乙基氨基] -3 -(2-烯丙基苯氧基)-丙烷-2-醇,6)1- [1-甲基-2-(4-氨基甲酰基苯氧基)乙氨基] -3-(2-甲基异硝基苄基苯氧基)丙烷-2-醇,7)1- [2-(4-氨基甲酰基苯氧基)乙氨基] -3-(3-烯丙基苯氧基)-丙烷-2-醇。所述化合物对β-受体具有阻断作用,并可用于治疗心血管疾病。

著录项

  • 公开/公告号FR2289172B1

    专利类型

  • 公开/公告日1980-11-21

    原文格式PDF

  • 申请/专利权人 HASSLE AB;

    申请/专利号FR19750032204

  • 发明设计人

    申请日1975-10-21

  • 分类号A61K31/135;C07C93/06;

  • 国家 FR

  • 入库时间 2022-08-22 15:07:55

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