会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明授权
    • .omega.-(N-acylamino)alkylphosphoryl ethanolamines, pharmaceutical
compositions containing them, and their uses
    • {107-(N-酰基氨基)烷基磷酰基乙醇胺,含有它们的药物组合物及其用途
    • US3985875A
    • 1976-10-12
    • US537601
    • 1974-12-30
    • Kouji HayashiMasahisa HashimotoKiyoshi NakamuraMasanao ShimizuNaonobu HatanoKunihiko Takeyama
    • Kouji HayashiMasahisa HashimotoKiyoshi NakamuraMasanao ShimizuNaonobu HatanoKunihiko Takeyama
    • C07F9/09A01N9/36
    • C07F9/091Y02P20/55Y10S530/86
    • New .omega.-(N-acylamino)alkylphosphoryl ethanolamines and their pharmaceutically acceptable acid addition salts have superior renin-inhibitory activities, antihypertensive activities and cholesterol-lowering activities. The .omega.-(N-acylamino)alkylphosphoryl ethanolamines are prepared by (1) reacting an .omega.-(N-acylamino) alkanol with a 2-(N-substituted amino)ethyl phosphate or its derivative, hydrolyzing the resulting product or splitting off the phosphoric acid-protective group of the resulting product thereby to form an .omega.-(N-acylamino) alkyl 2-(N-substituted amino) ethyl phosphate, and splitting off the amino-protective groups of the resulting phosphate, or (2) reacting an .omega.-(N-acylamino) alkanol with a phosphorus oxyhalide, reacting the resulting .omega.-(N-acylamino)alkyl dichlorophosphate with a 2-(N-substituted amino) ethanol, hydrolyzing the reaction product to form an .omega.-(N-acylamino) alkyl 2-(N-substituted)ethyl phosphate, and splitting off the amino-protective groups of said phosphate.
    • 新的ω-(N-酰基氨基)烷基磷酰基乙醇胺及其药学上可接受的酸加成盐具有优异的肾素抑制活性,降压活性和降胆固醇活性。 ω-(N-酰氨基)烷基磷酰基乙醇胺通过以下步骤制备:(1)使ω-(N-酰氨基)链烷醇与2-(N-取代氨基)乙基磷酸酯或其衍生物反应,水解得到的产物或将 得到产物的磷酸保护基,从而形成2-(N-取代氨基)乙基磷酸的ω-(N-酰基氨基)烷基酯,并分离得到的磷酸酯的氨基保护基,或(2)使 将具有卤代磷酸酯的ω-(N-酰基氨基)链烷醇与所得的ω-(N-酰基氨基)烷基二氯磷酸酯与2-(N-取代的氨基)乙醇反应,水解反应产物以形成ω-(N- 酰基氨基)烷基2-(N-取代)乙基磷酸酯,并分离出所述磷酸酯的氨基保护基团。