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    • 2. 发明授权
    • Phosphate ester compound of hydroxy acid substituted phenol ester, preparation method and medical use thereof
    • 羟基酸取代苯酚酯的磷酸酯化合物,其制备方法和医疗用途
    • US09243009B2
    • 2016-01-26
    • US13702204
    • 2010-10-13
    • Wensheng ZhangJun YangJin Liu
    • Wensheng ZhangJun YangJin Liu
    • C07F9/09
    • C07F9/09C07F9/091
    • Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y═C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
    • 提供羟基酸取代苯基酯的磷酸酯化合物,其制备方法和医疗用途。 标题化合物如式(I)所示,其中Y = C1-4直碳链,M1和/或M2 = H,碱金属离子,质子化胺或质子化氨基酸。 该化合物在其水溶液中具有良好的水溶性和高稳定性,并且可以在体内酶的作用下快速释放2,6-二异丙基苯酚,其具有镇静,催眠和/或麻醉的作用。 通过保护式(I)化合物中2,6-二异丙基苯酚的羟基,2,6-二异丙基苯酚的首过代谢活性降低,合成化合物可用于镇静,催眠和/或麻醉。
    • 4. 发明申请
    • Phosphate Ester Compound of Hydroxy Acid Substituted Phenol Ester, Preparation Method and Medical Use Thereof
    • 羟基取代苯酚酯的磷酸酯化合物及其制备方法及用途
    • US20130085120A1
    • 2013-04-04
    • US13702204
    • 2010-10-13
    • Wensheng ZhangJun YangJin Liu
    • Wensheng ZhangJun YangJin Liu
    • C07F9/09
    • C07F9/09C07F9/091
    • Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y=C1-4 straight carbon chain, M1 and/or M2=H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2,6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2,6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
    • 提供羟基酸取代苯基酯的磷酸酯化合物,其制备方法和医疗用途。 标题化合物如式(I)所示,其中Y = C 1-4直链碳链,M 1和/或M 2 = H,碱金属离子,质子化胺或质子化氨基酸。 该化合物在其水溶液中具有良好的水溶性和高稳定性,并且可以在体内酶的作用下快速释放2,6-二异丙基苯酚,其具有镇静,催眠和/或麻醉的作用。 通过保护式(I)化合物中2,6-二异丙基苯酚的羟基,2,6-二异丙基苯酚的首过代谢活性降低,合成化合物可用于镇静,催眠和/或麻醉。