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    • 3. 发明申请
    • ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS, AND USE
    • 乙酰甲基胆碱酯酶,合成方法和用途
    • WO2006050472A2
    • 2006-05-11
    • PCT/US2005039872
    • 2005-11-03
    • XENOPORT INCGALLOP MARK A
    • GALLOP MARK A
    • C07F9/301C07F9/4816
    • Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3­aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3­aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3­aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-­aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
    • 3-氨基丙基亚磷酸,3-氨基丙基次膦酸及其类似物的氨基氧基烷基氨基甲酸酯前药,包含3-氨丙基亚磷酸,氨基丙基次膦酸及其类似物的酰氨基烷基氨基甲酸酯前药的药物组合物,制备3-氨基丙基亚磷酸,3-氨基丙基次膦酸 及其类似物,公开了使用3-氨基丙基亚膦酸,3-氨基丙基次膦酸及其类似物的前药的方法及其药物组合物,用于治疗或预防诸如痉挛性或胃食道反流病等疾病或病症。 还公开了适用于口服给药的3-氨基丙基亚膦酸,3-氨基丙基次膦酸及其类似物的氨基氧烷基氨基甲酸酯前药和缓释口服剂型。