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    Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    1.
    发明公开
    Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 审中-公开
    Synthese von Acyloxalkylcarbamat-Prodrugs und Zwischenprodukten davon

    公开(公告)号：EP2354120A1

    公开(公告)日：2011-08-10

    申请号：EP10010650

    申请日：2004-08-20

    申请人： XENOPORT INC

    发明人： GALLOP MARK A ,  YAO FENMEI ,  LUDWIKOW MARIA J ,  PHAN THU ,  PENG GE

    IPC分类号： C07C271/22 ,  A61K31/195 ,  C07D207/40 ,  C07D207/416 ,  C07D213/79 ,  C07D213/80 ,  C07D307/30 ,  C07D333/38 ,  C07D401/04

    CPC分类号： C07C271/22 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/79 ,  C07D307/30 ,  C07D333/38

    摘要： The present invention relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-tluorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The present invention also relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

    摘要翻译： 本发明涉及（±）-4-氨基-3-（4-氟苯基）丁酸及其类似物的氨基氧基烷基氨基甲酸酯前药，其药物组合物，制备（±）-4-氨基-3-（ （±）-4-氨基-3-（4-氟苯基）丁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常见疾病和/或障碍 如痉挛和/或酸反流疾病。 本发明还涉及适用于口服给药的（±）-4-氨基-3-（4-氟苯基）丁酸及其类似物的氨氧基烷基氨基甲酸酯前药及其缓释口服剂型。