BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE
    32.
    发明申请
    BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE 审中-公开
    苯并咪唑衍生物的钡盐

    公开(公告)号:US20110086884A1

    公开(公告)日:2011-04-14

    申请号:US12973499

    申请日:2010-12-20

    CPC classification number: C07D401/12 A61K31/4439

    Abstract: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.

    Abstract translation: 本发明涉及(S) - 奥美拉唑的结晶钡盐,其为(S)-5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基) - 甲基]亚磺酰基〕-1H 苯并咪唑。 本发明还涉及制备(S) - 奥美拉唑的结晶钡盐的方法和包括如此制备的(S) - 奥美拉唑的结晶钡盐的药物组合物。

    PROCESS FOR THE PREPARATION OF ORLISTAT
    33.
    发明申请
    PROCESS FOR THE PREPARATION OF ORLISTAT 审中-公开
    制备ORLISTAT的过程

    公开(公告)号:US20090171104A1

    公开(公告)日:2009-07-02

    申请号:US12089245

    申请日:2006-05-10

    CPC classification number: C07D305/12

    Abstract: The present invention provides a process for preparing orlistat (I) by alkanoylating an amino orlistat using formic acid anhydride as an alkanoylating agent to obtain orlistat substantially free of the byproduct, (S)-N-acetylleucine (1S)-1-[[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl]methyl] dodecyl ester (deformyl-N-acetyl orlistat).

    Abstract translation: 本发明提供了通过使用甲酸酐作为烷酰化剂烷基化氨基奥利司他来获得基本上不含副产物的奥利司他的(S)-N-乙酰基亮氨酸(1S)-1 - [[( 2S,3S)-3-己基-4-氧代-2-氧杂环丁烷基]甲基]十二烷基酯(去甲酰基-N-乙酰基奥利司他)。

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