POLYMORPHS OF ESOMEPRAZOLE SALTS
    3.
    发明申请
    POLYMORPHS OF ESOMEPRAZOLE SALTS 审中-公开
    异山梨醇的多糖

    公开(公告)号:US20120095054A1

    公开(公告)日:2012-04-19

    申请号:US13331404

    申请日:2011-12-20

    IPC分类号: A61K31/4439 C07D401/12

    CPC分类号: C07D401/12

    摘要: The present invention relates to a high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention further provides an improved and commercially viable process for preparation of high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides an improved process for preparation of pure amorphous esomeprazole magnesium. The present invention further provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The present invention also provides solid form of esomeprazole calcium salt, its polymorphs (form 1, form 2 and amorphous form) and processes for their preparation thereof.

    摘要翻译: 本发明涉及基本上不含其三水合物形式的高测定的艾美拉唑镁二水合物。 本发明进一步提供了一种改进的和商业上可行的制备基本上不含其三水合物形式的高测定的艾美拉唑镁二水合物的方法。 本发明还提供了制备纯无定形埃索美拉唑镁的改进方法。 本发明进一步提供了一种改进的和商业上可行的制备基本上为中性形式的对映体纯的艾美拉唑或作为其药学上可接受的盐或其溶剂化物包括水合物的方法。 本发明还提供了埃索美拉唑钙盐的固体形式,其多晶型物(形式1,形式2和无定形形式)及其制备方法。

    NOVEL PROCESS FOR PREPARATION OF CEFPROZIL INTERMEDIATE
    5.
    发明申请
    NOVEL PROCESS FOR PREPARATION OF CEFPROZIL INTERMEDIATE 失效
    新西兰中间体的制备新方法

    公开(公告)号:US20090048460A1

    公开(公告)日:2009-02-19

    申请号:US12257738

    申请日:2008-10-24

    IPC分类号: C07C45/89

    CPC分类号: C07D501/22 C07F7/188

    摘要: The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation.[R-(Z)]-[4-hydroxy-α-[(3-methoxy-1-methyl-3-oxo-1-propenyl)amino]] benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.

    摘要翻译: 本发明涉及一种制备头孢司定的关键中间体的方法,并且在制备头孢丙烯时使用该中间体,从而避免杂质自身酰化。 [R-(Z)] - [4-羟基-α-[(3-甲氧基-1-甲基-3-氧代-1-丙烯基)氨基]]苯乙酸,单钾盐与氯甲酸乙酯反应,得到混合 酸酐,然后用N,O-双(三甲基甲硅烷基)乙酰胺进行甲硅烷基化。 所得甲硅烷基化的化合物与[7-三甲基甲硅烷基氨基-3-(Z / E-丙烯-1-基)-3-头孢烯-4-羧酸]三甲基甲硅烷基酯反应,并用盐酸水溶液脱保护,得到头孢丙烯。

    GEMIFLOXACIN PROCESS AND POLYMORPHS
    6.
    发明申请
    GEMIFLOXACIN PROCESS AND POLYMORPHS 审中-公开
    GEMIFLOXACIN工艺和聚合物

    公开(公告)号:US20110136855A1

    公开(公告)日:2011-06-09

    申请号:US12890815

    申请日:2010-09-27

    IPC分类号: A61K31/4375 C07D471/04

    CPC分类号: C07D471/04

    摘要: The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.

    摘要翻译: 本发明提供了以高产率制备吉米沙星及其药学上可接受的酸加成盐的新方法。 本发明还涉及吉米沙星游离碱及其水合物的新型多晶型物及其制备方法以及包含它们的药物组合物。 本发明还涉及吉米沙星的输注溶液及其制备方法。 因此,将7-氯-1-环丙基-6-氟-4-氧代-1,4-二氢-1,8-萘 - 吖啶-3-羧酸与乙酸酐,乙酸和硼酸的混合物 得到硼烷化合物,然后在三乙胺存在下用4-氨基甲基-3-甲氧基亚氨基 - 吡咯烷鎓二甲磺酸盐处理,然后用3.5%氢氧化钠溶液处理,得到吉米沙星游离碱。

    AMORPHOUS ESOMEPRAZOLE HYDRATE
    8.
    发明申请
    AMORPHOUS ESOMEPRAZOLE HYDRATE 失效
    非晶异氰酸酯水合物

    公开(公告)号:US20090198066A1

    公开(公告)日:2009-08-06

    申请号:US12399514

    申请日:2009-03-06

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: The present invention relates to a novel amorphous form of esomeprazole hydrate, to a process for its preparation and to a pharmaceutical composition containing it. Thus, tetrahydrofuran and water are added to esomeprazole potassium salt at 25-30° C., cooled to 20° C. and then the pH is adjusted to 7.5-8.0 with acetic acid. The reaction mass is cooled to 5° C., stirred for 2 to 3 hours at 0-5° C., filtered the mass, washed with chilled mixture of water and tetrahydrofuran (2:1) and again washed with water. The wet cake is dried at 30-35° C. under vacuum to reach the moisture content to 25-30%. The solid is again dried in rotovapour at 25-30° C. under nitrogen atmosphere to give amorphous esomeprazole hydrate.

    摘要翻译: 本发明涉及一种新型的非晶形式的艾美拉唑水合物,其制备方法和含有它的药物组合物。 因此,将四氢呋喃和水在25-30℃加入到艾美拉唑钾盐中,冷却至20℃,然后用乙酸将pH调节至7.5-8.0。 将反应物质冷却至5℃,在0-5℃下搅拌2〜3小时,过滤物质,用冷却的水和四氢呋喃(2:1)的混合物洗涤,再次用水洗涤。 将湿滤饼在真空下在30-35℃下干燥以达到25-30%的含水量。 在氮气氛下,将固体在旋转蒸发器中再次干燥25-30℃,得到无定形艾美拉唑水合物。