OPTICAL RESOLUTION OF SUBSTITUTED 2-(2- PYRIDINYLMETHYLSULPHINYL)-1H-BENZIMIDAZOLES
    42.
    发明公开
    OPTICAL RESOLUTION OF SUBSTITUTED 2-(2- PYRIDINYLMETHYLSULPHINYL)-1H-BENZIMIDAZOLES 审中-公开
    分辨率取代的2-(2-吡啶基甲基)-1H-苯并咪唑

    公开(公告)号:EP2486032A2

    公开(公告)日:2012-08-15

    申请号:EP09850200.8

    申请日:2009-10-09

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12 C07B57/00

    摘要: The present invention relates to process for preparation of optical resolution of substituted 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles either as a single enantiomer or in an enantiomerically enriched form. Thus, for example, R-1,1'-binaphtyl- 2-2'-diyl hydrogen phosphate was reacted with 2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)- 2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (Lansoprazole) in a mixture of benzene and cyclohexane to obtain diasteremeric complexes. The diasteremeric complexes were subjected to fractional crystallization to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro- ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole.R-1,1'-binaphthyl-2-2'-diyl hydrogen phosphate. The separated isomer was treated with sodium bicarbonate in a mixture of ethyl acetate and water to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2- pyridinyl]methyl]sulfinyl]-1H-benzimidazole (dexlansoprazole).

    PROCESS FOR FEBUXOSTAT
    45.
    发明公开
    PROCESS FOR FEBUXOSTAT 审中-公开
    VERFAHRENFÜRFEBUXOSTAT

    公开(公告)号:EP2718272A2

    公开(公告)日:2014-04-16

    申请号:EP12796916.0

    申请日:2012-05-21

    IPC分类号: C07D277/32

    CPC分类号: C07D277/56 A61K31/426

    摘要: The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 µm, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles.

    摘要翻译: 本发明提供了制备2-(4-羟基苯基)-4-甲基噻唑-5-甲酸乙酯的方法。 本发明还提供了制备2-(3-甲酰基-4-羟基苯基)-4-甲基噻唑-5-甲酸乙酯的方法。 本发明进一步提供了昂布斯坦的新型结晶形式,其制备方法和包含它们的药物组合物。 本发明还提供平均粒径小于约25μm的Febustostat结晶颗粒,制备所述结晶颗粒的方法和包含所述结晶颗粒的药物组合物。

    PROCESS FOR PEMETREXED DISODIUM
    48.
    发明公开
    PROCESS FOR PEMETREXED DISODIUM 审中-公开
    VERFAHRENFÜRPEMETREXED-DINATRIUM

    公开(公告)号:EP2675808A2

    公开(公告)日:2013-12-25

    申请号:EP12747282.7

    申请日:2012-02-14

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention provides a process for the preparation of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid dimethyl ester or salts thereof. The present invention also provides a process for the preparation of pemetrexed disodium substantially free of enatiomeric impurity.

    摘要翻译: 本发明提供了制备N- [4- [2-(2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基)乙基 ]苯甲酰基] -L-谷氨酸二甲酯或其盐。 本发明还提供了一种制备基本上不含对映体杂质的培美曲塞二钠的方法。

    POLYMORPHS OF DEXLANSOPRAZOLE SALTS
    49.
    发明公开
    POLYMORPHS OF DEXLANSOPRAZOLE SALTS 审中-公开
    多异氰酸酯

    公开(公告)号:EP2663306A1

    公开(公告)日:2013-11-20

    申请号:EP11855797.4

    申请日:2011-11-11

    IPC分类号: A61K31/44

    CPC分类号: A61K31/4439 C07D401/12

    摘要: The present invention provides a solid of dexlansoprazole sodium. The present invention also provides novel crystalline forms of dexlansoprazole sodium, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides a novel amorphous form of dexlansoprazole sodium, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a novel process for the preparation of dexlansoprazole amorphous form and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of dexlansoprazole crystalline form I. The present invention further provides a process for the preparation of dexlansoprazole crystalline form II.

    摘要翻译: 本发明提供了右兰索拉唑钠的固体。 本发明还提供了右兰索拉唑钠的新型结晶形式,其制备方法和包含它们的药物组合物。 本发明还提供了一种新型无定形形式的右兰索拉唑钠,其制备方法和包含它的药物组合物。 本发明还提供了一种制备右兰索拉唑无定形形式的新方法和包含它的药物组合物。 本发明还提供了一种制备右兰索拉唑结晶形式I的方法。本发明还提供一种制备右恩索拉唑结晶形式II的方法。