PROCESS FOR PEMETREXED DISODIUM
    63.
    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
    64.
    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。

    SALTS OF LAPATINIB
    66.
    发明公开
    SALTS OF LAPATINIB 审中-公开
    SALZE VON LAPATINIB

    公开(公告)号:EP2601178A2

    公开(公告)日:2013-06-12

    申请号:EP11814205.8

    申请日:2011-08-01

    IPC分类号: C07D239/72

    CPC分类号: C07D405/10 C07D405/04

    摘要: The present invention provides novel dioxalate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel monobesylate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of monohydrate form of lapatinib ditosylate. The present invention further provides a process for the preparation of anhydrous form of lapatinib ditosylate.

    摘要翻译: 本发明提供了拉帕替尼的新型二恶烷酸盐,其制备方法和包含其的药物组合物。 本发明还提供了新颖的拉帕替尼的单伯酯盐,其制备方法和包含它的药物组合物。 本发明进一步提供了制备拉帕替尼二磺酸一水合物形式的方法。 本发明还提供了制备无水形式的拉帕替尼二甲磺酸盐的方法。

    PROCESS FOR CINACALCET HYDROCHLORIDE
    67.
    发明公开
    PROCESS FOR CINACALCET HYDROCHLORIDE 审中-公开
    盐酸西那卡利的方法

    公开(公告)号:EP2593422A1

    公开(公告)日:2013-05-22

    申请号:EP10854669.8

    申请日:2010-07-16

    IPC分类号: C07C211/00

    摘要: 3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride.

    摘要翻译: 3- [3-(三氟甲基)苯基]丙醛是制备盐酸西那卡塞的关键中间体。 本发明提供了制备3- [3-(三氟甲基)苯基]丙醛的新方法。 本发明还提供了高收率制备盐酸西那卡塞的改进方法。 本发明进一步提供了一种纯化盐酸西那卡塞的方法。

    SALTS OF RALTEGRAVIR
    69.
    发明公开
    SALTS OF RALTEGRAVIR 审中-公开
    RALTEGRAVIR盐

    公开(公告)号:EP2575465A1

    公开(公告)日:2013-04-10

    申请号:EP10852079.2

    申请日:2010-05-25

    CPC分类号: C07D413/12 A61K31/513

    摘要: The present invention provides novel salts of raltegravir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides crystalline sodium salt of raltegravir, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of amorphous sodium salt of raltegravir. The present invention further provides a process for the preparation of raltegravir potassium crystalline form H1.

    摘要翻译: 本发明提供了raltegravir的新盐,其制备方法和包含它们的药物组合物。 本发明还提供了拉替拉韦的结晶钠盐,其制备方法和包含它的药物组合物。 本发明进一步提供了制备raltegravir的无定形钠盐的方法。 本发明进一步提供了制备raltegravir钾晶型H1的方法。

    POLYMORPHS OF DARUNAVIR
    70.
    发明公开
    POLYMORPHS OF DARUNAVIR 有权
    DARUNAVIR的多态性

    公开(公告)号:EP2513116A1

    公开(公告)日:2012-10-24

    申请号:EP09852224.6

    申请日:2009-12-16

    IPC分类号: C07D493/04

    摘要: The present invention provides novel solvated forms of darunavir and processes for there preparation. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45°C to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25°C, and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50°C for 12 hours to yield darunavir amorphous form.

    摘要翻译: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了用于制备达芦那韦无定形形式的新方法和包含它的药物组合物。 因此,例如,将地瑞纳韦2-甲基-2-丁醇溶剂合物溶于二氯甲烷中,在45℃下真空蒸馏以获得残余物,向残余物中加入环己烷并在20至25℃下搅拌30小时, 过滤分离的固体,用环己烷洗涤,并在50℃下真空干燥12小时,得到地瑞那韦无定形形式。