PROCESS FOR THE PREPARTION OF OLANZAPINE
    8.
    发明申请
    PROCESS FOR THE PREPARTION OF OLANZAPINE 失效
    制备奥兰波星的方法

    公开(公告)号:US20090137563A1

    公开(公告)日:2009-05-28

    申请号:US12093344

    申请日:2006-11-10

    CPC分类号: C07D495/04

    摘要: The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.

    摘要翻译: 本发明涉及制备式(2-甲基-4-(4-甲基哌嗪-1-基)-10H-噻吩并[2,3-b] [1,5]苯并二氮杂(奥氮平) I)通过在有机溶剂中将式(II)的4-氨基-2-甲基-10H-噻吩并[2,3-b] [1/5]苯并二氮杂盐酸盐与N-甲基哌嗪反应,其包括进行反应 在甲苯和1,3-二甲基-2-咪唑烷酮的混合物中。 本发明还包括式(IB)的新的2-甲基-4-(4-甲基哌嗪-1-基)-10H-噻吩并[2,3-b] [1,5]苯并二氮杂三水合物,其制备方法和 包含所述新化合物的药物组合物。

    INORGANIC SALT COMPLEXES OF VILDAGLIPTIN
    9.
    发明申请
    INORGANIC SALT COMPLEXES OF VILDAGLIPTIN 有权
    维拉胶的无机盐复合物

    公开(公告)号:US20130005790A1

    公开(公告)日:2013-01-03

    申请号:US13500356

    申请日:2010-10-07

    IPC分类号: C07D207/16 A61P3/10 A61K31/40

    CPC分类号: C07D207/16

    摘要: The present invention relates to the use of novel vildagliptin complexes for the manufacture of high purity vildagliptin of Formula I and/or pharmaceutical acceptable salts thereof. Further objects of the present invention are pharmaceutically acceptable complexes of vildagliptin and/or amorphous and crystalline forms, anhydrous forms, amorphous and crystalline hydrates, amorphous and crystalline solvates of the complexes and a process for the preparation thereof. Another object of the present invention is the high purity vildagliptin and pharmaceutically acceptable salts thereof prepared form the vildagliptin complexes of the present invention, a process for the preparation thereof and pharmaceutical compositions containing vildagliptin base, pharmaceutically acceptable salts and/or complexes and use thereof for the treatment of type 2 diabetes (NIDDM). The present invention provides pharmaceutically advantageous high purity vildagliptin complexes.

    摘要翻译: 本发明涉及新型维格列汀复合物用于制备式I的高纯度维格列汀和/或其药学上可接受的盐。 本发明的另外的目的是维格列汀和/或无定形和结晶形式,无水形式,无定形和结晶水合物,络合物的无定形和结晶溶剂合物的药学上可接受的复合物及其制备方法。 本发明的另一个目的是从本发明的维格列汀复合物制备的高纯度维格列汀及其药学上可接受的盐,其制备方法和含有维格列汀碱,药学上可接受的盐和/或配合物的药物组合物及其用途 治疗2型糖尿病(NIDDM)。 本发明提供药学上有利的高纯度维格列汀复合物。