Purification Method of Azacyclohexapeptide or Its Salt
    1.
    发明申请
    Purification Method of Azacyclohexapeptide or Its Salt 有权
    氮杂六肽或其盐的纯化方法

    公开(公告)号:US20130030150A1

    公开(公告)日:2013-01-31

    申请号:US13640836

    申请日:2011-04-15

    IPC分类号: C07K1/14 C07K7/64

    摘要: A purification method of the compound represented by formula 1 is provided, which includes the following steps: (1) loading crude compound 1 on macroporous adsorbent resin, (2) washing the macroporous adsorbent resin with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water, (3) eluting with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water. The purified compound represented by formula 1 is obtained.

    摘要翻译: 提供由式1表示的化合物的纯化方法,其包括以下步骤:(1)在大孔吸附树脂上加载粗化合物1,(2)用水溶液,有机溶剂或混合物洗涤大孔吸附树脂 有机溶剂和水的溶液,(3)用水溶液,有机溶剂或有机溶剂和水的混合溶液洗脱。 得到由式1表示的纯化化合物。

    Lubiprostone crystal, the use and the method for the preparation thereof
    2.
    发明授权
    Lubiprostone crystal, the use and the method for the preparation thereof 有权
    卢比石晶,其制备方法及用途

    公开(公告)号:US08748482B2

    公开(公告)日:2014-06-10

    申请号:US12935859

    申请日:2008-05-15

    IPC分类号: A61K31/352 C07D311/96

    摘要: The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2θ reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.

    摘要翻译: 本发明涉及一种利比膦石晶体及其制备方法,以及包含该组合物或试剂盒的药物组合物或试剂盒,以及所述晶体在制备用于治疗胃肠道疾病,特别是便秘的药物中的用途 。 所述晶体的X射线粉末衍射图包括在以下2θ测量的特征峰; 反射角:14.6±0.2°,17.0±0.2°和19.6±0.2°。 与无定形罗哌隆相比,本发明的晶体具有相对高的纯度,稳定的性质和易于储存和使用的优点。

    PROCESS FOR PURIFYING CYCLOLIPOPEPTIDE COMPOUNDS OR THE SALTS THEREOF
    3.
    发明申请
    PROCESS FOR PURIFYING CYCLOLIPOPEPTIDE COMPOUNDS OR THE SALTS THEREOF 有权
    净化环磷脂化合物或其盐的方法

    公开(公告)号:US20130281665A1

    公开(公告)日:2013-10-24

    申请号:US13877427

    申请日:2011-09-27

    IPC分类号: C07K1/22

    CPC分类号: C07K1/22 C07K7/56

    摘要: A process for purifying cyclic lipopeptide compounds or salts thereof comprising the steps of: (1) charging a crude compound of Formula I onto a macroporous adsorption resin; (2) washing the macroporous adsorption resin using water, an organic solvent or a mixed solution of an organic solvent and water as a washing liquid; and (3) eluting the compound of Formula I from the macroporous adsorption resin using water, an organic solvent or a mixed solution of an organic solvent and water as an eluent. The purification method has the advantages of using a small amount of organic solvents, using no silica gel, and causing little damage to the environment; the purity of the collected compound of formula I is also improved as compared with the methods previously disclosed.

    摘要翻译: 一种用于纯化环状脂肽化合物或其盐的方法,包括以下步骤:(1)将式I的粗制化合物装入大孔吸附树脂中; (2)使用水,有机溶剂或有机溶剂和水的混合溶液作为洗涤液洗涤大孔吸附树脂; 和(3)使用水,有机溶剂或有机溶剂和水的混合溶液作为洗脱剂,从大孔吸附树脂中洗脱式I化合物。 净化方法的优点是使用少量的有机溶剂,不使用硅胶,对环境几乎没有损害; 与以前公开的方法相比,所收集的式I化合物的纯度也得到改善。

    LUBIPROSTONE CRYSTAL, THE USE AND THE METHOD FOR THE PREPARATION THEREOF
    4.
    发明申请
    LUBIPROSTONE CRYSTAL, THE USE AND THE METHOD FOR THE PREPARATION THEREOF 有权
    LUBIPROSTONE水晶,其使用及其制备方法

    公开(公告)号:US20110028541A1

    公开(公告)日:2011-02-03

    申请号:US12935859

    申请日:2008-05-15

    摘要: The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2θ reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.

    摘要翻译: 本发明涉及一种利比膦石晶体及其制备方法,以及包含该组合物或试剂盒的药物组合物或试剂盒,以及所述晶体在制备用于治疗胃肠道疾病,特别是便秘的药物中的用途 。 所述晶体的X射线粉末衍射图包括在以下2θ测量的特征峰; 反射角:14.6±0.2°,17.0±0.2°和19.6±0.2°。 与无定形罗哌隆相比,本发明的晶体具有相对高的纯度,稳定的性质和易于储存和使用的优点。

    PROCESS FOR PURIFYING CYCLOLIPOPEPTIDE COMPOUNDS OR THE SALTS THEREOF
    6.
    发明申请
    PROCESS FOR PURIFYING CYCLOLIPOPEPTIDE COMPOUNDS OR THE SALTS THEREOF 有权
    净化环磷脂化合物或其盐的方法

    公开(公告)号:US20130296529A1

    公开(公告)日:2013-11-07

    申请号:US13877141

    申请日:2011-09-27

    IPC分类号: C07K7/56

    CPC分类号: C07K7/56

    摘要: A method for purifying a cyclic lipopepteide or a salt thereof is provided. The method comprises the steps: (1) extracting a fermentation broth containing a compound of formula I or a salt thereof, to obtain an extract 1 after filtration or centrifugation; (2) diluting or concentrating the extract 1 under vacuum to decrease the content of the organic solvent, to obtain an extract 2; (3) loading the extract 2 onto a macroporous absorption resin; (4) washing the macroporpous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution; and (5) eluting the compound of formula I off from the macroporous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution as an eluant. Compared with the prior art, the purification method has the advantages that fewer organic solvent is used, no silica gel is used, the harm to the environment is less, and the purity of the collected compound of formula I is improved.

    摘要翻译: 提供了一种纯化环磷脂或其盐的方法。 该方法包括以下步骤:(1)提取含有式I化合物或其盐的发酵液,过滤或离心后得到提取物1; (2)真空稀释或浓缩提取物1以降低有机溶剂的含量,得到提取物2; (3)将提取物2装载到大孔吸附树脂上; (4)用水,有机溶剂或水和有机溶剂的混合物洗涤大孔吸附树脂作为洗涤溶液; 和(5)用水,有机溶剂或水和有机溶剂的混合物作为洗脱液从大孔吸附树脂中除去式I化合物作为洗脱剂。 与现有技术相比,纯化方法的优点是使用少量有机溶剂,不使用硅胶,对环境的危害较小,提取了所收集的式I化合物的纯度。

    Process for purifying cyclolipopeptide compounds or the salts thereof
    10.
    发明授权
    Process for purifying cyclolipopeptide compounds or the salts thereof 有权
    环肽肽化合物或其盐的纯化方法

    公开(公告)号:US08877777B2

    公开(公告)日:2014-11-04

    申请号:US13877141

    申请日:2011-09-27

    CPC分类号: C07K7/56

    摘要: A method for purifying a cyclic lipopeptide or a salt thereof is provided. The method comprises the steps: (1) extracting a fermentation broth containing a compound of formula I or a salt thereof, to obtain an extract 1 after filtration or centrifugation; (2) diluting or concentrating the extract 1 under vacuum to decrease the content of the organic solvent, to obtain an extract 2; (3) loading the extract 2 onto a macroporous absorption resin; (4) washing the macroporous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution; and (5) eluting the compound of formula I off from the macroporous adsorption resin with water, an organic solvent, or a mixture of water and an organic solvent as a washing solution as an eluant. Compared with the prior art, the purification method has the advantages that fewer organic solvent is used, no silica gel is used, the harm to the environment is less, and the purity of the collected compound of formula I is improved.

    摘要翻译: 提供了一种纯化环状肽或其盐的方法。 该方法包括以下步骤:(1)提取含有式I化合物或其盐的发酵液,过滤或离心后得到提取物1; (2)真空稀释或浓缩提取物1以降低有机溶剂的含量,得到提取物2; (3)将提取物2装载到大孔吸附树脂上; (4)用水,有机溶剂或水和有机溶剂的混合物洗涤大孔吸附树脂作为洗涤液; 和(5)用水,有机溶剂或水和有机溶剂的混合物作为洗脱液从大孔吸附树脂中除去式I化合物作为洗脱剂。 与现有技术相比,纯化方法的优点是使用少量有机溶剂,不使用硅胶,对环境的危害较小,提取了所收集的式I化合物的纯度。