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    CRYSTAL FORM VII OF AGOMELATINE, PREPARATION METHOD AND USE THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    3.
    发明申请
    CRYSTAL FORM VII OF AGOMELATINE, PREPARATION METHOD AND USE THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 有权
    聚酰胺的晶体形式VII，其制备方法及其用途及含有其的药物组合物

    公开(公告)号：US20140011883A1

    公开(公告)日：2014-01-09

    申请号：US14006468

    申请日：2012-03-22

    申请人： Yu Huang ,  Ling Tong ,  Xueyan Zhu ,  Hanbin Shan ,  Zhedong Yuan ,  Xiong Yu

    发明人： Yu Huang ,  Ling Tong ,  Xueyan Zhu ,  Hanbin Shan ,  Zhedong Yuan ,  Xiong Yu

    IPC分类号： C07C233/22 ,  C07C231/24

    CPC分类号： C07C233/22 ,  A61K9/4866 ,  C07C231/24 ,  C07C233/18

    摘要： The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.

    摘要翻译： 本发明提供了一种新的结晶形式的阿莫西坦结晶形式VII，其制备方法，应用和药物组合物。 这种新的结晶形式提供高纯度，稳定的晶体结构和良好的再现性，而其生产方法适合大规模生产。 在稳定性和纯度方面，它优于迄今报道的许多结晶形式。 结果，本发明的结晶形式VII在药物制剂中具有优点。

    Agomelatine hydrobromide hydrate and preparation thereof
    4.
    发明授权
    Agomelatine hydrobromide hydrate and preparation thereof 有权
    氢溴酸阿莫拉坦及其制备方法

    公开(公告)号：US08729132B2

    公开(公告)日：2014-05-20

    申请号：US13635087

    申请日：2011-03-17

    申请人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    发明人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    IPC分类号： A01N37/18 ,  A61K31/16 ,  C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  C07C239/00

    CPC分类号： C07C233/18 ,  A61K31/165

    摘要： The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.

    摘要翻译： 本发明涉及其中X是Br的式I的氢溴酸阿尔美拉酸水合物，其制备和用途以及含有它的药物组合物。 通过本发明方法获得的氢溴酸氢溴酸水合物与阿魏酸相比具有显着增加的溶解度，因此更适用于制备药物制剂。 此外，该产品具有更高的稳定性和纯度。 使用本方法，可以通过简单的工艺获得高纯度的产品，没有任何复杂的步骤。

    Agomelatine hydrochloride hydrate and preparation thereof
    5.
    发明授权
    Agomelatine hydrochloride hydrate and preparation thereof 有权
    盐酸阿维美素水合物及其制备

    公开(公告)号：US08729131B2

    公开(公告)日：2014-05-20

    申请号：US13635063

    申请日：2011-03-17

    申请人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    发明人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    IPC分类号： A01N37/18 ,  A61K31/16 ,  C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  C07C239/00

    CPC分类号： C07C233/18 ,  A61K31/165

    摘要： The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

    摘要翻译： 本发明涉及式I的盐酸阿维生素水合物，其制备和用途以及含有它的药物组合物。 通过本发明方法获得的氢溴酸阿尔美拉坦氢氧化物水合物的溶解度高于阿魏酸，因此更适用于制备药物制剂。 此外，该产品具有更高的稳定性和纯度。 使用本方法，可以通过简单的工艺获得高纯度的产品，没有任何复杂的步骤。 其中X是Cl。

    AGOMELATINE HYDROCHLORIDE HYDRATE AND PREPARATION THEREOF
    7.
    发明申请
    AGOMELATINE HYDROCHLORIDE HYDRATE AND PREPARATION THEREOF 有权
    AGOMELATINE氢氯化物水合物及其制备方法

    公开(公告)号：US20130005820A1

    公开(公告)日：2013-01-03

    申请号：US13635063

    申请日：2011-03-17

    申请人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    发明人： Hanbin Shan ,  Zhedong Yuan ,  Xueyan Zhu ,  Peng Zhang ,  Hongjuan Pan ,  Xiong Yu

    IPC分类号： C07C233/18 ,  A61P25/22 ,  A61P25/24 ,  A61P3/00 ,  A61P9/12 ,  A61P25/18 ,  A61P25/00 ,  A61K31/165 ,  A61P9/00

    CPC分类号： C07C233/18 ,  A61K31/165

    摘要： The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

    摘要翻译： 本发明涉及式I的盐酸阿维生素水合物，其制备和用途以及含有它的药物组合物。 通过本发明方法获得的氢溴酸阿尔美拉坦氢氧化物水合物的溶解度高于阿魏酸，因此更适用于制备药物制剂。 此外，该产品具有更高的稳定性和纯度。 使用本方法，可以通过简单的工艺获得高纯度的产品，没有任何复杂的步骤。 其中X是Cl。

    Agomelatine intermediates and preparation method thereof
    8.
    发明授权
    Agomelatine intermediates and preparation method thereof 有权
    阿莫拉坦中间体及其制备方法

    公开(公告)号：US08779199B2

    公开(公告)日：2014-07-15

    申请号：US13702388

    申请日：2011-06-08

    申请人： Peng Zhang ,  Yu Huang ,  Zhedong Yuan ,  Hanbin Shan ,  Xiong Yu

    发明人： Peng Zhang ,  Yu Huang ,  Zhedong Yuan ,  Hanbin Shan ,  Xiong Yu

    IPC分类号： C07C233/22 ,  C07C231/06 ,  C07C233/18 ,  C07C231/12

    CPC分类号： C07C231/06 ,  C07C231/12 ,  C07C233/18 ,  C07C233/22 ,  C07C2602/10

    摘要： The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine. Said reaction processes are greatly simplified, with the reaction yield being improved and the difficulty in purification of previous method being overcome, as compare with the previous technique for preparation of agomelatine. Typically, the yield of the present invention is over 70%.

    摘要翻译： 本发明涉及用于制备阿格美兰碱的中间体化合物及其制备方法本发明的用于制备agomelatine的中间体是如下式所示的化合物A. 还提供两种新型中间体化合物。 当我们使用这些新的中间体化合物来制备agomelatine时，其操作简单，控制良好，纯度高，无需精馏和柱层析分离等复杂操作，适用于工业生产。 同时，两种新中间体本身的制备方法简单高产，仅使用最常用的7-甲氧基 - 四氢萘酮作为起始原料，经过一步反应得到中间体，再加入一步 将中间体化合物转化成所需的产物agomelatine。 所述反应过程被大大简化，与先前用于制备agMelatine的技术相比，反应产率提高并克服了先前方法的纯化困难。 通常，本发明的产率超过70％。