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1. 发明申请

US20110313198A1 AGOMELATINE HYDROHALIDE COMPLEX AND PREPARATION METHOD THEREOF 有权
标题翻译： AGOMELATINE HYDROHALIDE COMPLEX及其制备方法
公开(公告)号：US20110313198A1
公开(公告)日：2011-12-22
申请号：US13138511
申请日：2010-02-26
申请人： Peng Zhang , Hanbin Shan , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
发明人： Peng Zhang , Hanbin Shan , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
IPC分类号： C07C233/22
CPC分类号： C07C233/18
摘要： The present invention relates to a complex of agomelatine and to preparation thereof. The hydrogen halide complex of agomelatine obtained through the present method is more soluble, more stable, and of higher purity than agomelatine itself, making it more suitable to be used in pharmaceutical preparation. Using this method, product of high purity can be obtained through a simple process, without having to incur further complicated steps.
摘要翻译：本发明涉及一种阿维菌素及其制备方法。通过本发明方法获得的agomelatine的卤化氢配合物比agomelatine本身更可溶，更稳定和更高纯度，使其更适合用于制药。使用这种方法，可以通过简单的工艺获得高纯度的产品，而不必进一步复杂的步骤。

2. 发明授权

US08524949B2 Agomelatine hydrohalide complex and preparation method thereof 有权
标题翻译：阿莫拉坦氢卤化物络合物及其制备方法
公开(公告)号：US08524949B2
公开(公告)日：2013-09-03
申请号：US13138511
申请日：2010-02-26
申请人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
发明人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Hongjuan Pan , Xiong Yu
IPC分类号： C07C233/05
CPC分类号： C07C233/18
摘要： The present invention relates to a complex of agomelatine and to preparation thereof. The hydrogen halide complex of agomelatine obtained through the present method is more soluble, more stable, and of higher purity than agomelatine itself, making it more suitable to be used in pharmaceutical preparation. Using this method, product of high purity can be obtained through a simple process, without having to incur further complicated steps.
摘要翻译：本发明涉及一种阿维菌素及其制备方法。通过本发明方法获得的agomelatine的卤化氢配合物比agomelatine本身更可溶，更稳定和更高纯度，使其更适合用于制药。使用这种方法，可以通过简单的工艺获得高纯度的产品，而不必进一步复杂的步骤。

3. 发明授权

US08614251B2 Crystalline form VI of agomelatine, preparation method and application thereof 有权
标题翻译：琼脂糖的结晶形式VI，其制备方法和应用
公开(公告)号：US08614251B2
公开(公告)日：2013-12-24
申请号：US13138615
申请日：2010-03-09
申请人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
发明人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
IPC分类号： A01N37/18 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： A61K31/165 , C07C233/18
摘要： The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2θ 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
摘要翻译：本发明提供了一种新的结晶形式的agomelatine，其制备和用途。阿魏酸晶体形式的X射线粉末衍射图在衍射角2θ11.13°，11.82°，17.49°，18.29°，19.48°，19.72°，20.50°，21.76°，22.54°，22.97°处显示主峰， 24.56°，25.36°，27.16°和31.93°。所述新的结晶形式的特征在于高纯度，稳定性和良好的再现性，因此对于药物制剂是有利的。此外，所述结晶形式的稳定性和溶解度也优于几种现有的结晶形式。

4. 发明申请

US20120004313A1 CRYSTALLINE FORM VI OF AGOMELATINE, PREPARATION METHOD AND APPLICATION THEREOF 有权
标题翻译：聚酰胺的结晶形式VI，其制备方法和应用
公开(公告)号：US20120004313A1
公开(公告)日：2012-01-05
申请号：US13138615
申请日：2010-03-09
申请人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
发明人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
IPC分类号： A61K31/165 , C07C231/00 , A61P25/00 , A61P1/00 , A61P25/24 , A61P25/18 , A61P9/00 , C07C233/29 , A61P25/22
CPC分类号： A61K31/165 , C07C233/18
摘要： The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2θ 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
摘要翻译：本发明提供了一种新的结晶形式的agomelatine，其制备和用途。阿格美拉汀晶型的X射线粉末衍射图显示了衍射角2θ处的主峰; 11.13°，11.82°，17.49°，18.29°，19.48°，19.72°，20.50°，21.76°，22.54°，22.97°，24.56°，25.36°，27.16°和31.93°。所述新的结晶形式的特征在于高纯度，稳定性和良好的再现性，因此对于药物制剂是有利的。此外，所述结晶形式的稳定性和溶解度也优于几种现有的结晶形式。

5. 发明授权

US08779199B2 Agomelatine intermediates and preparation method thereof 有权
标题翻译：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％。

6. 发明申请

US20130267738A1 AGOMELATINE INTERMEDIATES AND PREPARATION METHOD THEREOF 有权
标题翻译： AGOMELATINE中间体及其制备方法
公开(公告)号：US20130267738A1
公开(公告)日：2013-10-10
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： C07C231/06 , C07C233/22
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agomelatine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％。

7. 发明授权

US08729132B2 Agomelatine hydrobromide hydrate and preparation thereof 有权
标题翻译：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。

8. 发明授权

US09527803B2 Crystal form VII of agomelatine, preparation method and use thereof and pharmaceutical composition containing same 有权
标题翻译：琼脂糖凝胶晶形VII，其制备方法和用途以及含有它们的药物组合物
公开(公告)号：US09527803B2
公开(公告)日：2016-12-27
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： C07C231/24 , C07C233/22 , A61K9/48
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势。

9. 发明授权

US09434760B2 Prolinamide derivatives as thrombin inhibitors, preparation method and application thereof 有权
标题翻译：脯氨酰胺衍生物作为凝血酶抑制剂，其制备方法和应用
公开(公告)号：US09434760B2
公开(公告)日：2016-09-06
申请号：US13884196
申请日：2011-11-04
申请人： Min Li , Hanbin Shan , Yu Huang , Zhedong Yuan , Xiong Yu
发明人： Min Li , Hanbin Shan , Yu Huang , Zhedong Yuan , Xiong Yu
IPC分类号： A61K38/06 , C07K5/02 , C07D207/16 , C07D205/04 , C07D211/60 , A61K47/12 , A61K47/38 , A61K9/20 , A61K9/48
CPC分类号： C07K5/0215 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K38/06 , A61K47/12 , A61K47/38 , C07D205/04 , C07D207/16 , C07D211/60
摘要： Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
摘要翻译：提供式（I）的化合物，其药学上可接受的盐，其用于抑制凝血酶的制备方法和应用，以及在治疗和预防凝血酶介导的凝血酶相关疾病中的应用。

10. 发明授权

US08729131B2 Agomelatine hydrochloride hydrate and preparation thereof 有权
标题翻译：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。

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