公开(公告)号：US20120270946A1

公开(公告)日：2012-10-25

申请号：US13505360

申请日：2010-07-30

申请人： Bingming He ,  Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Xiaoliang Gao ,  Xiaoming Ji

发明人： Bingming He ,  Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Xiaoliang Gao ,  Xiaoming Ji

IPC分类号： C07C233/17 ,  A61P27/02 ,  A61K31/165

CPC分类号： C07C405/00 ,  C07B2200/13 ,  C07C2601/08

摘要： The crystalline form A of Bimatoprost of formula I, its preparation method and use are provided. There are characteristic peaks where diffraction angles 2θ are 3.2+0.2°, 5.5+0.2°, 11.4+0.2°, 16.7+0.2°, 17.6+0.2°, 19.9+0.2°, 20.8±02° and 22.8+0.2° in the X-ray powder diffraction pattern of the crystalline form A.

摘要翻译： 提供了式I的比马前列素的结晶形式A及其制备方法和用途。 有特征峰，衍射角2＆ 在X射线粉末衍射图中，为3.2±0.2°，5.5±0.2°，11.4±0.2°，16.7±0.2°，17.6±0.2°，19.9±0.2°，20.8±02°和22.8±0.2° 结晶形式A.

公开(公告)号：US08664275B2

公开(公告)日：2014-03-04

申请号：US13505360

申请日：2010-07-30

申请人： Bingming He ,  Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Xiaoliang Gao ,  Xiaoming Ji

发明人： Bingming He ,  Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Xiaoliang Gao ,  Xiaoming Ji

IPC分类号： A61K31/165 ,  C07C235/34

CPC分类号： C07C405/00 ,  C07B2200/13 ,  C07C2601/08

摘要： The crystalline form A of Bimatoprost of formula I, its preparation method and use are provided. There are characteristic peaks where diffraction angles 2θ are 3.2±0.2°, 5.5±0.2°, 11.4±0.2°, 16.7±0.2°, 17.6±0.2°, 19.9±0.2°, 20.8±02° and 22.8±0.2° in the X-ray powder diffraction pattern of the crystalline form A.

摘要翻译： 提供了式I的比马前列素的结晶形式A及其制备方法和用途。 有衍射角2θ为3.2±0.2°，5.5±0.2°，11.4±0.2°，16.7±0.2°，17.6±0.2°，19.9±0.2°，20.8±02°和22.8±0.2°的特征峰 晶型A的X射线粉末衍射图

公开(公告)号：US08748482B2

公开(公告)日：2014-06-10

申请号：US12935859

申请日：2008-05-15

申请人： Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Bingming He ,  Huichun Yang ,  Jushang Zheng

发明人： Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Bingming He ,  Huichun Yang ,  Jushang Zheng

IPC分类号： A61K31/352 ,  C07D311/96

CPC分类号： C07D311/94 ,  C07C51/00 ,  C07C405/0025

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。

公开(公告)号：US20110028541A1

公开(公告)日：2011-02-03

申请号：US12935859

申请日：2008-05-15

申请人： Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Bingming He ,  Huichun Yang ,  Jushang Zheng

发明人： Zhijun Tang ,  Zhonghao Zhuo ,  Yunman Zheng ,  Bingming He ,  Huichun Yang ,  Jushang Zheng

IPC分类号： A61K31/352 ,  C07D311/94 ,  A61P1/00

CPC分类号： C07D311/94 ,  C07C51/00 ,  C07C405/0025

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。

公开(公告)号：US20140128315A1

公开(公告)日：2014-05-08

申请号：US14113296

申请日：2012-04-20

申请人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

发明人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： A61K38/12 ,  A61K31/19

CPC分类号： A61K38/12 ,  A61K31/19 ,  A61K38/005 ,  C07K7/54 ,  C07K7/56

摘要： Disclosed are a high purity of caspofungin or salts thereof, and a preparation method thereof, and use thereof. Disclosed are a caspofungin or salts thereof with low solvent residue and hyposaline, and a preparation process comprising: dissolving a crude product of caspofungin or slats thereof into a system of water and acetic acid, them mixing with a first organic solvent ethyl alcohol, subsequently mixing with a second organic solvent ethyl acetate, then being subject to filtration and drying together with water, to obtain caspofungin or salts thereof with high stability, low solvent residue and hyposaline.

摘要翻译： 公开了高纯度的卡泊芬净或其盐，及其制备方法及其用途。 公开了具有低溶剂残留和次高效的卡泊芬净或其盐，以及制备方法，包括：将卡泊芬净或其盐的粗产物溶解在水和乙酸的体系中，将其与第一有机溶剂乙醇混合，随后混合 用第二有机溶剂乙酸乙酯，然后与水一起过滤和干燥，得到高稳定性，低溶剂残留和次高效的卡泊芬净或其盐。

公开(公告)号：US08969513B2

公开(公告)日：2015-03-03

申请号：US13884750

申请日：2011-11-10

申请人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

发明人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： C07K7/56 ,  A61K38/12 ,  A61K38/00

CPC分类号： C07K7/56 ,  A61K38/00 ,  A61K38/12

摘要： Disclosed are a caspofungin analog and applications thereof. The caspofungin analog is a compound having a structure as indicated in Formula (4), or pharmaceutically acceptable salts thereof. R1 can be chosen from hydroxyl, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy. R2, R3, R4, R5 can be chosen from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine. Also disclosed are a preparation method for and applications of the compound.

摘要翻译： 公开了卡泊芬净类似物及其应用。 卡泊芬净类似物是具有式（4）所示结构的化合物或其药学上可接受的盐。 R 1可以选自羟基，苄氧基，苯氧基，取代的苯氧基或取代的苄氧基。 R2，R3，R4，R5可以选自氢，C1-C6烷基，C1-C6烷氧基，羟基，苄氧基苯基，取代的苄氧基苯基，硝基，氟，氯，溴或碘。 还公开了该化合物的制备方法和应用。

公开(公告)号：US20130231457A1

公开(公告)日：2013-09-05

申请号：US13884686

申请日：2011-11-10

申请人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

发明人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： C07K7/64

CPC分类号： C07K7/64 ,  C07K7/56

摘要： Disclosed is a preparation method for caspofungin, comprising the steps: (a) a compound as represented in Formula 2 and a strong leaving group 5 are mixed to obtain a compound as represented in Formula 3; (b) the compound as represented in Formula 3 and ethylenediamine are mixed to obtain a compound as represented in Formula 4; and, (c) the compound as represented in Formula 4 is mixed with a hydroxyl protection agent, and then a borane complex is mixed in to obtain a compound as represented in Formula 1.

摘要翻译： 公开了卡泊芬净的制备方法，其包括以下步骤：（a）如式2所示的化合物和强离去基团5混合，得到式3所示的化合物; （b）将式3所示的化合物和乙二胺混合，得到式4所示的化合物; 和（c）将式4中所示的化合物与羟基保护剂混合，然后混合硼烷络合物，得到式1所示的化合物。

公开(公告)号：US09115177B2

公开(公告)日：2015-08-25

申请号：US14116947

申请日：2012-05-11

申请人： Guangjun Jiao ,  Shidong Liu ,  Bingming He ,  Zhijun Tang ,  Xiaoming Ji

发明人： Guangjun Jiao ,  Shidong Liu ,  Bingming He ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： C07K1/113 ,  C07K7/56 ,  C07K1/14 ,  C07D413/12

CPC分类号： C07K1/14 ,  C07D413/12 ,  C07K1/113 ,  C07K7/56

摘要： The method of the preparation of micafungin sodium comprises the step of mixing the weak base and the aqueous solution containing micafungin acid (the structure is illustrated by formula I) or the mixed aqueous solution containing the compound of formula I and organic solvent in order to obtain the sodium salt of micafungin (the structure is illustrated by formula II).

摘要翻译： 咪达能素钠的制备方法包括将弱碱与含有米怕酸的水溶液（式I所示的结构）或含有式I化合物和有机溶剂的混合水溶液混合的步骤，以获得 米卡芬净的钠盐（结构由式II表示）。

公开(公告)号：US09446091B2

公开(公告)日：2016-09-20

申请号：US14113296

申请日：2012-04-20

申请人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

发明人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： C07K7/56 ,  A61K38/12 ,  A61K38/00 ,  C07K7/54 ,  A61K31/19

CPC分类号： A61K38/12 ,  A61K31/19 ,  A61K38/005 ,  C07K7/54 ,  C07K7/56

摘要： Disclosed are a high purity of caspofungin or salts thereof, and a preparation method thereof, and use thereof. Disclosed are a caspofungin or salts thereof with low solvent residue and hyposaline, and a preparation process comprising: dissolving a crude product of caspofungin or salts thereof into a system of water and acetic acid, then mixing with a first organic solvent ethyl alcohol, subsequently mixing with a second organic solvent ethyl acetate, then being subject to filtration and drying together with water, to obtain caspofungin or salts thereof with high stability, low solvent residue and hyposaline.

摘要翻译： 公开了高纯度的卡泊芬净或其盐，及其制备方法及其用途。 公开了具有低溶剂残留和次高效的卡泊芬净或其盐，以及制备方法，包括：将卡泊芬净或其盐的粗产物溶解在水和乙酸的体系中，然后与第一有机溶剂乙醇混合，随后混合 用第二有机溶剂乙酸乙酯，然后与水一起过滤和干燥，得到高稳定性，低溶剂残留和次高效的卡泊芬净或其盐。

公开(公告)号：US20130296229A1

公开(公告)日：2013-11-07

申请号：US13884750

申请日：2011-11-10

申请人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

发明人： Bingming He ,  Ming Li ,  Zhijun Tang ,  Xiaoming Ji

IPC分类号： C07K7/56

CPC分类号： C07K7/56 ,  A61K38/00 ,  A61K38/12

摘要： Disclosed are a caspofungin analog and applications thereof. Said caspofungin analog is a compound having a structure as indicated in Formula (4), or pharmaceutically acceptable slats thereof. R1 can be chosen from hydroxyl, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy. R2, R3, R4, R5 can be chosen from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine. Also disclosed are a preparation method for and applications of said compound.

摘要翻译： 公开了卡泊芬净类似物及其应用。 所述卡泊芬净类似物是具有式（4）所示结构的化合物或其药学上可接受的盐条。 R 1可以选自羟基，苄氧基，苯氧基，取代的苯氧基或取代的苄氧基。 R2，R3，R4，R5可以选自氢，C1-C6烷基，C1-C6烷氧基，羟基，苄氧基苯基，取代的苄氧基苯基，硝基，氟，氯，溴或碘。 还公开了所述化合物的制备方法和应用。