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：US20130331312A1

公开(公告)日：2013-12-12

申请号：US13982872

申请日：2012-01-31

申请人： Yunhai Hong ,  Ying Xue ,  Xiaoming Ji

发明人： Yunhai Hong ,  Ying Xue ,  Xiaoming Ji

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/26

摘要： The present invention provides a medicinal composition containing micafungin or a pharmaceutically acceptable salt thereof and trehalose as a stabilizing agent.

摘要翻译： 本发明提供含有微风孔蛋白或其药学上可接受的盐和海藻糖作为稳定剂的药用组合物。

公开(公告)号：US20130296529A1

公开(公告)日：2013-11-07

申请号：US13877141

申请日：2011-09-27

申请人： Zhaoli Zhang ,  Shidong Liu ,  Zhonghao Zhuo ,  Xiaoming Ji

发明人： Zhaoli Zhang ,  Shidong Liu ,  Zhonghao Zhuo ,  Xiaoming Ji

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。

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：US20130190404A1

公开(公告)日：2013-07-25

申请号：US13811200

申请日：2011-07-20

申请人： Ming Li ,  Zhijun Tang ,  Xiaoming Ji ,  Xiaoliang Gao

发明人： Ming Li ,  Zhijun Tang ,  Xiaoming Ji ,  Xiaoliang Gao

IPC分类号： C07C59/46 ,  C07C215/10

CPC分类号： C07C59/46 ,  A61K31/5575 ,  C07B2200/13 ,  C07C215/10 ,  C07C405/00

摘要： Disclosed is a crystal of carboprost tromethamine as represented by Formula (I). The crystal has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 6.6±0.2°, 9.9±0.2°, 18.5±0.2° and 20.1±0.2°. Furthermore, also disclosed are preparation method and the use of the crystal.

摘要翻译： 公开了由式（I）表示的碳前列素氨基甲酸盐的晶体。 该晶体在以下2θ角度的X射线衍射图中具有特征峰：6.6±0.2°，9.9±0.2°，18.5±0.2°和20.1±0.2°。 此外，还公开了制备方法和使用晶体。

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：US08981048B2

公开(公告)日：2015-03-17

申请号：US13884775

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 a preparation method and applications thereof. The caspofungin analog has a structure as represented in Formula 3.

摘要翻译： 公开了卡泊芬净类似物及其制备方法和应用。 卡泊芬净类似物具有式3所示的结构。

公开(公告)号：US08912309B2

公开(公告)日：2014-12-16

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： C07K1/113 ,  C07K7/56 ,  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：US20140114049A1

公开(公告)日：2014-04-24

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： C07K1/14

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：US20140057320A1

公开(公告)日：2014-02-27

申请号：US13982797

申请日：2012-01-31

申请人： Shidong Liu ,  Zhaoli Zhang ,  Yi Chen ,  Xiusheng Wang ,  Liangliang Zhou ,  Xiaoming Ji

发明人： Shidong Liu ,  Zhaoli Zhang ,  Yi Chen ,  Xiusheng Wang ,  Liangliang Zhou ,  Xiaoming Ji

IPC分类号： C07K7/54

CPC分类号： C07K7/54 ,  C07K7/56 ,  C12N1/14 ,  C12P7/64 ,  C12R1/645

摘要： Provided is a method for preparing a compound represented by Formula I or a salt thereof, wherein Coleophoma empetri F-11899 (FERM BP2635) and/or a mutant strain thereof is cultured in a medium containing amino acid or a salt thereof, an insoluble organic source, and a sugar alcohol, to produce the compound of Formula I or a salt thereof.

摘要翻译： 本发明提供了制备式I化合物或其盐的方法，其中，在含有氨基酸或其盐的培养基中培养含有绒毛母细胞F-11899（FERM BP2635）和/或其突变株的不溶性有机物 来源和糖醇，以制备式I化合物或其盐。