公开(公告)号：US20230270757A1

公开(公告)日：2023-08-31

申请号：US18007020

申请日：2021-07-27

申请人： GNT PHARMA CO., LTD.

发明人： Weiqiang ZHAN ,  Zhanguo WANG ,  Wei ZHANG ,  Lingyan FU ,  Qian LIN ,  Xiaoli CHEN ,  Guoyang LV ,  Liyin ZHONG ,  Xinliang XU ,  Fangmeng ZHU

IPC分类号： A61K31/606 ,  A61K9/19 ,  A61K9/00

CPC分类号： A61K31/606 ,  A61K9/19 ,  A61K9/0019

摘要： A salfaprodil freeze-dried powder injection, and a preparation method thereof and the use thereof are proposed. The preparation method may include adding salfaprodil into water for injection, filtering after the salfaprodil is completely dissolved, and adjusting pH of filtrate with an alkaline substance water solution. The method may also include adding the injection water to achieve a constant volume, filling with an inert gas for protection, and performing sterilization and filtration to obtain a salfaprodil solution, which is then freeze-dried to obtain the -salfaprodil freeze-dried powder injection.

公开(公告)号：US20240116853A1

公开(公告)日：2024-04-11

申请号：US18256350

申请日：2021-12-06

申请人： GNT PHARMA CO., LTD.

发明人： Xinliang XU ,  Guoqing ZHANG ,  Chenghan ZHUANG ,  Lei WANG ,  Byoung Joo GWAG ,  Chun San AHN ,  Jing Yu JIN

IPC分类号： C07C229/64

CPC分类号： C07C229/64 ,  C07B2200/13 ,  C07C2601/16

摘要： 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid crystal forms and a preparation method therefor are proposed. Crystal form I is a monoclinic crystal system, which has a Pc space group and can be obtained by slow cooling, evaporating the solvent at a constant temperature, evaporating the solvent at an increased temperature, or adding an anti-solvent. Crystal form II is a triclinic crystal system, which has a P1 space group and can be obtained by rapid cooling or freeze-drying. According to the method, the process is simple, costs are low, and the yield exceeds 90%; and the crystal forms of the crystal forms I and II have high purity, the crystal shapes thereof are intact, and have excellent fluidity, facilitating preparation, particularly the preparation of a pharmaceutical preparation for preventing and/or treating degenerative diseases of the central nervous system. Furthermore, the two crystal forms have a better apparent solubility than that of raw materials.

公开(公告)号：US20240051915A1

公开(公告)日：2024-02-15

申请号：US18256308

申请日：2021-12-06

申请人： GNT PHARMA CO., LTD.

发明人： Xinliang XU ,  Chenghan ZHUANG ,  Lei WANG ,  Xin LU ,  Bo ZHANG ,  Byoung Joo GWAG ,  Chun San AHN ,  Jing Yu JIN

IPC分类号： C07C227/18 ,  C07C303/28

CPC分类号： C07C227/18 ,  C07C303/28

摘要： A method for preparing 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid is proposed. The method may include protection, condensation, and hydrolysis. By means of the screening of a hydroxyl protecting reagent for a starting material, for example, 2-(4-trifluoromethyl)phenethylalcohol and the optimization of other process parameters, the contents of meta-isomer impurities and disubstituted impurities in a target product are effectively controlled. Accordingly, the quality of the product is significantly improved, the reaction yield is also greatly improved, and the improved product quality can satisfy related requirements of preparation research.