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公开(公告)号：US20240335387A1
公开(公告)日：2024-10-10
申请号：US18292804
申请日：2021-08-05
发明人： Tengfei Liu , Jialei Fang , Yanan Wang , Laiyi Ni
IPC分类号： A61K9/19 , A61K9/00 , A61K9/16 , A61K31/495
CPC分类号： A61K9/19 , A61K9/0019 , A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K31/495
摘要： Provided are a lyophilized vortioxetine pamoate powder for injection and a preparation method therefor. The prepared powder for injection product has good permeability and stability, and is very suitable for industrialization.
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公开(公告)号：US20230174478A1
公开(公告)日：2023-06-08
申请号：US17922140
申请日：2020-04-30
发明人： Yipeng ZHAN , Haisheng FAN , Kai YIN , Xiang JI , Boyang LIU , Xiaowen GUO , Luning HUANG , Anping TAO , Jianguo AN , Hong GU
IPC分类号： C07D207/27
CPC分类号： C07D207/27
摘要： Disclosed is a method for preparing a brivaracetam intermediate shown in formula B-R, comprising: reacting a compound shown in formula B-P and a resolving agent to prepare a compound shown in formula B-Q; and converting the compound shown in formula B-Q into the brivaracetam intermediate shown in formula B-R, wherein the resolving agent is a (1S,2S)-(+)-1,2-diaminocyclohexane compound. Also provided is a method for preparing brivaracetam. According to the method, a mixture of two diastereoisomers of (S)-2-3-propylpyrrolidine-1-yl butyric acid can be conveniently and effectively resolved, and the use of a chiral HPLC column is avoided, thereby greatly shortening the process time, simplifying the operation, reducing the process cost, and facilitating industrial production and enviormental protection.
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公开(公告)号：US11519890B2
公开(公告)日：2022-12-06
申请号：US17258226
申请日：2018-07-10
发明人： Tan Xiao , Tianpei Huang , Jinsheng Lin , Qiang Zhou , Tong Wu , Danfeng Ye , Hong Cai , Wenquan Zhu , Wenbin Chen , Min Li
摘要： Disclosed is a detection method for N-nitrosodimethylamine (NDMA) impurities, comprising: (1) obtaining a test solution containing a sample to be tested; and (2) detecting the test solution by means of gas chromatography-mass spectrometry to determine the content of an N-nitrosodimethylamine impurity in the sample. The method provided in the present invention has a good separating effect, a wide linear range, a high sensitivity and a good method durability, and can detect the content of N-nitrosodimethylamine (NDMA) in the sample rapidly and effectively.
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公开(公告)号：US20220162189A1
公开(公告)日：2022-05-26
申请号：US17430794
申请日：2020-02-18
发明人： Wenxiang ZHOU , Wenfeng HUANG , Jiaxing HU
IPC分类号： C07D403/06
摘要： Disclosed is a method for preparing voriconazole and an intermediate thereof In the method, a voriconazole condensate isomer is reacted as a starting material in the presence of an acid to obtain 4-chloro-6-ethyl-5-fluoropyrimidine and 2′,4′-difluoro-2-[1-(1H-1,2,4-triazolyl)]acetophenone. A method for preparing voriconazole by using the intermediate thus obtained is further disclosed. By adopting the method of the present invention, the utilization rate of starting materials and auxiliary materials for preparing voriconazole on the basis of the prior art can be greatly improved, thereby reducing costs.
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公开(公告)号：US20210387971A1
公开(公告)日：2021-12-16
申请号：US17291237
申请日：2018-11-06
发明人： Jinsheng LIN , Xiaofei LIU , Dan LI , Jing WANG , Yue LI , Wenquan ZHU , Wenbin CHEN , Min LI
IPC分类号： C07D403/06
摘要： Provided are a pregabalin lactam methylene dimer and a preparation method therefor. The method comprises the following steps: dissolving pregabalin in a reaction solvent, reacting same with an aldehyde in an acidic system and isolating the obtained target product pregabalin lactam methylene dimer. The preparation method for pregabalin lactam methylene dimer provided by the present application has a simple operation, a high product yield, a good purity and a low cost.
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6.发明申请公开(公告)号：US20200306245A1
公开(公告)日：2020-10-01
申请号：US16647847
申请日：2017-09-20
发明人： Jinsheng LIN , Tianpei HUANG , Feifei LAN , Xiaoyan XU , Libin HU , Dan LI , Wenquan ZHU , Min LI , Zhiyun WANG
IPC分类号： A61K31/4965 , A61K47/38
摘要： Disclosed is N-formyl vortioxetine, and also disclosed is a method for preparing the N-formyl vortioxetine and a stable solid preparation of vortioxetine.
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7.发明申请公开(公告)号：US20200270230A1
公开(公告)日：2020-08-27
申请号：US16645777
申请日：2018-09-17
发明人： Xin Xu , Zhen Zhang , Yunfei Li , Liming Zhang , Fengying Guo , Qingyun Jiang , Dongsheng Li , Linli Zhang , Jinqian Song , Lei Liu , Qiang Liu , Jing Su , Yijin Wang , Jian Ge
IPC分类号： C07D405/04 , C07D405/14 , C07D495/04 , C07D417/14
摘要： Disclosed are a class of μ-opioid receptor agonists and a preparation method therefor and the use thereof in the field of medicine, belonging to the field of medicinal chemistry. The μ-opioid receptor agonists significantly increase the selectivity for a G protein signaling pathway, and not only can exhibit excellent pharmacodynamic effects, but also significantly improve safety.
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公开(公告)号：US20200172479A1
公开(公告)日：2020-06-04
申请号：US16638105
申请日：2018-08-09
申请人： Zhejiang Huahai Pharmaceutical Co., Ltd , Zhejiang Huahai TianCheng Pharmaceutical Co., Ltd , Zhejiang Huahai Zhicheng Pharmaceutical Co., Ltd
发明人： Xinlei Chen , Zhicheng Hu , Liang Zheng , Peng Dong
IPC分类号： C07D207/27
摘要： A preparing method for high-purity levetiracetam, comprising: adjusting the pH of an extracted aqueous layer obtained by dissociating (S)-α-ethyl-2-oxo-1-pyrrolidineacetic acid (R)-methylbenzylamine salt to 5-9; removing water; adding an organic solvent to form a solution and then performing an esterification reaction with ethyl chloroformate or methylchlorofonmate; and carrying out an ammonolysis reaction to obtain the levetiracetam. The method simplifies production process, increases yield, reduces or even avoids the use of triethylamine in the esterification process, and reduces the emission of a great amount of three wastes.
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公开(公告)号：US20200165284A1
公开(公告)日：2020-05-28
申请号：US16486985
申请日：2018-02-06
发明人： Gang QIAN , Yanbao ZHOU , Linxiang ZHANG , Wenling ZHANG
IPC分类号： C07H7/06
摘要： Disclosed is a method for preparing a canagliflozin form. The method comprises the following steps: adding canagliflozin into an organic solvent and dissolving same, then distilling into a certain amount of an oil; then, adding an anti-solvent to the oil, stirring same with a precipitated solid, cooling, filtering, and drying to obtain the canagliflozin amorphous form. The preparation method has the characteristics of a low solvent ratio, a high yield, a simple operation, easy recovery, less three wastes and good producibility, with the resulting product having a stable quality, good fluidity, and being suitable for the preparation of formulations, etc., and the preparation process is easy to apply to large commercial production, and has a high value in terms of promotion and application.
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公开(公告)号：US10550109B2
公开(公告)日：2020-02-04
申请号：US16300301
申请日：2017-05-12
发明人： Yinglu Jiao , Handa Li , Boyu Wang , Luning Huang , Xi Chen , Hong Gu
IPC分类号： C07D409/14
摘要： Disclosed are a crystal form of brexpiprazole and a preparation method therefor. The X-ray powder diffraction pattern, which is detected with Cu—Kα radiation, of the crystal form of brexpiprazole has characteristic peaks at the positions where 2θ is about 9.1±0.2, 15.2±0.2, 15.7±0.2, 17.6±0.2, 18.1±0.2, 24.4±0.2. The crystal form I of brexpiprazole has a high purity, good stability and good reproducibility, and is suitable for industrial production.
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