Patents Assigned to Zhejiang Huahai Pharmaceutical Co., Ltd.
  • Patent number: 11845710
    Abstract: The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: December 19, 2023
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD, SHANGHAI AOBO PHARMTECH, INC., LTD.
    Inventors: Chen Liu, Xing Li, Huaxiang Ye, Jicheng Zhang, Luning Huang, Anping Tao, Jianguo An, Hong Gu
  • Patent number: 11801239
    Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals having an average particle size of 2-52 ?m.
    Type: Grant
    Filed: November 10, 2021
    Date of Patent: October 31, 2023
    Assignees: Shanghai Synergy Pharmaceutical Sciences Co., Ltd., Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventors: Jian Ge, Yunfei Li, Lihong Lin, Dengxue Sun, Jiamiao Wang, Yijin Wang, Zhiyun Wang
  • Patent number: 11707461
    Abstract: Disclosed is N-formyl vortioxetine, and also disclosed is a method for preparing the N-formyl vortioxetine and a stable solid preparation of vortioxetine.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: July 25, 2023
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
    Inventors: Jinsheng Lin, Tianpei Huang, Feifei Lan, Xiaoyan Xu, Libin Hu, Dan Li, Wenquan Zhu, Min Li, Zhiyun Wang
  • Patent number: 11519890
    Abstract: 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.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: December 6, 2022
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
    Inventors: Tan Xiao, Tianpei Huang, Jinsheng Lin, Qiang Zhou, Tong Wu, Danfeng Ye, Hong Cai, Wenquan Zhu, Wenbin Chen, Min Li
  • Patent number: 11498897
    Abstract: A preparing method for high-purity levetiracetam, comprising: adjusting the pH of an extracted aqueous layer obtained by dissociating (S)-?-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.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: November 15, 2022
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Zhejiang Huahai Tiancheng Pharmaceutical Co., Ltd., Zhejiang Huahai Zhicheng Pharmaceutical Co., Ltd.
    Inventors: Xinlei Chen, Zhicheng Hu, Liang Zheng, Peng Dong
  • Patent number: 11434210
    Abstract: A method for synthesizing valsartan, comprising the steps of: synthesizing a valsartan methyl ester intermediate to obtain a reaction mixture of the valsartan methyl ester intermediate; diluting the reaction mixture by salt water or water, and then using a first extraction solvent to extract the valsartan methyl ester intermediate; adding alkali to an organic layer containing the valsartan methyl ester intermediate for hydrolyzing, removing the organic layer, regulating pH of a water layer to be acidic by using acid, using the first extraction solvent to extract, concentrating a part of solvent, or distilling the solvent to dryness, and then adding a new solvent; finally, crystallizing, filtering, and drying to obtain the valsartan.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: September 6, 2022
    Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd
    Inventors: Xiaohui Zhou, Xiaoren Zhu, Yuanxun Zhu, Peng Dong, Peng Wang, Jinsheng Lin, Wenquan Zhu, Min Li
  • Patent number: 11420948
    Abstract: The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high.
    Type: Grant
    Filed: August 6, 2019
    Date of Patent: August 23, 2022
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
    Inventors: Wenjing Liao, Jianfeng Ge, Jicheng Zhang, Luning Huang, Anping Tao, Eric Gu
  • Patent number: 11365178
    Abstract: The present invention relates to a method for preparing an intermediate (Formula IV) of sodium elagolix. The intermediate is prepared by the following route. The method has advantages of simple and safe operation, high yield, less environmental pollution, good economic effect and suitability for industrial production, wherein R represents C1-C4 substituted or unsubstituted benzyl or allyl.
    Type: Grant
    Filed: December 25, 2018
    Date of Patent: June 21, 2022
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI SYNCORES TECHNOLOGIES, INC
    Inventors: Hu Su, Xiaowen Guo, Yukun Liang, Kaiqiang Shi, Jintao Yang, Kang He, Anping Tao, Luning Huang, Jianguo An, Xi Chen, Hong Gu
  • Publication number: 20220185816
    Abstract: Related are a JAK kinase inhibitor, a preparation method for same, and applications thereof in the field of medicine, related to the field of medicinal chemistry. Provided is a novel small molecule JAK inhibitor, which has the structure as represented by formula (II). The compound provides improved efficacy and safeness in preventing or treating a JAK-related indication.
    Type: Application
    Filed: March 11, 2020
    Publication date: June 16, 2022
    Applicants: SHANGHAI SYNERGY PHARMACEUTICAL SCIENCES CO., LTD, ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Xin XU, Jia CHEN, Zhen ZHANG, Guan WANG, Linli ZHANG, Qiang LI, Chenghao XI, Minkai QU, Xiaojuan ZHANG, Chunqiao CHEN, Fan YANG, Xiaoer XIA, Yijin WANG, Yunfei LI, Jian GE
  • Publication number: 20220062249
    Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals having an average particle size of 2-52 ?m.
    Type: Application
    Filed: November 10, 2021
    Publication date: March 3, 2022
    Applicants: Shanghai Synergy Pharmaceutical Sciences Co., Ltd, Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventors: Jian GE, Yunfei LI, Lihong LIN, Dengxue SUN, Jiamiao WANG, Yijin WANG, Zhiyun WANG
  • Patent number: 11197850
    Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals, and the average grain size of the crystals ranges from 0.5 ?m to 100 ?m.
    Type: Grant
    Filed: February 13, 2018
    Date of Patent: December 14, 2021
    Assignees: Shanghai Synergy Pharmaceutical Sciences Co., Ltd., Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventors: Jian Ge, Yunfei Li, Lihong Lin, Dengxue Sun, Jiamiao Wang, Yijin Wang, Zhiyun Wang
  • Patent number: 11168063
    Abstract: The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: November 9, 2021
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Shanghai Aobo Pharmtech, Inc., Ltd.
    Inventors: Wei Xu, Xi Chen, Hong Gu
  • Publication number: 20210300883
    Abstract: The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high.
    Type: Application
    Filed: August 6, 2019
    Publication date: September 30, 2021
    Applicants: Zhejiang Huahai Pharmaceutical Co., Ltd, SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
    Inventors: Wenjing LIAO, Jianfeng GE, Jicheng ZHANG, Luning HUANG, Anping TAO, Eric GU
  • Publication number: 20210276968
    Abstract: Provided herein is a method for preparing an Escitalopram bis-hydroxynaphthoate ((S)-(+)-1-(3+(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-cyanisobenzofuranone) crystal form A. Said method is ecofriendly and non pollutive, and the obtained Escitalopram bis-hydroxynaphthoate crystal form A is highly pure and easy to reproduce.
    Type: Application
    Filed: October 12, 2019
    Publication date: September 9, 2021
    Applicants: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI AOBO PHARMTECH, INC., LTD.
    Inventors: Wei XU, Xi CHEN, Hong GU
  • Patent number: 11091508
    Abstract: Provided are a fosaprepitant phosphate intermediate (IV) preparation method, a fosaprepitant phosphate intermediate (IV-A) and a method of (AA) for preparing fosaprepitant dimeglumine by using the intermediate (IV-A). IV: R1 and R2 are independently selected from C1-C7 alkyl groups or benzyl groups; IV-A: R1 and R2 are independently selected from C1-C7 alkyl groups, and R1 and R2 are not both benzyl groups.
    Type: Grant
    Filed: May 9, 2017
    Date of Patent: August 17, 2021
    Assignees: SHANGHAI AOBO PHARMTECH, INC., LTD., ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Jicheng Zhang, Zeng Li, Luning Huang, Qian Chen, Anping Tao, Hong Gu
  • Patent number: 11072601
    Abstract: Disclosed are a class of ?-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 ?-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.
    Type: Grant
    Filed: September 17, 2018
    Date of Patent: July 27, 2021
    Assignees: SHANGHAI SYNERGY PHARMACEUTICAL SCIENCES CO., LTD., ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: 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
  • Patent number: 11014885
    Abstract: Disclosed is a new method for preparing a donepezil pamoate (1-benzyl-4-[(5,6-dimethoxyindan-2-one)methyl]piperidine pamoate). The donepezil pamoate prepared by using the method has a high purity and a good flowability.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: May 25, 2021
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Shanghai Aobo Pharmtech, Inc., Ltd.
    Inventors: Wei Xu, Xi Chen, Hong Gu
  • Patent number: 10961194
    Abstract: Provided is a method for purifying ropinirole hydrochloride (4-2-di-n-propylaminoethyl-1,3-dihydro-2H-indole-2-ketohydrochloride). The method comprises: adding ropinirole hydrochloride containing a monopropyl impurity A into water, adding organic solvent, stirring and dissolving at room temperature, adding alkali, stirring, standing, demixing, and removing an aqueous layer; optionally, drying the organic layer by using anhydrous magnesium sulfate, and filtering; and adding acyl chloride or acid anhydride into the organic layer, stirring, concentrating the organic layer to be dry, adding an organic solvent into the obtained oily matter, adding concentrated hydrochloric acid, and stirring, so as to obtain the ropinirole hydrochloride. By using the method, the impurity A in the ropinirole hydrochloride can be effectively removed, and the ropinirole hydrochloride can be obtained with a high yield and a high purity, so that the impurity A is controlled and the purity of the product reaches a medicinal standard.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: March 30, 2021
    Assignees: ZHEJIANG HUAHAI LICHENG PHARMACEUTICAL CO., LTD., ZHEJIANG HUAHAI PHARMACEUTICALS CO., LTD.
    Inventors: Guoliang Tu, Zhongming Xu, Tao Zhou, Wenfeng Huang, Shiwen Zhang
  • Patent number: 10836751
    Abstract: The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of methyl 4-(1-alkoxy-1,3-dioxo-3-phenyl propan-2-yl)-3-nitrobenzoate (compound IV) and methyl 3-benzoyl-2-oxoindoline-6-formate (compound V). The method for preparing nintedanib (I) provided by the present application has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: November 17, 2020
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Shanghai Syncores Technologies, Inc.
    Inventors: Zeng Li, Xiaosong Cheng, Xianliang He, Jicheng Zhang, Luning Huang, Anping Tao, Hong Gu
  • Patent number: 10781173
    Abstract: Provided is a method for preparing apremilast of formula I. Method one: (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine N-acetyl-L-leucine salt of formula II is reacted with 3-acetylaminophthalic anhydride of formula III in an aprotic solvent to produce the compound of formula I; method two: (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine N-acetyl-L-leucine salt of formula II is reacted with 3-acetylaminophthalic anhydride of formula III in an organic solvent in the presence of an organic alkali or an alkali metal hydride to produce the compound of formula I. The method for preparing apremilast requires inexpensive raw materials and reagents, is suitable for industrial production, and has great economic effects.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: September 22, 2020
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
    Inventors: Xiaoqiu Du, Lianchao Zhou, Jiegen Liu