Patents Assigned to Zhejiang Huahai Pharmaceutical Co., Ltd.
  • 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
  • Patent number: 10766895
    Abstract: Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100?C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: September 8, 2020
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
    Inventors: Haisheng Fan, Xiaowen Guo, Luning Huang, Hong Gu
  • Patent number: 10633368
    Abstract: Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.
    Type: Grant
    Filed: January 16, 2017
    Date of Patent: April 28, 2020
    Assignee: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
    Inventors: Hu Huang, Wenfeng Huang, Guoliang Tu, Jiegen Liu, Zhongming Xu, Qianghui Wu, Zhaoyang Meng, Yuling Fang
  • Patent number: 10633329
    Abstract: A method for preparing a lisinopril intermediate is provided. The method includes: treating (R)-hydroxy-4-phenylbutyrate with sulfonyl chloride in an organic solvent in the presence of a base to obtain a solution of sulfonate; reacting the obtained solution with a salt of trifluoroacetyl lysine; and obtaining a N2-[1-(S)-alkoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine by separating after the reaction is completed. The method provided has a shorter synthesis route, is easy to operate, has a low cost, and is suitable for industrial production.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: April 28, 2020
    Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., ZHEIJIANG HUAHAI TIANCHENG PHARMACEUTICALS CO., LTD., ZHEJIANG HUAHAI LICHENG PHARMACEUTICALS CO., LTD.
    Inventors: Songqing Wang, Peng Dong, Yang Zheng, Quanjun Li
  • Patent number: 10617649
    Abstract: Disclosed is a preparation method for an azacitidine for injection, wherein each injection vial of azacitidine for injection contains 100 mg of azacitidine and 100 mg of mannitol. The preparation method comprises the steps of measuring 80% of the total volume of water for injection at a temperature of 2-6° C.; adding mannitol, and stirring to completely dissolved at a temperature of 2-6° C.; adding azacitidine, stirring to completely dissolved at a temperature of 2-6° C. to obtain an azacitidine solution for injection; filling each injection vial with 23 ml azacitidine solution for injection after filtration; freeze-drying at a preset temperature; and stoppering, capping and packaging after nitrogen filling. The preparation method has the advantages of a simple process, low energy consumption, high production efficiency and stable product quality.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: April 14, 2020
    Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventors: Xiangjie Shi, Jiening Liu, Xinshi Wang, Libin Hu, Hao Chen, Zhiyun Wang
  • Patent number: 10618891
    Abstract: The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: April 14, 2020
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Shanghai Aobo Pharmtech, Inc., Ltd.
    Inventors: Jianping Lin, Xiaowen Guo, Xiaofei Gao, Chao Huang, Yuanbing Guo, Anping Tao, Luning Huang, Hong Gu
  • Publication number: 20200087256
    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: Application
    Filed: June 5, 2018
    Publication date: March 19, 2020
    Applicants: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI AOBO PHARMTECH, INC., LTD.
    Inventors: Wei XU, Xi CHEN, Hong GU
  • Publication number: 20200087273
    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: Application
    Filed: June 5, 2018
    Publication date: March 19, 2020
    Applicants: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD., SHANGHAI AOBO PHARMTECH, INC., LTD.
    Inventors: Wei XU, Xi CHEN, Hong GU