Patents by Inventor Fuli Zhang
Fuli Zhang has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 10676442Abstract: The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.Type: GrantFiled: August 30, 2017Date of Patent: June 9, 2020Assignees: China State Institute of Pharmaceutical Industry, Shanghai Institute of Pharmaceutical IndustryInventors: Meihua Xie, Fuli Zhang, Taizhi Wu, Jialiang Zhong
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Patent number: 10508112Abstract: Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.Type: GrantFiled: June 21, 2018Date of Patent: December 17, 2019Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Weiwei Xu, Hua Bai
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Publication number: 20190177277Abstract: The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.Type: ApplicationFiled: August 30, 2017Publication date: June 13, 2019Inventors: Meihua XIE, Fuli ZHANG, Taizhi WU, Jialiang ZHONG
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Publication number: 20180297998Abstract: Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.Type: ApplicationFiled: June 21, 2018Publication date: October 18, 2018Inventors: Fuli ZHANG, Zhezhou YANG, Rusheng BAO, Weiwei XU, Hua BAI
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Patent number: 10035798Abstract: Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using ?-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.Type: GrantFiled: February 12, 2015Date of Patent: July 31, 2018Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Weiwei Xu, Hua Bai
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Publication number: 20180030049Abstract: Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using ?-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.Type: ApplicationFiled: February 12, 2015Publication date: February 1, 2018Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli ZHANG, Zhezhou YANG, Rusheng BAO, Weiwei XU, Hua BAI
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Patent number: 9676736Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.Type: GrantFiled: April 15, 2013Date of Patent: June 13, 2017Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Fuli Zhang, Chonghao Liu, Pengcheng Qiu, Jian Chai, Qingfeng Cai
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Patent number: 9527804Abstract: The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.Type: GrantFiled: June 23, 2014Date of Patent: December 27, 2016Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Pengcheng Qiu, Linyong Jin, Hu Pan, Linyu Pan, Dongming Jiang, Weiwei Xu
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Patent number: 9434702Abstract: Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.Type: GrantFiled: February 8, 2013Date of Patent: September 6, 2016Assignees: Zhejiang Hisun Pharamceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Chunbo Yang, Bin Liang, Pengcheng Qiu, Hairong Luo, Jiang Li, Jian Chai, Qingfeng Cai
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Patent number: 9353049Abstract: The present invention provides a preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate, preparation methods for intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium, (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium, as well as a method for using (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium to prepare rivastigmine which can be used for the treatment of Alzheimer's disease.Type: GrantFiled: May 16, 2012Date of Patent: May 31, 2016Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Chunbo Yang, Daoxin Chen, Zhiqing Yang, Rentong Sun, Hua Bai
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Publication number: 20160130218Abstract: The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.Type: ApplicationFiled: June 23, 2014Publication date: May 12, 2016Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Pengcheng Qiu, Linyong Jin, Hu Pan, Linyu Pan, Dongming Jiang, Weiwei Xu
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Patent number: 9079892Abstract: A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.Type: GrantFiled: February 22, 2013Date of Patent: July 14, 2015Assignees: CHINA NATIONAL MEDICINES GUORUI PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Fuli Zhang, Bin Liang, Chunbo Yang, Chonghao Liu, Yang Gao, Jian Wang, Min Jiang
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Publication number: 20150087828Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.Type: ApplicationFiled: April 15, 2013Publication date: March 26, 2015Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Chonghao Liu, Pengcheng Qiu, Jian Chai, Qingfeng Cai
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Publication number: 20150038704Abstract: A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.Type: ApplicationFiled: February 22, 2013Publication date: February 5, 2015Applicants: China National Medicines Guorui Pharmaceutical Co., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Bin Liang, Chunbo Yang, Chonghao Liu, Yang Gao, Jian Wang, Min Jiang
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Publication number: 20150011757Abstract: Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.Type: ApplicationFiled: February 8, 2013Publication date: January 8, 2015Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Chunbo Yang, Bin Liang, Pengcheng Qiu, Hairong Luo, Jiang Li, Jian Chai, Qingfeng Cai
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Publication number: 20140073809Abstract: The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production.Type: ApplicationFiled: May 16, 2012Publication date: March 13, 2014Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Fuli Zhang, Zhezhou Yang, Chunbo Yang, Daoxin Chen, Zhiqing Yang, Rentong Sun, Hua Bai
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Patent number: 8618308Abstract: The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole, or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole.Type: GrantFiled: November 17, 2008Date of Patent: December 31, 2013Assignee: Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Taizhi Wu, Meihua Xie
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Patent number: 8324429Abstract: The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N—[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.Type: GrantFiled: January 10, 2008Date of Patent: December 4, 2012Assignees: Shanghai Institute of Pharmaceutical Industry, Zhejian Hisun Pharmaceutical Co., Ltd.Inventors: Fuli Zhang, Meng Hu, Meihua Xie, Anping Lai, Rentong Sun, Daoxin Chen, Rusheng Bao, Hua Bai
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Publication number: 20120095237Abstract: The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate (formula I) by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), therefore purified compound of formula I can be produced. Producing of olmesartan medoxomil at high purity is assured by said processes. R in formula I is selected from C1-C6 alkyl.Type: ApplicationFiled: November 17, 2008Publication date: April 19, 2012Applicant: Shanghai Institute of Pharmaceutical IndustryInventors: Fuli Zhang, Taizhi Wu, Meihua Xie
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Publication number: 20100286437Abstract: The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N—[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.Type: ApplicationFiled: January 10, 2008Publication date: November 11, 2010Inventors: Fuli Zhang, Meng Hu, Meihua Xie, Anping Lai, Rentong Sun, Daoxin Chen, Rusheng Bao, Hua Bai