Patents Assigned to Shanghai Institute of Pharmaceutical Industry
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Patent number: 11667604Abstract: A phenyl-containing compound, an intermediate thereof, a preparation method therefor and an application thereof. Provided is a compound represented by formula I or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy or C(?O)OR8; where R8 is C1-C4 alkyl; R6 is (II), (III) or (IV); and R7 is —OH, —NH2, —NHCH3, —N(CH3)2 or C1-4 alkoxy. The compound has a low critical micelle concentration (CMC) and good dilution resistance and is capable of enclosing an insoluble drug to form a small-molecule micelle having a high drug loading capacity and good stability.Type: GrantFiled: July 14, 2020Date of Patent: June 6, 2023Assignees: SHANGHAI MODERN PHARMACEUTICAL ENGINEERING RESEARCH CENTER CO., LTD., SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jun He, Zhefeng Wang, Yuezhu Zhao, Yani Yang, Qinghui Fu, Wei Bian, Yuan Zhao, Chen Ge, Yue Zhang, Bing Yi, Minghao Niu, Jiuhui Zhang
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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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Patent number: 10112901Abstract: Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.Type: GrantFiled: July 3, 2014Date of Patent: October 30, 2018Assignees: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.Inventors: Yajun Guo, Hanbin Shan, Xueyan Zhu, Zhedong Yuan, Xiong Yu, Meng Guo, Mingtong Hu, Duzheng Wang, Yu Huang
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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: 9745309Abstract: The present invention provides a method for preparing an intermediate compound of sitagliptin represented by formula I. The preparation method comprises: dissolving a compound represented by formula II into an organic solvent; and under the catalysis of fatty acid and effect of chlorosilane, performing a reduction reaction of carbon-carbon double bonds, so as to obtain the intermediate compound of sitagliptin represented by formula I, R being methyl or formoxyl. The preparation method of the present invention avoids precious metal as a catalyst, and accordingly, the cost is low, the post-treatment is simple, the product has a high yield, chemical purity and optical purity, and de % is greater than 99.6%, and the preparation method can be used in synthesis of sitagliptin and is suitable for industrial production.Type: GrantFiled: September 9, 2014Date of Patent: August 29, 2017Assignees: Shanghai Institute of Pharmaceutical Industry, Zhejiang Medicine Co., Ltd.Inventors: Kuaile Lin, Zhengyan Cai, Jing Pan, Weicheng Zhou, Guofeng Wu, Lirong Yue, Dadong Shen
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Patent number: 9663451Abstract: The present invention relates to new forms of co-crystals of agomelatine and p-toluenesulphonic acid, to a process for their preparation and to pharmaceutical compositions containing them. The co-crystals according to the invention have better solubility than agomelatine and are therefore more suitable for the preparation of pharmaceutical compositions. They also have better stability and purity and, moreover, are obtained by a simple process which does not include any difficult steps.Type: GrantFiled: July 30, 2014Date of Patent: May 30, 2017Assignees: LES LABORATOIRES SERVIER, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Hanbin Shan, Yuhui Shen, Ying Luo, Philippe Letellier, Michael Lynch
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Patent number: 9650403Abstract: Disclosed are a platinum (II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammine platinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum (II) compound. Also provided are an application of the platinum (II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum (II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum (II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity.Type: GrantFiled: March 19, 2014Date of Patent: May 16, 2017Assignees: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Baoquan Zhu, Yongzhi Shu, Jun Lin, Haifeng Hu, Quanhai Liu, Bin Zhou
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Patent number: 9573891Abstract: Complexes of agomelatine and sulphonic acids of formula (I): Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.Type: GrantFiled: July 28, 2014Date of Patent: February 21, 2017Assignees: LES LABORATOIRES SERVIER, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Hanbin Shan, Yuhui Shen, Ying Luo, Philippe Letellier, Michael Lynch
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Patent number: 9550741Abstract: Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D3 receptor, 5-HT1A receptor and 5-HT2A receptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof.Type: GrantFiled: May 8, 2014Date of Patent: January 24, 2017Assignee: Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Xiaowen Chen, Zhilong Ma, Li Zhang, Ning Cui
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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: 9527803Abstract: The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.Type: GrantFiled: March 22, 2012Date of Patent: December 27, 2016Assignees: LES LABORATOIRES SERVIER, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Yu Huang, Ling Tong, Xueyan Zhu, Hanbin Shan, Zhedong Yuan, Xiong Yu
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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: 9434760Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.Type: GrantFiled: November 4, 2011Date of Patent: September 6, 2016Assignee: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
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Publication number: 20160194345Abstract: Disclosed are a platinum (II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammine platinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum (II) compound. Also provided are an application of the platinum (II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum (II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum (II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity.Type: ApplicationFiled: March 19, 2014Publication date: July 7, 2016Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Baoquan ZHU, Yongzhi SHU, Jun LIN, Haifeng HU, Quanhai LIU, Bin ZHOU
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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: 9238632Abstract: Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range.Type: GrantFiled: April 9, 2013Date of Patent: January 19, 2016Assignees: NHWA Pharma, Corporation, Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Guan Wang, Guisen Zhang, Yali Li, Xiangqing Xu, Xiaowen Chen, Shicheng Liu, Song Zhao, Minquan Yu
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Publication number: 20150218193Abstract: Water-soluble derivatives and/or prodrugs of acacetin are described herein. The compounds can be used as cardioprotection agents against myocardial infarction induced by ischemia-reperfusion. In one embodiment the compounds are used to treat ischemic cardiac diseases. In the preferred embodiment, the compounds are used to treat and/or prevent myocardial infarction in humans.Type: ApplicationFiled: February 3, 2014Publication date: August 6, 2015Applicants: Shanghai Institute of Pharmaceutical Industry, Versitech LimitedInventors: Gui-Rong Li, Feng Lin