Patents by Inventor Weiren Xu
Weiren Xu 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: 11466025Abstract: The present invention provides a compound having a structure of formula (I), a preparation method and use thereof, and a pharmaceutical composition containing the compound, wherein R is methyl, ethyl, propyl, vinyl or propenyl. The present invention also provides a crystalline form of the compound, a preparation method and use of the crystalline form, and a pharmaceutical composition comprising the crystalline form. The compounds having the structure of formula (I) of the present invention are present in a solid form, which not only can solve the problem of clopidogrel resistance, but also can solve the problem of severe hemorrhagic side effect and poor safety of some drugs, as well as the problem of poor stability of existing compounds. It can be developed into an ADP receptor antagonist antiplatelet agent with clear therapeutic effect, no resistance and better stability.Type: GrantFiled: August 22, 2018Date of Patent: October 11, 2022Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD.Inventors: Changjiang Huang, Shijun Zhang, Lingjun Li, Lei Liu, Yuquan Li, Jing Yuan, Hui Yan, Songhui Wang, Xuemin Zheng, Qunchao Wei, Xuyuan Liu, Wei Wei, Weiren Xu, Lida Tang, Meixiang Zou
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Patent number: 11149013Abstract: The present invention provides a crystal form of urate transporter 1 inhibitor and a preparation method and use thereof. The crystal form is characterized by a stable state of appearance and a capability of further improving the purity and storage stability of the compound, etc., and suitable as a pharmaceutical raw material.Type: GrantFiled: January 18, 2019Date of Patent: October 19, 2021Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD.Inventors: Guilong Zhao, Changying Liu, Huihui Chen, Yuquan Li, Haizhi Zhang, Xuyuan Liu, Yuqiang Liu, Yafei Xie, Jingwei Wu, Wei Liu, Weiren Xu, Lida Tang, Meixiang Zou
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Patent number: 11091448Abstract: Provided is a method for preparing a URAT1 inhibitor, 2-((5-bromo-4-((4-bromonaphthalen-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio) acetic acid represented by the following formula ZXS-BR, the reaction equation of which being shown as follows. Compared with the prior art, the preparation method provided by the present application is of low cost, ease of handling, ease of quality control, and applicable to industrialization.Type: GrantFiled: June 26, 2017Date of Patent: August 17, 2021Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD.Inventors: Guilong Zhao, Changying Liu, Yuqiang Liu, Huihui Chen, Yuquan Li, Haizhi Zhang, Yafei Xie, Jingwei Wu, Wei Liu, Weiren Xu, Meixiang Zou, Lida Tang
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Publication number: 20200369628Abstract: The present invention provides a crystal form of urate transporter 1 inhibitor and a preparation method and use thereof. The crystal form is characterized by a stable state of appearance and a capability of further improving the purity and storage stability of the compound, etc., and suitable as a pharmaceutical raw material.Type: ApplicationFiled: January 18, 2019Publication date: November 26, 2020Applicant: Tianjin Institute of Pharmaceutical Research Co., Ltd.Inventors: Guilong Zhao, Changying Liu, Huihui Chen, Yuquan Li, Haizhi Zhang, Xuyuan Liu, Yuqiang Liu, Yafei Xie, Jingwei Wu, Wei Liu, Weiren Xu, Lida Tang, Meixiang Zou
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Publication number: 20200361952Abstract: The present invention provides a compound having a structure of formula (I), a preparation method and use thereof, and a pharmaceutical composition containing the compound, wherein R is methyl, ethyl, propyl, vinyl or propenyl. The present invention also provides a crystalline form of the compound, a preparation method and use of the crystalline form, and a pharmaceutical composition comprising the crystalline form. The compounds having the structure of formula (I) of the present invention are present in a solid form, which not only can solve the problem of clopidogrel resistance, but also can solve the problem of severe hemorrhagic side effect and poor safety of some drugs, as well as the problem of poor stability of existing compounds. It can be developed into an ADP receptor antagonist antiplatelet agent with clear therapeutic effect, no resistance and better stability.Type: ApplicationFiled: August 22, 2018Publication date: November 19, 2020Applicant: Tianjin Institute of Pharmaceutical Research Co., Ltd.Inventors: Changjiang Huang, Shijun Zhang, Lingjun Li, Lei Liu, Yuquan Li, Jing Yuan, Hui Yan, Songhui Wang, Xuemin Zheng, Qunchao Wei, Xuyuan Liu, Wei Wei, Weiren Xu, Lida Tang, Meixiang Zou
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Patent number: 10584104Abstract: The present invention relates to the pharmaceutical field for the treatment of hyperuricemia and gout. In particular, the present invention relates to a carboxylic acid urate transporter 1 (URAT1) inhibitor of a general formula (I) containing a diarylmethane structure and a preparation method thereof, and a pharmaceutical composition containing the same and a use thereof in the preparation of medicaments for treating hyperuricemia and gout, wherein R1 is selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, F, Cl, Br, I, CN, NO2, SR4 or OR4; R2 is selected from H, F, Cl, Br or I; R3 is selected from H or C1-C4 alkyl; X is selected from S or CH2; wherein R4 is selected from C1-C10 alkyl.Type: GrantFiled: April 28, 2016Date of Patent: March 10, 2020Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD.Inventors: Guilong Zhao, Wei Liu, Qian Shang, Zhixing Zhou, Yuli Wang, Yuquan Li, Haizhi Zhang, Chuan Li, Changying Liu, Yuqiang Liu, Yafei Xie, Jingwei Wu, Huihui Chen, Weiren Xu, Lida Tang
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Publication number: 20190233381Abstract: Provided is a method for preparing a URAT1 inhibitor, 2-((5-bromo-4-((4-bromonaphthalen-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio) acetic acid represented by the following formula ZXS-BR, the reaction equation of which being shown as follows. Compared with the prior art, the preparation method provided by the present application is of low cost, ease of handling, ease of quality control, and applicable to industrialization.Type: ApplicationFiled: June 26, 2017Publication date: August 1, 2019Inventors: Guilong Zhao, Changying Liu, Yuqiang Liu, Huihui Chen, Yuquan Li, Haizhi Zhang, Yafei Xie, Jingwei Wu, Wei Liu, Weiren Xu, Meixiang Zou, Lida Tang
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Patent number: 10294259Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.Type: GrantFiled: November 11, 2016Date of Patent: May 21, 2019Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Yuli Wang, Bingni Liu, Yafei Xie, Yuqiang Liu, Peng Liu, Jiang Wu, Jiajia Hou, Wei Wei, Wen Du, Weiren Xu, Lida Tang, Meixiang Zou
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Publication number: 20180134670Abstract: The present invention relates to the pharmaceutical field for the treatment of hyperuricemia and gout. In particular, the present invention relates to a carboxylic acid urate transporter 1 (URAT1) inhibitor of a general formula (I) containing a diarylmethane structure and a preparation method thereof, and a pharmaceutical composition containing the same and a use thereof in the preparation of medicaments for treating hyperuricemia and gout, wherein R1 is selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, F, Cl, Br, I, CN, NO2, SR4 or OR4; R2 is selected from H, F, Cl, Br or I; R3 is selected from H or C1-C4 alkyl; X is selected from S or CH2; wherein R4 is selected from C1-C10 alkyl.Type: ApplicationFiled: April 28, 2016Publication date: May 17, 2018Inventors: GUILONG ZHAO, WEI LIU, QIAN SHANG, ZHIXING ZHOU, YULI WANG, YUQUAN LI, HAIZHI ZHANG, CHUAN LI, CHANGYING LIU, YUQIANG LIU, YAFEI XIE, JINGWEI WU, HUIHUI CHEN, WEIREN XU, LIDA TANG
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Publication number: 20170057989Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.Type: ApplicationFiled: November 11, 2016Publication date: March 2, 2017Applicant: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Yuli Wang, Bingni Liu, Yafei Xie, Yuqiang Liu, Peng Liu, Jiang Wu, Jiajia Hou, Wei Wei, Wen Du, Weiren Xu, Lida Tang, Meixiang Zou
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Patent number: 9505734Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.Type: GrantFiled: December 5, 2013Date of Patent: November 29, 2016Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Yuli Wang, Bingni Liu, Yafei Xie, Yuqiang Liu, Peng Liu, Jiang Wu, Jiajia Hou, Wei Wei, Wen Du, Weiren Xu, Lida Tang, Meixiang Zou
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Publication number: 20160046595Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.Type: ApplicationFiled: December 5, 2013Publication date: February 18, 2016Applicant: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Yuli Wang, Bingni Liu, Yafei Xie, Yuqiang Liu, Peng Liu, Jiang Wu, Jiajia Hou, Wei Wei, Wen Du, Weiren Xu, Lida Tang, Meixiang Zou
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Publication number: 20150274799Abstract: Provided is a GLP-1 analogue having the structure as shown in the general formula A: 7HAEX10TFTSX15VSSYLEX22QAAKEFIX30WLX33KGRG37n1X1Cn2X2 ??(general formula A), wherein X10 is glycine or cysteine, X15 is aspartic acid or cysteine, X22 is glycine or cysteine, X30 is alanine or cysteine, X33 is valine or cysteine, and at least one of X10, X15, X22, X30 and X33 is cysteine, X1 and X2 respectively is glycine, alanine or valine, n1=1-30, n2=1-30. The general formula A contains two cysteines to form disulfide bonds. Also provided are the preparation methods and the use of said GLP-1 analogue. Said GLP-1 analogue has a prolonged blood half-life compared with GLP-1, and can be used for the treatment of diabetes and obesity.Type: ApplicationFiled: February 8, 2012Publication date: October 1, 2015Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventors: Min Gong, Gang Fu, Weiren Xu, Lida Tang, Xiaowen Ren, Peng Liu, Yuli Wang, Jiang Wu, Meixiang Zou
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Publication number: 20150232527Abstract: Provided are a glucagon-like peptide-1 (GLP-1) analogue monomer and dimmer, a preparation method thereof, and an application thereof. The GLP-1 analogue monomer comprises one cysteine; and the dimer is formed by two monomer molecules connected via an intermolecular disulfide bond formed by the cysteine. The GLP-1 monomer comprising cysteine has the following general formula: 7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37, wherein X10 is glycine or cysteine, X15 is aspartate or cysteine, X22 is glycine or cysteine, X23 is glutamine or cysteine, X30 is alanine or cysteine, and X33 is valine or cysteine; and only one of X10, X15, X22, X23, X30, and X33 is cysteine. The glucagon-like peptide-1 analogue dimer of the present invention has an in vivo half-life of more than 8 to 96 hours, thus facilitating clinical promotion and application.Type: ApplicationFiled: March 28, 2012Publication date: August 20, 2015Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventors: Min Gong, Weiren Xu, Lida Tang, Gang Fu, Meixiang Zou, Jiang Wu
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Patent number: 9062087Abstract: The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.Type: GrantFiled: January 14, 2011Date of Patent: June 23, 2015Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Hua Shao, Weiren Xu, Wei Liu, Yuli Wang, Lida Tang, Chubing Tan, Bingni Liu, Shijun Zhang
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Patent number: 8835134Abstract: This invention provides a method for preparing cycloastragenol monoglucoside CMG (cycloastragenol-6-O-?-D-glucoside), comprising the steps of: a. using astragaloside IV or Astragali extracts prepared by a conventional method as raw materials and adding an appropriate solvent thereinto to form a raw material solution; b. adding hydrolase and allowing for hydrolysis at a constant temperature to obtain a hydrolysate; c. separating the hydrolysate with macroporous adsorption resin; and d. obtaining the product by purification and separation. The present invention further provides cycloastragenol-6-O-?-D-glucoside prepared according to the method of this invention as well as its use in the preparation of a medicament for treating cardiovascular diseases and pharmaceutical compositions comprising the same.Type: GrantFiled: September 8, 2008Date of Patent: September 16, 2014Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Yingmei Han, Guangping Xia, Weiren Xu, Zhuanyou Zhao, Wulin Liu, Naxia Zhao, Peng Liu, Shijun Zhang, Xiaoli Fu, Yuli Wang, Weiting Wang, Lida Tang
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Patent number: 8481577Abstract: The present invention relates to the field of drugs associated with treating diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.Type: GrantFiled: June 16, 2011Date of Patent: July 9, 2013Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Guilong Zhao, Weiren Xu, Yuli Wang, Lida Tang, Yiliang Li, Meixiang Zou, Wei Liu, Hua Shao, Chubing Tan, Peng Liu
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Publication number: 20130023486Abstract: The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.Type: ApplicationFiled: January 14, 2011Publication date: January 24, 2013Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventors: Guilong Zhao, Hua Shao, Weiren Xu, Wei Liu, Yuli Wang, Lida Tang, Chubing Tan, Bingni Liu, Shijun Zhang
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Publication number: 20110281922Abstract: The present invention relates to the field of drugs associated with treating diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.Type: ApplicationFiled: June 16, 2011Publication date: November 17, 2011Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventors: Guilong ZHAO, Weiren Xu, Yuli Wang, Lida Tang, Yiliang Li, Meixiang Zou, Wei Liu, Hua Shao, Chubing Tan, Peng Liu
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Publication number: 20110218161Abstract: This invention provides a method for preparing cycloastragenol monoglucoside CMG (cycloastragenol-6-O-?-D-glucoside), comprising the steps of: a. using astragaloside IV or Astragali extracts prepared by a conventional method as raw materials and adding an appropriate solvent thereinto to form a raw material solution; b. adding hydrolase and allowing for hydrolysis at a constant temperature to obtain a hydrolysate; c. separating the hydrolysate with macroporous adsorption resin; and d. obtaining the product by purification and separation. The present invention further provides cycloastragenol-6-O-?-D-glucoside prepared according to the method of this invention as well as its use in the preparation of a medicament for treating cardiovascular diseases and pharmaceutical compositions comprising the same.Type: ApplicationFiled: September 8, 2008Publication date: September 8, 2011Applicant: Tianjin Institute of Pharmaceutical ResearchInventors: Yingmei Han, Guangping Xia, Weiren Xu, Zhuanyou Zhao, Wulin Liu, Naxia Zhao, Peng Liu, Shijun Zhang, Xiaoli Fu, Yuli Wang, Weiting Wang, Lida Tang