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).

  • Patent number: 11466025
    Abstract: 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: Grant
    Filed: August 22, 2018
    Date of Patent: October 11, 2022
    Assignee: 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
  • Patent number: 11149013
    Abstract: 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: Grant
    Filed: January 18, 2019
    Date of Patent: October 19, 2021
    Assignee: 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
  • Patent number: 11091448
    Abstract: 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: Grant
    Filed: June 26, 2017
    Date of Patent: August 17, 2021
    Assignee: 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
  • Publication number: 20200369628
    Abstract: 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: Application
    Filed: January 18, 2019
    Publication date: November 26, 2020
    Applicant: 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
  • Publication number: 20200361952
    Abstract: 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: Application
    Filed: August 22, 2018
    Publication date: November 19, 2020
    Applicant: 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
  • Patent number: 10584104
    Abstract: 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: Grant
    Filed: April 28, 2016
    Date of Patent: March 10, 2020
    Assignee: 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
  • Publication number: 20190233381
    Abstract: 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: Application
    Filed: June 26, 2017
    Publication date: August 1, 2019
    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
  • Patent number: 10294259
    Abstract: 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: Grant
    Filed: November 11, 2016
    Date of Patent: May 21, 2019
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: 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
  • Publication number: 20180134670
    Abstract: 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: Application
    Filed: April 28, 2016
    Publication date: May 17, 2018
    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
  • Publication number: 20170057989
    Abstract: 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: Application
    Filed: November 11, 2016
    Publication date: March 2, 2017
    Applicant: Tianjin Institute of Pharmaceutical Research
    Inventors: 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
  • Patent number: 9505734
    Abstract: 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: Grant
    Filed: December 5, 2013
    Date of Patent: November 29, 2016
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: 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
  • Publication number: 20160046595
    Abstract: 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: Application
    Filed: December 5, 2013
    Publication date: February 18, 2016
    Applicant: Tianjin Institute of Pharmaceutical Research
    Inventors: 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
  • Publication number: 20150274799
    Abstract: 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: Application
    Filed: February 8, 2012
    Publication date: October 1, 2015
    Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
    Inventors: Min Gong, Gang Fu, Weiren Xu, Lida Tang, Xiaowen Ren, Peng Liu, Yuli Wang, Jiang Wu, Meixiang Zou
  • Publication number: 20150232527
    Abstract: 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: Application
    Filed: March 28, 2012
    Publication date: August 20, 2015
    Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
    Inventors: Min Gong, Weiren Xu, Lida Tang, Gang Fu, Meixiang Zou, Jiang Wu
  • Patent number: 9062087
    Abstract: 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: Grant
    Filed: January 14, 2011
    Date of Patent: June 23, 2015
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: Guilong Zhao, Hua Shao, Weiren Xu, Wei Liu, Yuli Wang, Lida Tang, Chubing Tan, Bingni Liu, Shijun Zhang
  • Patent number: 8835134
    Abstract: 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: Grant
    Filed: September 8, 2008
    Date of Patent: September 16, 2014
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: Yingmei Han, Guangping Xia, Weiren Xu, Zhuanyou Zhao, Wulin Liu, Naxia Zhao, Peng Liu, Shijun Zhang, Xiaoli Fu, Yuli Wang, Weiting Wang, Lida Tang
  • Patent number: 8481577
    Abstract: 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: Grant
    Filed: June 16, 2011
    Date of Patent: July 9, 2013
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: Guilong Zhao, Weiren Xu, Yuli Wang, Lida Tang, Yiliang Li, Meixiang Zou, Wei Liu, Hua Shao, Chubing Tan, Peng Liu
  • Publication number: 20130023486
    Abstract: 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: Application
    Filed: January 14, 2011
    Publication date: January 24, 2013
    Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
    Inventors: Guilong Zhao, Hua Shao, Weiren Xu, Wei Liu, Yuli Wang, Lida Tang, Chubing Tan, Bingni Liu, Shijun Zhang
  • Publication number: 20110281922
    Abstract: 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: Application
    Filed: June 16, 2011
    Publication date: November 17, 2011
    Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
    Inventors: Guilong ZHAO, Weiren Xu, Yuli Wang, Lida Tang, Yiliang Li, Meixiang Zou, Wei Liu, Hua Shao, Chubing Tan, Peng Liu
  • Publication number: 20110218161
    Abstract: 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: Application
    Filed: September 8, 2008
    Publication date: September 8, 2011
    Applicant: Tianjin Institute of Pharmaceutical Research
    Inventors: Yingmei Han, Guangping Xia, Weiren Xu, Zhuanyou Zhao, Wulin Liu, Naxia Zhao, Peng Liu, Shijun Zhang, Xiaoli Fu, Yuli Wang, Weiting Wang, Lida Tang