Patents by Inventor Kaixian Chen

Kaixian Chen 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: 10927107
    Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: February 23, 2021
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yiping Wang, Fei Zhao, Jing Zhao, Jiang Wang, Cong Xi, Chenglin Wu, Hao Shen, Xu Han, Hualiang Jiang, Kaixian Chen
  • Publication number: 20210040066
    Abstract: Disclosed are a novel tetrahydroisoquinoline compound, a method for preparing intermediates thereof, a pharmaceutical composition thereof and the use thereof. The tetrahydroisoquinoline compound of the present invention has a good inhibitory effect on phosphodiesterase (PDE4), and can be used in the prevention, treatment or auxiliary treatment of multiple diseases associated with the activity or expression of phosphodiesterase, especially PDE4-associated immune and inflammatory diseases, such as psoriasis and arthritis.
    Type: Application
    Filed: February 3, 2019
    Publication date: February 11, 2021
    Inventors: Yechun XU, Hong LIU, Wei TANG, Xianglei ZHANG, Zhanni GU, Heng LI, Xu HAN, Fenghua ZHU, Chunlan FENG, Guangyu DONG, Tiantian CHEN, Wuyan CHEN, Hualiang JIANG, Kaixian CHEN
  • Publication number: 20210015824
    Abstract: Disclosed is use of a thieno[3,2-d]pyrimidin-4-one compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.
    Type: Application
    Filed: March 8, 2019
    Publication date: January 21, 2021
    Inventors: Hong LIU, Jia LI, Jiang WANG, Yi ZANG, Jian LI, Jingya LI, Dandan SUN, Hualiang JIANG, Kaixian CHEN
  • Patent number: 10875883
    Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: December 29, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Shengbin Zhou, Panfeng Peng, Yong Nian, Shuni Wang, Shuangjie Shu, Hao Shen, Hualiang Jiang, Kaixian Chen
  • Patent number: 10836743
    Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: November 17, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jia Li, Jiang Wang, Mingbo Su, Shuni Wang, Yubo Zhou, Wei Zhu, Wei Xu, Chunpu Li, Hualiang Jiang, Kaixian Chen
  • Patent number: 10800776
    Abstract: A fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof are described. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: October 13, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yu Zhou, Wenjing Xia, Dong Zhang, Hualiang Jiang, Kaixian Chen
  • Publication number: 20200190066
    Abstract: It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.
    Type: Application
    Filed: May 18, 2018
    Publication date: June 18, 2020
    Inventors: Cheng LUO, Yuli XIE, Bing ZHOU, Zhiyi YAO, Liyan YUE, Wei WAN, Bidong ZHANG, Yuanyuan ZHANG, Hualiang JIANG, Kaixian CHEN
  • Publication number: 20200170966
    Abstract: The present invention relates to use of an aminomethylenecyclohexane-1,3-dione compound, more particularly to use of a compound shown in the following formula (I) or a pharmaceutically acceptable salt thereof alone or in combination with other drug in preparing a drug for regulating or treating a disease related to autophagy, especially mammalian ATG8 homologous proteins.
    Type: Application
    Filed: May 18, 2018
    Publication date: June 4, 2020
    Inventors: Cheng LUO, Liyan YUE, Wei WAN, Yuanyuan ZHANG, Hualiang JIANG, Kaixian CHEN
  • Patent number: 10640514
    Abstract: The invention describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: May 5, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
  • Patent number: 10618900
    Abstract: Compounds of formula I are provided. Also provided are methods of preparing the compounds of formula (I), and methods of using the compounds of formula (I) as a negative allosteric modulator of a metabotropic glutamate receptor (mGluR) subtype 5.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: April 14, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yu Zhou, Dong Zhang, Jian Li, Hualiang Jiang, Kaixian Chen
  • Patent number: 10611774
    Abstract: The invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid and a preparation method for the salt form. Also disclosed is a pharmaceutical composition of the formula I compound salt form.
    Type: Grant
    Filed: March 22, 2017
    Date of Patent: April 7, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
  • Publication number: 20200069609
    Abstract: The present invention provides a method (I) for modifying a mammalian ATG8 homologue by a covalent bond, comprising: providing a compound SM-LG including a moiety SM- having a function of modulating a mammalian ATG8 homologue and a leaving moiety -LG; the compound SM-LG reacts with a mammalian ATG8 homologue to produce a covalent complex of the mammalian ATG8 homologue. The invention also provides a covalent complex of the mammalian ATG8 homologue obtained by the method and uses of the same.
    Type: Application
    Filed: May 18, 2018
    Publication date: March 5, 2020
    Inventors: Cheng LUO, Zhiyi YAO, Yuli XIE, Wei WAN, Liyan YUE, Yuanyuan ZHANG, Hualiang JIANG, Kaixian CHEN
  • Publication number: 20200071291
    Abstract: The present invention provides an isoindolone-imide ring-1,3-dione-2-ene compound, and a preparation method, a pharmaceutical composition and use thereof. Specifically, the present invention provides a compound of Formula (I) below or a pharmaceutically acceptable salt thereof, wherein Ar is an isoindolinone-imide group represented by Formula (II), L is absent or is a divalent, trivalent or tetravalent linking group, and X is a group represented by Formula (III). Definitions of the other groups are as described in the specification. The compound of Formula (I) is an autophagy modulators, particularly a mammalian ATG8 homolog modulator.
    Type: Application
    Filed: May 17, 2018
    Publication date: March 5, 2020
    Inventors: Zhiyi YAO, Cheng LUO, Yuli XIE, Liyan YUE, Wei WAN, Yuanyuan ZHANG, Hualiang JIANG, Kaixian CHEN
  • Patent number: 10550143
    Abstract: C, O-spiro aryl glycoside compounds are provided. Specifically provided are C, O-spiro aryl glycoside compounds represented by the formula (I), wherein the definitions of each variable group are described in the specification. Also provided are methods of preparing and using the C, O-spiro aryl glycoside compounds. The C, O-spiro aryl glycoside compounds can be used as SGLT2 inhibitors and for treating diseases, such as diabetes, atherosclerosis, and adiposity.
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: February 4, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Jia Li, Jiang Wang, Jingya Li, Hui Chen, Dan Li, Jian Li, Yibing Wang, Hualiang Jiang, Kaixian Chen
  • Patent number: 10392401
    Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: August 27, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Shengbin Zhou, Mingbo Su, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
  • Publication number: 20190233456
    Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
    Type: Application
    Filed: September 19, 2017
    Publication date: August 1, 2019
    Inventors: Hong LIU, Jiang WANG, Shengbin ZHOU, Panfeng PENG, Yong NIAN, Shuni WANG, Shuangjie SHU, Hao SHEN, Hualiang JIANG, Kaixian CHEN
  • Publication number: 20190210998
    Abstract: The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.
    Type: Application
    Filed: June 2, 2017
    Publication date: July 11, 2019
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Jia Li, Wei Zhu, Yubo Zhou, Jiang Wang, Mingbo Su, Shuni Wang, Wei Xu, Chunpu Li, Weijuan Kan, Hualiang Jiang, Kaixian Chen
  • Publication number: 20190202827
    Abstract: A fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof are described. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.
    Type: Application
    Filed: May 17, 2017
    Publication date: July 4, 2019
    Inventors: Hong LIU, Yu ZHOU, Wenjing XIA, Dong ZHANG, Hualiang JIANG, Kaixian CHEN
  • Publication number: 20190194185
    Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.
    Type: Application
    Filed: March 29, 2017
    Publication date: June 27, 2019
    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yiping Wang, Fei Zhao, Jing Zhao, Jiang Wang, Cong Xi, Chenglin Wu, Hao Shen, Xu Han, Hualiang Jiang, Kaixian Chen
  • Publication number: 20190135818
    Abstract: The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase.
    Type: Application
    Filed: May 24, 2017
    Publication date: May 9, 2019
    Inventors: Hualiang JIANG, Hong LIU, Meiyu GENG, Mingyue ZHENG, Jing AI, Yulan WANG, Xiaowei WU, Shuangjie LI, Xia PENG, Chunpu LI, Kaixian CHEN, Bao WANG