Patents by Inventor Guangxin Xia

Guangxin Xia 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).

  • Publication number: 20240116925
    Abstract: A salt of a nitrogen-containing fused heterocyclic compound or a crystal form thereof, and a preparation method therefor, a pharmaceutical composition thereof, and a use thereof, in particular, a salt of compound I as shown below or a crystal form thereof, and a preparation method, a pharmaceutical composition and a use. The salt of compound I or the crystal form thereof exhibits at least one of the following advantages: improved bioavailability, great mechanical properties, improved chemical stability, excellent fluidity, great compressibility, and improved dissolution characteristics.
    Type: Application
    Filed: February 9, 2022
    Publication date: April 11, 2024
    Inventors: Hui CHEN, Guangxin XIA, Qian WANG, Junyao LIU, Yanan HAN, Ying KE
  • Publication number: 20240101552
    Abstract: Provided is the carbonyl heterocyclic compound shown in formula (I) or a pharmaceutically acceptable salt thereof, capable of being used as a compound having a targeted lanthionine synthetase C-like protein 2 pathway and being used for the treatment of various conditions, including infectious diseases, autoimmune diseases, diabetes, and chronic inflammatory diseases.
    Type: Application
    Filed: September 18, 2021
    Publication date: March 28, 2024
    Inventors: Chaoxin ZHANG, Guangxin XIA, Zhijun XIANG, Ying KE, Jiangsong LOU, Menghao ZHAO, Lijun HAO
  • Publication number: 20230398123
    Abstract: The present invention relates to pharmaceutical methods, compositions, combinations for the treatment and/or prevention of inflammatory bowel diseases (IBD). The invention relates particularly to methods and compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt thereof, for treating IBD.
    Type: Application
    Filed: September 3, 2021
    Publication date: December 14, 2023
    Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Xin NAKANISHI, Guangxin XIA, Wei SU
  • Publication number: 20230365563
    Abstract: A quinazoline compound as shown in formula I, and a pharmaceutically acceptable salt, solvate, prodrug, metabolite or isotopic compound thereof having a good inhibiting effect on a KRAS mutant protein.
    Type: Application
    Filed: September 30, 2021
    Publication date: November 16, 2023
    Inventors: Chaoxin ZHANG, Haibin MAO, Guangxin XIA, Yuhong FU, Xuesong WANG, Yingchun CAI, Xing MA, Wei DENG, Ying KE, Jianmin FU
  • Publication number: 20230330093
    Abstract: The present invention provides a use of a nitrogen-containing saturated heterocyclic compound.
    Type: Application
    Filed: September 3, 2021
    Publication date: October 19, 2023
    Inventors: Guangxin XIA, Wei SU, Xuesong WANG, Ying KE
  • Patent number: 11578074
    Abstract: A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: February 14, 2023
    Assignee: Shanghai Pharmaceuticals Holding Cd., Ltd.
    Inventors: Guangxin Xia, Di Li, Jing Zhang, Lingjun Duan, Hongjian Zuo, Wenbo Xiao, Jia Xu, Yanjun Liu
  • Publication number: 20230028539
    Abstract: A pharmaceutical composition, a complementary kit and an application thereof; the pharmaceutical composition comprises pramipexole and safinamide, the mass ratio of pramipexole to safinamide being 1:300-1:30; and the pharmaceutical composition has a good curative effect and has few side effects, and effectively improve the condition of a patient. The capabilities thereof in restoring dopamine levels are better than those from using pramipexole or safinamide alone. In addition, the composition has better neuroprotective activity, and therefore damage to the dopaminergic system and the normal sensitivity of the dopamine system to dopamine agonists are reduced. The composition can restore or balance a potential unbalanced response to “increasing dopaminergic treatment” that is caused by the use of a dopamine agonist alone; the composition can reduce the amount of pramipexole when used alone so as to reduce the risk of side effects and drug resistance.
    Type: Application
    Filed: November 20, 2020
    Publication date: January 26, 2023
    Inventors: Wei SU, Guangxin XIA, Xuesong WANG, Ying KE, Guangqing BI, Jian HUANG
  • Publication number: 20220380433
    Abstract: The present invention relates to an immune cell, which contains a TMEM59 protein and/or a functional fragment thereof, a chimeric antigen receptor (CAR) and/or a coding element thereof, as well as a use of the immune cell in the preparation of a drug for treating tumors. Further provided are a method for promoting the proliferation of immune cells and a method for promoting the production of memory cells.
    Type: Application
    Filed: November 12, 2020
    Publication date: December 1, 2022
    Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Xuemei LIAO, Jingwei HUANG, Zhuo CHEN, Yang LIU, Xiaocui CHENG, Manman XIE, Rongfang SUN, Yingying LI, Guangxin XIA, Ying KE, Yanjun LIU
  • Publication number: 20220324868
    Abstract: Disclosed in the present invention are a pyrazolone-fused pyrimidine compound, and a preparation method and a use therefor. Provided in the present invention is a pyrazolone-fused pyrimidine compound as in formula (I), said compound having better inhibitory activity towards WEE1 kinase.
    Type: Application
    Filed: August 28, 2020
    Publication date: October 13, 2022
    Inventors: Qian WANG, Guoyong HUO, Guangxin XIA, Jiangsong LOU, Sijie SHU, Hui GE, Lin ZHANG, Chen SHI, Zhihui ZHANG, Yu MAO, Bingbin ZHANG, Jianxin YU, Yanjun LIU, Ying KE, Chi ZHANG
  • Publication number: 20220259210
    Abstract: Disclosed are a pyrazolone-fused pyrimidine compound, a preparation method for same and applications thereof. Provided in the present invention is the pyrazolone-fused pyrimidine compound as represented by formula (II). The compound has improved inhibitory activity with respect to WEE1 kinase.
    Type: Application
    Filed: June 28, 2020
    Publication date: August 18, 2022
    Inventors: Qian WANG, Sijie SHU, Guangxin XIA, Hui GE, Bingbin ZHANG, Guoyong HUO, Lin ZHANG, Chen SHI, Jiangsong LOU, Chi ZHANG, Zhihui ZHANG, Yu MAO, Jianxin YU, Ying KE, Yanjun LIU
  • Publication number: 20220195397
    Abstract: A modified immune effector cell and a use thereof, a cell population containing the immune effector cell, and a pharmaceutical composition. The expression and/or activity of an S1PR1 protein of the modified immune effector cell is up-regulated.
    Type: Application
    Filed: April 3, 2020
    Publication date: June 23, 2022
    Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Xuemei LIAO, Jingwei HUANG, Zhuo CHEN, Manman XIE, Andi LI, Yang LIU, Guangxin XIA, Yanjun LIU, Ying KE
  • Publication number: 20220048915
    Abstract: Disclosed by the present invention are a nitrogen-containing heterocyclic compound, and a composition thereof, a preparation method therefor and an application thereof. The structure of the nitrogen-containing heterocyclic compound according to the present invention is shown in Formula I. The nitrogen-containing heterocyclic compound according to the present invention or a pharmaceutically acceptable salt thereof has better inhibitory activity on p38 protein kinase and/or higher bioavailability. In addition, the preparation method is simple.
    Type: Application
    Filed: December 2, 2019
    Publication date: February 17, 2022
    Inventors: Di LI, Lingjun DUAN, Tixu ZHENG, Yang WANG, Kaijun JIN, Wei SU, Yuan HONG, Jia XU, Guangxin XIA, Ying KE
  • Patent number: 10988476
    Abstract: The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.
    Type: Grant
    Filed: April 15, 2020
    Date of Patent: April 27, 2021
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
  • Patent number: 10870627
    Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 22, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Di Li, Ning Zhou, Ao Chen, Liang Zhao, Jiansheng Han, Yanjun Liu
  • Patent number: 10828305
    Abstract: Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: November 10, 2020
    Assignee: Shanghai Pharmaceuticals Holding Co., Ltd.
    Inventors: Guangxin Xia, Di Li, Hongjian Zuo, Guangsheng Wu, Lingjun Duan, Jing Zhang, Yu Mao, Yanjun Liu
  • Publication number: 20200239470
    Abstract: The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.
    Type: Application
    Filed: April 15, 2020
    Publication date: July 30, 2020
    Inventors: Guangxin XIA, Qian WANG, Chen SHI, Xiong ZHAI, Hui GE, Xuemei LIAO, Yu MAO, Zhixiong XIANG, Yanan HAN, Guoyong HUO, Yanjun LIU
  • Publication number: 20200190091
    Abstract: A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target.
    Type: Application
    Filed: August 31, 2018
    Publication date: June 18, 2020
    Inventors: Guangxin XIA, Di LI, Jing ZHANG, Lingjun DUAN, Hongjian ZUO, Wenbo XIAO, Jia XU, Yanjun LIU
  • Patent number: 10662186
    Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: May 26, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
  • Patent number: 10519150
    Abstract: The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: December 31, 2019
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Jianshu Xie, Guohui Jia, Jiansheng Han, Naoko Ueda, Toru Iijima
  • Publication number: 20190300491
    Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
    Type: Application
    Filed: September 22, 2017
    Publication date: October 3, 2019
    Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin XIA, Di LI, Ning ZHOU, Ao CHEN, Liang ZHAO, Jiansheng HAN, Yanjun LIU