Patents by Inventor Wu Du

Wu Du 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: 20250082763
    Abstract: A combination drug for treating triple-negative breast cancer. Androgen receptor-targeting degraders (including PROTACs) can effectively prevent and/or treat triple negative breast cancer (including androgen receptor-positive triple negative breast cancer). The combined use of an androgen receptor degrader and a targeting drug (including PI3K? inhibitors and PARP inhibitors), immunotherapy drug or chemotherapy drug can effectively prevent and/or treat triple negative breast cancer.
    Type: Application
    Filed: November 18, 2024
    Publication date: March 13, 2025
    Inventors: Jing LI, Wu DU, Guoqing LIU, Yongxu HUO, Kefan CHEN, Xinghai LI
  • Publication number: 20250082764
    Abstract: Provided is a drug for treating triple negative breast cancer. Provided is use of an androgen receptor (AR) degrader (including PROTAC) in the preparation of a drug for preventing and/or treating triple negative breast cancer (including androgen receptor positive triple negative breast cancer). Provided is use of an AR degrader in combination with a targeting drug (comprising a PI3K? inhibitor and a PARP inhibitor), an immunotherapy drug or a chemotherapeutic drug in the preparation of a drug for preventing and/or treating triple negative breast cancer.
    Type: Application
    Filed: November 18, 2024
    Publication date: March 13, 2025
    Inventors: Jing LI, Wu DU, Guoqing LIU, Yongxu HUO, Kefan CHEN, Xinghai LI
  • Publication number: 20250051347
    Abstract: A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines.
    Type: Application
    Filed: July 29, 2022
    Publication date: February 13, 2025
    Applicant: Hinova Pharmaceuticals, Inc.
    Inventors: Wu Du, Xinghai Li, Kun Wen, Dekun Qin, Shaohua Zhang, Song Chen, Jingyi Duan, Haibin Lv, Haibo Li, Yu Li, Jinyun He, Muyang Chen, Shijuan Liu, Yiwei Fu, Yikai Guan, Zhilin Tu
  • Patent number: 12194040
    Abstract: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.
    Type: Grant
    Filed: December 24, 2019
    Date of Patent: January 14, 2025
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Yu Li, Kun Wen, Xinghai Li, Yuanwei Chen
  • Publication number: 20240277710
    Abstract: A pharmaceutical composition for the treatment of cancer and a use thereof are provided. The pharmaceutical composition consists of an FAK inhibitor and a CD44 inhibitor. Also provided is a drug combination of an FAK inhibitor and a CD44 inhibitor for the treatment of cancer. The CD44 inhibitor and FAK inhibitor drug combination can have synergistic effects, significantly improving tumor inhibition effects, reducing toxic side effects, and overcoming tumor drug resistance.
    Type: Application
    Filed: May 24, 2022
    Publication date: August 22, 2024
    Inventors: Jing LI, Wu DU, Yongxu HUO, Xinghai LI
  • Patent number: 11926618
    Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.
    Type: Grant
    Filed: August 20, 2020
    Date of Patent: March 12, 2024
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Yu Li, Haibo Li, Yuanwei Chen, Chengzhi Zhang, Xinghai Li
  • Publication number: 20240059678
    Abstract: A synthesis method for an aminopyrimidine FAK inhibitor compound, relating to the field of pharmaceutical synthesis. In the synthesis method, R1 is hydrogen or a carboxylic acid protecting group, R2 is selected from C1˜C6 alkyl or C1˜C6 deuterated alkyl, R3 and R4 are each independently selected from hydrogen or deuterium, and R5 is selected from C1˜C6 alkyl or C1˜C6 deuterated alkyl. The synthesis method is simple to operate, and has low costs. The product prepared can obtain a high total yield (?66%) and a high purity (?99%), and the product yield and purity are superior to those in the prior art (in the prior art, the total yield is about 11%, and the purity is 99%). The synthesis method achieves excellent effects, can also successfully prepare a final product on kilogram scale, and is suitable for industrial production, having a good application prospect.
    Type: Application
    Filed: January 18, 2022
    Publication date: February 22, 2024
    Inventors: Wu DU, Haibin LV, Yu LI, Tongtao KUANG, Xi GENG
  • Patent number: 11891379
    Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I), R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: February 6, 2024
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Yu Li, Kun Wen, Xinghai Li, Yuanwei Chen
  • Patent number: 11753392
    Abstract: A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R4—NH—R5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: September 12, 2023
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Kun Wen, Jinyun He, Haibo Li, Dekun Qin, Xinghai Li, Yuanwei Chen
  • Publication number: 20230091225
    Abstract: Bifunctional chimeric heterocyclic compounds of formula (I) is effective for targeted degradation of androgen receptors and use thereof. The compound of formula (I) also has an isotopic compound, an optical isomer, a tautomer, pharmacologically acceptable salt, a prodrug thereof, or a solvate. In formula (I), ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.
    Type: Application
    Filed: April 16, 2020
    Publication date: March 23, 2023
    Inventors: Wu DU, Kun WEN, Yiwei FU, Haibin LV, Jinyun HE, Dekun QIN, Yu LI, Jingyi DUAN, Yong LI, Chaowu AI, Zhilin TU, Yuanwei CHEN, Xinghai LI, Haibo LI
  • Patent number: 11591301
    Abstract: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: February 28, 2023
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Wen Ren, Haibin Lv, Haibo Li, Kun Wen, Jinyun He, Dekun Qin, Xinghai Li, Yuanwei Chen
  • Publication number: 20220332707
    Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.
    Type: Application
    Filed: August 20, 2020
    Publication date: October 20, 2022
    Inventors: Wu DU, Yu LI, Haibo LI, Yuanwei CHEN, Chengzhi ZHANG, Xinghai LI
  • Patent number: 11447477
    Abstract: Provided is a compound represented by formula (I). Also provided are a pharmaceutical composition containing the compound of formula (I) and use of the compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for preparing drugs for preventing and/or treating diseases having pathological features of IDO-mediated tryptophan metabolic pathways.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 20, 2022
    Assignee: HINOVA PHARMACEUTICALS INC.
    Inventors: Wu Du, Chaowu Ai, Yu Li, Kun Wen, Haibin Lv, Wen Ren, Jinyun He, Dekun Qin, Xinghai Li, Yuanwei Chen
  • Publication number: 20220257774
    Abstract: An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound is represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide). The compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.
    Type: Application
    Filed: May 15, 2020
    Publication date: August 18, 2022
    Inventors: Wu DU, Haibin LV, Haibo LI, Dekun QIN, Chaowu AI, Yu LI, Jingyi DUAN, Zhilin TU, Chengzhi ZHANG, Yuanwei CHEN, Xinghai LI
  • Publication number: 20220177459
    Abstract: The compound shown in formula I has dual inhibitory effects on AR and BRD4. The compound is not only capable of inhibiting the proliferation of androgen receptor AR multi-expressed prostate cancer cell line LNCAP/AR, but also shows good inhibitory effects on prostate cancer lines VCaP and RRRV1, which are resistant to prostate cancer drugs (enzalutamide) on the market. The compound is also capable of being used for preparing proteolysis-targeting chimeras (PROTACs) for inducing the degradation of AR/BRD4 dual targets, and has good prospects for application in the preparation of drugs for the treatment of AR and BRD4-related diseases.
    Type: Application
    Filed: March 31, 2020
    Publication date: June 9, 2022
    Inventors: Wu DU, Haibin LV, Dekun QIN, Haibo LI, Yu LI, Zhilin TU, Yuanwei CHEN, Xinghai LI
  • Publication number: 20220125788
    Abstract: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.
    Type: Application
    Filed: December 24, 2019
    Publication date: April 28, 2022
    Inventors: Wu DU, Yu LI, Kun WEN, Xinghai LI, Yuanwei CHEN
  • Publication number: 20220087996
    Abstract: A compound represented by formula (I), or a stereochemical isomer thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, can inhibit the activity of histone acetylase p300 and inhibit the proliferation activity of a variety of tumor cells.
    Type: Application
    Filed: November 27, 2019
    Publication date: March 24, 2022
    Inventors: Lei FAN, Fei WANG, Xiaoquan WU, Kexin XU, Ke CHEN, Tongchuan LUO, Shaohua ZHANG, Wu DU, Chengzhi ZHANG, Yongxu HUO, Zhilin TU, Xinghai LI, Yuanwei CHEN
  • Publication number: 20220064150
    Abstract: Amine substituted reverse pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Application
    Filed: November 10, 2021
    Publication date: March 3, 2022
    Inventors: Chang-Sun Lee, Ramil Baiazitov, Liangxian Cao, Thomas W. Davis, Wu Du, Ronggang Liu, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko, Richard Gerald Wilde
  • Patent number: 11180483
    Abstract: Amine substituted reverse pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: November 23, 2021
    Assignee: PTC Therapeutics, Inc.
    Inventors: Chang-Sun Lee, Ramil Baiazitov, Liangxian Cao, Thomas W. Davis, Wu Du, Ronggang Liu, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko, Richard Gerald Wilde
  • Publication number: 20210290553
    Abstract: A formulation of androgen receptor inhibitor HC-1119 is prepared from the following ingredients by weight ratio: 1 to 100 parts of the androgen receptor inhibitor HC-1119, 100 to 1000 parts of a solvent, and 0.11 to 11 parts of an antioxidant. The HC-1119 is dissolved in Labrasol so as to significantly improve the solubility of HC-1119, and thus greatly improve the bioavailability, reduce the difference in blood drug concentration and exposure among individuals, and increase the safety of medication. And the HC-1119 soft capsule has good stability.
    Type: Application
    Filed: May 13, 2019
    Publication date: September 23, 2021
    Inventors: Xing WEI, Ming QI, Wu DU, Xinghai LI, Yuanwei CHEN