Patents by Inventor Yongxin Han

Yongxin Han 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).

  • TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170305902
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
    Type: Application
    Filed: August 24, 2015
    Publication date: October 26, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
  • PYRIDINE-SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITORS
    Publication number: 20170226084
    Abstract: The present invention discloses pharmaceutically acceptable acid salts of pyridine-substituted 2-aminopyridine derivatives as protein kinase inhibitors, preparation methods, pharmaceutical compositions thereof, and use thereof for the treatment of diseases associated with protein kinase.
    Type: Application
    Filed: July 31, 2015
    Publication date: August 10, 2017
    Inventors: Feng GONG, Xinlu LI, Rui ZHAO, Xiquan ZHANG, Xinhe XU, Xijie LIU, Dengming XIAO, Yongxin HAN
  • Quinazoline derivative and preparation method therefor
    Patent number: 9725439
    Abstract: The present invention relates to a quinazoline derivative shown in formula (I) and a preparation method therefor, a pharmaceutical composition comprising the compound shown in formula (I), and an application of the compound in preparing drugs for curing and preventing tumors. The compound of the present invention can irreversibly prevent EGFR phosphorylation, and effectively depress signal transduction of cancer cells, and accordingly has higher anti-tumor activity in vitro and in vivo.
    Type: Grant
    Filed: September 28, 2014
    Date of Patent: August 8, 2017
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., CENTAURUS BIOPHARMA CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.
    Inventors: Dengming Xiao, Yan Zhu, Yuandong Hu, Huting Wang, Jijun Li, Yong Peng, Hui Zhang, Hong Luo, Fansheng Kong, Yongxin Han
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 9718819
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yunfu Luo, Zhiyu Lei
  • Substituted 2-aminopyridine protein kinase inhibitor
    Patent number: 9708295
    Abstract: The present invention discloses substituted 2-aminopyridine derivatives as protein kinase inhibitors; specifically, the invention relates to 2-aminopyridine derivatives having protein kinase inhibitory properties, their manufacture, pharmaceutical compositions containing them, and use of the compounds and the pharmaceutical compositions thereof for the treatment of diseases associated with protein kinase.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: July 18, 2017
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., Centaurus Biopharma Co., Ltd., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD.
    Inventors: Dengming Xiao, Xinhe Xu, Xijie Liu, Yuandong Hu, Honghao Yu, Zhihua Liu, Yong Peng, Yinghui Sun, Hong Luo, Fansheng Kong, Yongxin Han, Jian Sun
  • INHIBITOR OF BRUTON'S TYROSINE KINASE
    Publication number: 20170144986
    Abstract: Provided are a compound represented by formula (III) or pharmaceutically acceptable salts, solvates, active metabolites, polymorphs, esters, tautomers or prodrugs thereof, pharmaceutical compositions containing the compound represented by formula (III), and the application of the pharmaceutical compositions as selective inreversible inhibitor of Bruton's tyrosine kinase for the prevention and treatment of inflammation, autoimmune diseases (such as rheumatoid arthritis) associated with aberrant B cell proliferation and cancers.
    Type: Application
    Filed: May 7, 2015
    Publication date: May 25, 2017
    Inventors: Yongxin HAN, Li ZHU, Dengming XIAO, Yong PENG, Hong LUO
  • Kinase modulating compounds, compositions containing the same and use thereof
    Patent number: 9550781
    Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: January 24, 2017
    Assignees: Centaurus Biopharma Co., Ltd., Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 9469634
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: October 18, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Chun Sing Li
  • QUINAZOLINE DERIVATIVE AND PREPARATION METHOD THEREFOR
    Publication number: 20160214964
    Abstract: The present invention relates to a quinazoline derivative shown in formula (I) and a preparation method therefor, a pharmaceutical composition comprising the compound shown in formula (I), and an application of the compound in preparing drugs for curing and preventing tumors.
    Type: Application
    Filed: September 28, 2014
    Publication date: July 28, 2016
    Inventors: Dengming XIAO, Yan ZHU, Yuandong HU, Huting WANG, Jijun LI, Yong PENG, Hui ZHANG, Hong LUO, Fansheng KONG, Yongxin HAN
  • AKT PROTEIN KINASE INHIBITORS
    Publication number: 20160152576
    Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: January 31, 2014
    Publication date: June 2, 2016
    Applicant: Array BioPharma, Inc.
    Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicolas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
  • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20160145255
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: February 1, 2016
    Publication date: May 26, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
  • Fused aromatic PTP-1B inhibitors
    Patent number: 9334295
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: October 28, 2014
    Date of Patent: May 10, 2016
    Assignee: KANEQ PHARMA INC.
    Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly
  • HCV NS3 protease inhibitors
    Patent number: 9328138
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: May 3, 2016
    Assignees: MSD Italia S.R.L., Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, John McCauley, Nigel Liverton, Christiane Grisé-Bard, Marie-Christine Brochu, Sylvie Charron, Virender Aulakh, Benoit Bachand, Patrick Beaulieu, Helmi Zaghdane, Yongxin Han, Marco Ferrara, Steven Harper, Vincenzo Summa, Samuel Chackalamannil, Srikanth Venkatraman, Unmesh Shah, Francisco Velazquez
  • Arylalkene derivatives and use thereof as selective estrogen receptor modulators
    Patent number: 9309211
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: April 12, 2016
    Assignee: Centaurus Biopharma Co., Ltd.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR
    Publication number: 20160002205
    Abstract: Disclosed are a 2-aminopyridine derivative having protein kinase inhibition activity, preparation method and pharmaceutical composition thereof. Also disclosed are uses of the compound and the pharmaceutical composition thereof in the preparation of drugs for treating and/or preventing protein kinase-related diseases.
    Type: Application
    Filed: January 27, 2014
    Publication date: January 7, 2016
    Inventors: Dengming Xiao, Xinhe Xu, Xijie Liu, Yuandong Hu, Honghao Yu, Zhihua Liu, Yong Peng, Yinghui Sun, Hong Luo, Fansheng Kong, Yongxin Han, Jian Sun
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20150299171
    Abstract: The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans.
    Type: Application
    Filed: November 29, 2013
    Publication date: October 22, 2015
    Inventors: Yongxin HAN, Rong YU, Zanping WANG, Zhi LIANG, Quan HU, Li ZHU, Yuandong HU, Yinghui SUN, Na ZHAO, Yong PENG, Xiaofeng ZHAI, Hong LUO, Dengming XIAO
  • HCV NS3 protease inhibitors
    Patent number: 8987195
    Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: March 24, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Thomas Bara, Sathesh Bhat, Dipshikha Biswas, Linda Brockunier, Duane A. Burnett, Samuel Chackalamannil, Mariappan V. Chelliah, Austin Chen, Martin Clasby, Vince J. Colandrea, Zhuyan Guo, Yongxin Han, Charles Jayne, Hubert Josien, Karen Marcantonio, Shouwu Miao, Santhosh Neelamkavil, Patrick Pinto, Murali Rajagopalan, Unmesh Shah, Francisco Velazquez, Srikanth Venkatraman, Yan Xia
  • Thiophenecarboxamide derivatives as EP4 receptor ligands
    Patent number: 8969394
    Abstract: The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: March 3, 2015
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Marc Blouin, Jason Burch, Yongxin Han, Christophe Mellon
  • FUSED AROMATIC PHOSPHONATE DERIVATIVES AS PRECURSORS TO PTP-1B INHIBITORS
    Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • FUSED AROMATIC PTP-1B INHIBITORS
    Publication number: 20150045325
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 12, 2015
    Applicant: Kaneq Pharma Inc.
    Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly