Patents by Inventor Chun-Sing Li

Chun-Sing Li 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).

  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 10556900
    Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: February 11, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
  • Linkers and their application towards ADC
    Patent number: 10280229
    Abstract: The present invention relates to linkers, containing amide surrogates with a regular or a novel lysosomal enzymatic cleavable dipeptidic unit, to connect cytotoxic drugs to antibodies. The present invention also relates to ADCs (antibody-drug conjugates) derived from these amide surrogate linkers for the treatment of cancers.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: May 7, 2019
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Chun Sing Li, Jian Li, Yong Cang, Shuhui Chen, Gang Li, Xiongbin Xu, Lun Lu
  • Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
    Patent number: 9975888
    Abstract: The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: May 22, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Chun Sing Li, Tingting Yu
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20180105518
    Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: April 4, 2016
    Publication date: April 19, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
  • TrKA kinase inhibitors, compositions and methods thereof
    Patent number: 9914736
    Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: March 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9896447
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: February 20, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9862707
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • TRKA kinase inhibitors, compositions and methods thereof
    Patent number: 9862716
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi-Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
  • NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20170349585
    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: June 7, 2017
    Publication date: December 7, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9815846
    Abstract: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: November 14, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi-Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Kerim Babaoglu, Dongfang Meng, Jane Wu, Ping Liu, Harold B. Wood, Jianming Bao, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • 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
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9718782
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: August 1, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • LINKERS AND THEIR APPLICATION TOWARDS ADC
    Publication number: 20170202974
    Abstract: The present invention relates to linkers, containing amide surrogates with a regular or a novel lysosomal enzymatic cleavable dipeptidic unit, to connect cytotoxic drugs to antibodies. The present invention also relates to ADCs (antibody-drug conjugates) derived from these amide surrogate linkers for the treatment of cancers.
    Type: Application
    Filed: July 13, 2015
    Publication date: July 20, 2017
    Applicant: MEDSHINE DISCOVERY INC.
    Inventors: Chun Sing LI, Jian LI, Yong CANG, Shuhui CHEN, Gang LI, Xiongbin XU, Lun LU
  • TrKA Kinase Inhibitors, Compositions and Methods Thereof
    Publication number: 20170158698
    Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: June 8, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170114056
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 27, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi- Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170114071
    Abstract: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 27, 2017
    Applicants: Merck Sharp & Dohme Corp., MSD R & D (China) Co., LTD.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi- Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Kerim Babaoglu, Dongfang Meng, Jane Wu, Ping Liu, Harold B. Wood, Jianming Bao, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20170107204
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: March 23, 2015
    Publication date: April 20, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • 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
  • ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
    Publication number: 20160297809
    Abstract: The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
    Type: Application
    Filed: November 7, 2014
    Publication date: October 13, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Craig A. Coburn, Milana M. Maletic, Yunfu Luo, Zhiqi Qi, Chun Sing Li, Tingting Yu
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20160229850
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: September 17, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao