Title:
AMIDE COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/111499
Kind Code:
A1
Abstract:
Provided in the present application are an amide compound, and an isomer, a pharmaceutically acceptable salt, and a pharmaceutical composition thereof, and the use thereof. The amide compound has a structure as represented by formula I. The amide compound of the present application has a significant JAK kinase inhibitory activity, especially a JAK1 kinase inhibitory activity, has a higher inhibitory activity on JAK1 kinase than on JAK2 kinase, and can be used as a highly selective JAK1 kinase inhibitor. Therefore, the amide compound of the present application can be used for preparing drugs for treating JAK1 kinase-mediated diseases.
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Inventors:
HUANG LIYE (CN)
LI HUA (CN)
LIU HUABIN (CN)
WANG ZHIYUAN (CN)
LI TAO (CN)
OUYANG FEIYAN (CN)
ZHANG XINMIAO (CN)
LI HUA (CN)
LIU HUABIN (CN)
WANG ZHIYUAN (CN)
LI TAO (CN)
OUYANG FEIYAN (CN)
ZHANG XINMIAO (CN)
Application Number:
PCT/CN2021/132652
Publication Date:
June 02, 2022
Filing Date:
November 24, 2021
Export Citation:
Assignee:
SHENZHEN BO LI JIAN MEDICINE CO LTD (CN)
International Classes:
A61K31/506; C07D403/14; A61P11/06; A61P37/00
Domestic Patent References:
| WO2020211839A1 | 2020-10-22 |
Other References:
HAMMAREN H. M. ET AL.: "The regulation of JAKs in cytokine signaling and its breakdown in disease", CYTOKINE, vol. 118, 2019, pages 48 - 63
O'SHEA J. J. ET AL.: "The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention", ANNUAL REVIEW OF MEDICINE, vol. 66, 2015, pages 311 - 328, XP055536085, DOI: 10.1146/annurev-med-051113-024537
BERTSIAS G.: "Therapeutic targeting of JAKs: from hematology to rheumatology and from the first to the second generation of JAK inhibitors", MEDITERRANEAN JOURNAL OF RHEUMATOLOGY, vol. 31, 2020, pages 105 - 111
TAYLOR P. C.: "Clinical efficacy of launched JAK inhibitors in rheumatoid arthritis", RHEUMATOLOGY, vol. 58, 2019, pages i17 - i26, XP055801975, DOI: 10.1093/rheumatology/key225
KEYSTONE E. C. ET AL.: "Safety and efficacy of baricitinib at 24 weeks in patients with rheumatoid arthritis who have an inadequate response to methotrexate", ANNALS OF THE RHEUMATIC DISEASES, vol. 74, 2015, pages 333 - 340
VIRTANEN A. T. ET AL.: "Selective JAKinibs: Prospects in Infammatory and Autoimmune Diseases", BIODRUGS, vol. 33, 2019, pages 15 - 32
PARMENTIER J. M. ET AL.: "In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494", BMC RHEUMATOLOGY, vol. 2, 2018, pages 23
VAN ROMPAEY L. ET AL.: "Preclinical Characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases", JOURNAL OF IMMUNOLOGY, vol. 191, 2013, pages 3568 - 3577, XP055272590, DOI: 10.4049/jimmunol.1201348
MENET C. J. ET AL.: "Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, 2014, pages 9323 - 9342, XP055272599, DOI: 10.1021/jm501262q
"Remington's Pharmaceutical Sciences", 1985, MACK PUBLISHING COMPANY, pages: 1418
JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 66, 1977, pages 2
T. HIGUCHIV STELLA: "A.C.S. Symposium Series and Bioreversible Carriers in Drug Design", vol. 14, 1987, AMERICAN PHARMACEUTICAL ASSOCIATION AND PERGAMON PRESS, article "Pro-drugs as Novel Delivery Systems"
O'SHEA J. J. ET AL.: "The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention", ANNUAL REVIEW OF MEDICINE, vol. 66, 2015, pages 311 - 328, XP055536085, DOI: 10.1146/annurev-med-051113-024537
BERTSIAS G.: "Therapeutic targeting of JAKs: from hematology to rheumatology and from the first to the second generation of JAK inhibitors", MEDITERRANEAN JOURNAL OF RHEUMATOLOGY, vol. 31, 2020, pages 105 - 111
TAYLOR P. C.: "Clinical efficacy of launched JAK inhibitors in rheumatoid arthritis", RHEUMATOLOGY, vol. 58, 2019, pages i17 - i26, XP055801975, DOI: 10.1093/rheumatology/key225
KEYSTONE E. C. ET AL.: "Safety and efficacy of baricitinib at 24 weeks in patients with rheumatoid arthritis who have an inadequate response to methotrexate", ANNALS OF THE RHEUMATIC DISEASES, vol. 74, 2015, pages 333 - 340
VIRTANEN A. T. ET AL.: "Selective JAKinibs: Prospects in Infammatory and Autoimmune Diseases", BIODRUGS, vol. 33, 2019, pages 15 - 32
PARMENTIER J. M. ET AL.: "In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494", BMC RHEUMATOLOGY, vol. 2, 2018, pages 23
VAN ROMPAEY L. ET AL.: "Preclinical Characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases", JOURNAL OF IMMUNOLOGY, vol. 191, 2013, pages 3568 - 3577, XP055272590, DOI: 10.4049/jimmunol.1201348
MENET C. J. ET AL.: "Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, 2014, pages 9323 - 9342, XP055272599, DOI: 10.1021/jm501262q
"Remington's Pharmaceutical Sciences", 1985, MACK PUBLISHING COMPANY, pages: 1418
JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 66, 1977, pages 2
T. HIGUCHIV STELLA: "A.C.S. Symposium Series and Bioreversible Carriers in Drug Design", vol. 14, 1987, AMERICAN PHARMACEUTICAL ASSOCIATION AND PERGAMON PRESS, article "Pro-drugs as Novel Delivery Systems"
Attorney, Agent or Firm:
BEYOND ATTORNEYS AT LAW (CN)
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