CAS: 944118-01-8; Anti-4-((5-Hydroxyadamantan-2-yl)Amino)-1H-Pyrrolo[2,3-B]Pyridine-5-Carboxamide

该化合物是 Janus kinase (JAK) 抑制剂,主要用于治疗风湿性关节炎(RA),有选择地针对JAK1,JAK2和JAK3, 调控用于炎症和免疫反应的细胞基质信号路径,它的口腔生物利用率和一次日服剂量疗法为病人提供了方便.临床研究表明,它在减少RA症状和减缓疾病蔓延方面,特别是在对常规疗法反应不力的病人中,效果有效.Peficitinib 的精明化药效活性药动因特征和可管理的安全特征使其成为可行的治疗选择.它的行动机制与其他JAK抑制剂相匹配,但其独特的选择性可能促成不同的临床结果.

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    专利信息


    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-12390420-B1
    优先权日:2024-10-22
    标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
    发明人:EGUCHI MASAKATSU
    权利人:BRYET US INC
    摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2025161441-A1
    优先权日:2022-02-25
    标 题 :Medicine comprising combination of anti-mutant-calr antibody and another drug
    发明人:KOMATSU NORIO; ISHIDA YOJI; ARAKI MARITO; TSUCHIYA TOSHIYUKI; CHIKADA Tsubasa; IMAI MISA; FUKASAWA HIROSHI
    权利人:JUNTENDO EDUCATIONAL FOUND; MEIJI SEIKA PHARMA CO LTD
    摘要:A pharmaceutical which exhibits sufficient anticancer effects by using an antibody which binds to a mutant CALR protein and another anticancer agent in combination. A pharmaceutical for preventing and/or treating a cancer, including an antibody which specifically binds to a mutant calreticulin protein or a functional fragment thereof and a drug selected from the group consisting of an alkylating agent, a platinum preparation, an antimetabolite, a ribonucleotide reductase inhibitor, a nucleotide analog, a topoisomerase inhibitor, a microtubule polymerization inhibitor, an antitumor antibiotic, an interferon, a cytokine preparation, a molecular targeting drug, a nucleic acid synthesis inhibitor, a jak inhibitor, and a cancer immunotherapeutic agent in combination.

    专利号:US-2018230127-A1
    优先权日:2015-08-13
    标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
    发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

    专利号:US-2023119606-A1
    优先权日:2020-02-18
    标 题:Immune cell modulators
    发明人:SHERDEN NATHANIEL; YU SHEN; STONER ISAAC
    权利人:OCTAGON THERAPEUTICS INC
    摘要:Disclosed are immune cell-selective small molecule compounds that modulate certain immune cell-specific receptors and enzymes, and methods of their synthesis and use to treat proliferative disorders.

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    主要参考文献


    1: Ouranos K, Avila DV, Mylona EK, Vassilopoulos A, Vassilopoulos S, Shehadeh F, Mylonakis E. Cumulative incidence and risk of infection in patients with rheumatoid arthritis treated with janus kinase inhibitors: A systematic review and meta-analysis. PLoS One. 2024 Jul 31;19(7):e0306548. doi: 10.1371/journal.pone.0306548.
    2: Chandrashekara S. Pharmacokinetic review of janus kinase inhibitors and its clinical implications for the management of rheumatoid arthritis. Expert Opin Drug Metab Toxicol. 2024 Jun
    26:1-8. doi: 10.1080/17425255.2024.2373092. Epub ahead of print. 19(6):e0305621. doi: 10.1371/journal.pone.0305621.

    合成参考文献


    参考文献:10.1007/s00894-020-04512-3
    摘要:Pery N, Rizvi NB, Shafiq MI. Development of piperidinyl dipyrrrolopyridine-based dual inhibitors of Janus kinase and Bruton’s tyrosine kinase: a potential therapeutic probability to deal with rheumatoid arthritis. Journal of Molecular Modeling. 2020 Aug 17;26(9):235. doi: 10.1007/s00894-020-04512-3.
    参考文献:10.1038/s41584-021-00665-4
    摘要:Noack M, Miossec P. Importance of lymphocyte-stromal cell interactions in autoimmune and inflammatory rheumatic diseases. Nat Rev Rheumatol. 2021 Sep;17(9):550–64. doi: 10.1038/s41584-021-00665-4.
    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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