CAS: 1369761-01-2; 4-(Cyclopropylamino)-2-((4-(4-(Ethylsulfonyl)Piperazin-1-yl)Phenyl)Amino)Pyrimidine-5-Carboxamide Hydrochloride

该化合物是一种SYK/JAK 脂酶抑制剂,在肿瘤学,特别是血解恶性肿瘤方面可能具有治疗用途,其行动机制包括针对B细胞受体(BCR)和细胞受体(cytokine)信号中涉及的关键信号路径,这些路径对于某些癌症细胞的生存和扩散至关重要;盐酸盐形式增加了溶解性和生物利用率,有利于配方和管理;临床研究显示,锡酸盐表现出对SYK和JAK家庭血清的强大抑制性活动,为针对抗药性或耐性疾病提供了有希望的方法;其选择性特征可以减少非目标效应,支持临床环境的进一步调查.

结构式图片

上下游产品

2,4-dihydroxypyrimidine-5-carboxylic acid 2,4-dichloropyrimidine-5-carbonyl chloride 2,4-dichloro-pyrimidine-5-carboxylic acid amide 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester

合成工艺路线路线简述

    📜赛度替尼置于盐酸体系中,用 异丙醇 用作溶剂,化学反应 18.0H,反应生成Cerdulatinib盐酸盐
    参考文献:Wo2019213606A5
    标题:Wo2019213606A5

    海关参考信息

    专利信息


    专利号:US-11339145-B2
    优先权日:2018-05-04
    标题 :Synthesis of cerdulatinib
    发明人:PANDEY ANJALI; SRAN ARVINDER; CHEN YING; POGGIALI DANIELE; FUMAGALLI TIZIANO
    权利人:ALEXION PHARMA INC
    摘要:The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I:or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.

    专利号:US-2019337930-A1
    优先权日:2018-05-04
    标 题 :Synthesis of cerdulatinib

    专利号:US-2021147392-A1
    优先权日:2018-05-04
    标 题:Synthesis of cerdulatinib

    专利号:JP-7343526-B2
    优先权日:2018-05-04
    标 题 :Synthesis of cerdulatinib

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Traidl S, Freimooser S, Werfel T. Janus kinase inhibitors for the therapy of atopic dermatitis. Allergol Select. 2021 Aug 27;5:293-304. doi: 10.5414/ALX02272E.
    2: Montilla AM, Gómez-García F, Gómez-Arias PJ, Gay-Mimbrera J, Hernández-Parada J, Isla-Tejera B, Ruano J. Scoping Review on the Use of Drugs Targeting JAK/STAT Pathway in Atopic Dermatitis, Vitiligo, and Alopecia Areata. Dermatol Ther (Heidelb). 2019 Dec;9(4):655-683. doi: 10.1007/s13555-019-00329-y. Epub 2019 Oct 13.
    3: Coffey GP, Feng J, Betz A, Pandey A, Birrell M, Leeds JM, Der K, Kadri S, Lu P, Segal J, Wang YL, Michelson G, Curnutte JT, Conley PB. Cerdulatinib Pharmacodynamics and Relationships to Tumor Response Following Oral Dosing in Patients with Relapsed/Refractory B-cell Malignancies. Clin Cancer Res. 2019 Feb 15;25(4):1174-1184. doi: 10.1158/1078-0432.CCR-18-1047. Epub 2018 Oct 17. 6(41):43881-96. doi: 10.18632/oncotarget.6316.

    合成参考文献


    参考文献:10.1186/s43141-023-00577-8
    摘要:Akinnusi PA, Olubode SO, Adebesin AO, Alade AA, Nwoke VC, Shodehinde SA. Optimal molecular binding data and pharmacokinetic profiles of novel potential triple-action inhibitors of chymase, spleen tyrosine kinase, and prostaglandin D2 receptor in the treatment of asthma. Journal of Genetic Engineering and Biotechnology. 2023 Dec;21(1):113. doi: 10.1186/s43141-023-00577-8.
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