CAS: 1202757-89-8; N-(3-((5-Fluoro-2-((4-(2-Methoxyethoxy)Phenyl)Amino)Pyrimidin-4-yl)Amino)Phenyl)Acrylamide

该化合物是一个小分子,在医学化学领域引起注意,特别是其治疗各种血液恶性肿瘤和自体免疫疾病的潜在治疗应用.作为BTK抑制器,AVL-292通过干扰对B细胞生存和扩散至关重要的信号路径而起作用,而B细胞经常卷入这些条件.该化合物的特点是它能够有选择地与BTK酶结合,从而抑制其活动,而不会显著影响其他血管,从而有助于最大限度地减少目标外效应.AVL-292进行了各种临床和临床研究,以评估其功效和安全特征.其致癌性特性,包括吸收,分布,代谢和排泄,对于确定其治疗潜力至关重要.

结构式图片

上下游产品

CAS号1202759-91-8 N4-(3-氨基苯基)-5-氟... | CAS号814-68-6 丙烯酰氯

合成工艺路线路线简述

    Tert-Butyl (3-((2-Chloro-5-Fluoropyrimidin-4-yl)Amino)Phenyl)Carbamate置于对甲苯磺酸,三氟乙酸体系中,用 乙醇,二氯甲烷 用作溶剂,化学反应 28.67H,反应生成N-[3-[[5-氟-2-[[4-(2-甲氧基乙氧基)苯基]氨基]-4-嘧啶基]氨基]苯基]-2-丙烯酰胺
    参考文献:Heteroaryl Compounds And Uses Thereof
    标题:Heteroaryl Compounds And Uses Thereof
    摘要:本发明提供了化合物,药学上可接受的组合物以及使用它们的方法.

    海关参考信息

    专利信息


    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-9278919-B1
    优先权日:2015-03-13
    标题:Synthesis of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
    发明人:XU YONG
    权利人:XU YONG
    摘要:A method for preparing BTK inhibitor CC-292 of formula 1, comprising: (1) contacting a compound of formula 2 with a compound of formula 3 to obtain a compound of formula 4; (2) contacting the compound of formula 4 with a compound of formula 5 to obtain a compound of formula 6; (3) contacting the compound of formula 6 with trifluoromethanesulfonic anhydride to obtain a compound of formula 7; and (4) contacting the compound of formula 7 with a compound of formula 8 to obtain the compound of formula 1,

    专利号:US-12441733-B2
    优先权日:2018-03-26
    标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
    发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
    权利人:NOVARTIS AG
    摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    专利号:CN-118922420-A
    优先权日:2022-03-25
    标题 :Synthesis of TYK2 inhibitors and their intermediates
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    主要参考文献


    1: Burger JA. Bruton's tyrosine kinase (BTK) inhibitors in clinical trials. Curr Hematol Malig Rep. 2014 Mar;9(1):44-9. doi: 10.1007/s11899-013-0188-8.

    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.
    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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