CAS: 761439-42-3; 5-Chloro-N4-(2-(Isopropylsulfonyl)Phenyl)-N2-(2-Methoxy-4-(4-(4-Methylpiperazin-1-yl)Piperidin-1-yl)Phenyl)Pyrimidine-2,4-Diamine

该化合物是一种合成有机化合物,其结构复杂,包括多种功能组,如管状素和管状松脂,丙胺核心和磺酰胺组.该化合物一般被归类为小分子,可能具有与药用化学有关的特性,特别是在药物开发方面.其结构特征表明与生物目标可能发生相互作用,使其在药用研究中引起兴趣.氯和甲氧基化合物的存在可能会影响其溶性,稳定性和生物活动.与这一类别中的许多化合物一样,其功效和安全特征需要通过临床前期和临床研究的严格测试来评估.

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物理性质

MSDS等安全信息

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    专利信息


    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.

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    主要参考文献


    1: Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, Gray NS, Warmuth M. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. doi: 10.1073/pnas.0609412103. Epub 2006 Dec 21. Erratum in: Proc Natl Acad Sci U S A. 2007 Feb 6;104(6):2025.
    2: McDermott U, Iafrate AJ, Gray NS, Shioda T, Classon M, Maheswaran S, Zhou W, Choi HG, Smith SL, Dowell L, Ulkus LE, Kuhlmann G, Greninger P, Christensen JG, Haber DA, Settleman J. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res. 2008 May 1;68(9):3389-95. doi: 10.1158/0008-5472.CAN-07-6186. 14(13):4275-83. doi: 10.1158/1078-0432.CCR-08-0168.
    4: George RE, Sanda T, Hanna M, Fröhling S, Luther W 2nd, Zhang J, Ahn Y, Zhou W, London WB, McGrady P, Xue L, Zozulya S, Gregor VE, Webb TR, Gray NS, Gilliland DG, Diller L, Greulich H, Morris SW, Meyerson M, Look AT. Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature. 2008 Oct 16;455(7215):975-8. doi: 10.1038/nature07397.

    合成参考文献


    参考文献:10.1186/1471-2407-12-612
    摘要:Jokinen E, Laurila N, Koivunen JP. Alternative dosing of dual PI3K and MEK inhibition in cancer therapy. BMC Cancer. 2012 Dec 21;12():612.
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