CAS: 648449-76-7; 5-((2,2-Difluorobenzo[d][1,3]Dioxol-5-yl)Methylene)Thiazolidine-2,4-Dione

该化合物是属于硫氨碘酮类的合成有机化合物,众所周知,硫氨碘酮类在药理学中,特别是在糖尿病治疗中具有作用;该化合物具有硫磺碘酮核心特征,其特点是五人环,含有硫和氮,与一种有助于其独特特性的苯二酚混合物结合;二氟二氮基聚物的存在增强了其脂性,可能会影响其生物活动;该化合物通常因其对葡萄糖代谢和胰岛素敏感度的潜在影响而进行研究,使其对糖尿病研究感兴趣;该化合物的结构复杂性表明,它可能表现出与生物目标的具体相互作用,可能导致治疗用途;与许多合成化合物一样,其稳定性,溶解性和再活性可能因环境条件和其他物质的存在而有所不同;安全性和处理防范措施应当受到观察,因为其化学性质.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    海关参考信息

    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.

    专利号:WO-2024213057-A1
    优先权日:2023-04-12
    标题:Use of combination of lsd1 inhibitor and drug to treat cancer
    发明人:LIU HONG; LI JIA; HUANG HE; WANG JIANG; ZHOU YUBO; REN XUELIAN; LI CHUNPU; KAN WEIJUAN; XU ZICHAO; HU XIAOBEI; WU HENGBO; WANG HANLIN; YE YUNFEI; QIU XIAOHUI; SU MINGBO
    权利人:SHANGHAI INST MATERIA MEDICA CAS
    摘要:A use of a combination of an LSD1 inhibitor and a drug to treat cancer. Specifically, provided is a composition comprising: a tranylcypromine compound and/or a derivative thereof; and a drug selected from a kinase inhibitor, an anti-cancer drug acting upon or affecting the DNA, an antiviral compound, an antihypertension compound, an antidiabetic compound, a JAK-STAT signaling pathway inhibitor, an NF-κB signaling pathway inhibitor, a protein synthesis inhibitor, a 5-hydroxytryptamine receptor agonist, a dystroglycan modulator, a GABA receptor modulator, or a combination thereof. The two active ingredients have a synergistic effect, and the synergistic treatment effect is significantly better than that of the two individually, thereby remarkably improving the cancer treatment effect.
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    主要参考文献


    1: Li H, Park D, Abdul-Muneer PM, Xu B, Wang H, Xing B, Wu D, Li S. PI3Kγ inhibition alleviates symptoms and increases axon number in experimental autoimmune encephalomyelitis mice. Neuroscience. 2013 Dec 3;253:89-99. doi: 10.1016/j.neuroscience.2013.08.051. Epub 2013 Sep 3. doi: 10.1016/j.biocel.2012.07.009. Epub 2012 Jul 17. doi: 10.1073/pnas.1009652107. Epub 2010 Aug 16.
    4: Hasan AM, Mourtada-Maarabouni M, Hameed MS, Williams GT, Dent G. Phosphoinositide 3-kinase gamma mediates chemotactic responses of human eosinophils to platelet-activating factor. Int Immunopharmacol. 2010 Sep;10(9):1017-21. doi: 10.1016/j.intimp.2010.05.014. Epub 2010 Jun 4. doi: 10.1016/j.jhep.2010.05.015. Epub 2010 Jul 17.
    6: Camps M, Rückle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Françon B, Martin T, Gretener D, Perrin D, Leroy D, Vitte PA, Hirsch E, Wymann MP, Cirillo R, Schwarz MK, Rommel C. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
    参考文献:10.1016/j.jhep.2010.05.015
    摘要:Hohenester S, Gates A, Wimmer R, Beuers U, Anwer MS, Rust C, Webster CRL. Phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. Journal of Hepatology. 2010 Nov;53(5):918–26. doi: 10.1016/j.jhep.2010.05.015.
    参考文献:10.1016/j.intimp.2010.05.014
    摘要:Hasan AM, Mourtada-Maarabouni M, Hameed MS, Williams GT, Dent G. Phosphoinositide 3-kinase gamma mediates chemotactic responses of human eosinophils to platelet-activating factor. Int Immunopharmacol. 2010 Sep;10(9):1017–21. doi: 10.1016/j.intimp.2010.05.014.
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