CAS: 209410-46-8; 5-(2,6-Dichlorophenyl)-2-((2,4-Difluorophenyl)Thio)-6H-Pyrimido[1,6-B]Pyridazin-6-One

该化合物是合成有机化合物,其特点是复杂的循环结构,具有合成有机化合物,其特征是:一种火水化合物和pyridazine核心,有助于其潜在的生物活动;二氯苯和二氟苯组的存在表明,它具有重大的卤化作用,能够增强对化合物与生物目标的相互作用产生影响.硫醚联系在结构中引入硫磺,有可能影响其再活动性和溶解性.这种化合物可能表现出药用特性,从而引起对医药化学的兴趣,特别是在开发新的治疗剂方面.其具体特性,例如熔点,溶性,溶性以及光谱数据,通常通过实验方法来确定.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    2,6-二氯苯乙腈置于peppsitm-Ipr 硫酸,Potassium Tert-Butylate,Sodium T-Butanolate体系中,用 甲苯 用作溶剂,化学反应 23.0H,反应生成5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-B]哒嗪-6-酮
    参考文献:Rapid Synthesis Of Vx-745: P38 Map Kinase Inhibition In Werner Syndrome Cells
    标题:Rapid Synthesis Of Vx-745: P38 Map Kinase Inhibition In Werner Syndrome Cells
    摘要:The P38 Mitogen-Activated Protein Kinase Inhibitor Vx-745 Is Prepared Rapidly And Efficiently In A Four-Step Sequence Using A Combination Of Conductive Heating And Microwave-Niediated Steps. Its Inhibitory Activity Was Confirmed In Htert Immortalized Hca2 And Ws Dermal Fibroblasts At 0.5-1.0 Mu M Concentration By Elisa And Immunoblot Assay,And Displays Excellent Kinase Selectivity Over The Related Stress-Activated Kinase Jnk. (C) 2007 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2007.07.016

    海关参考信息

    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-12006337-B2
    优先权日:2018-05-30
    标题:Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof
    发明人:HOLTZMAN MICHAEL J; ROMERO ARTHUR G; GEROVAC BENJAMIN J; HAN ZHENFU; KEELER SHAMUS P; WU KANGYUN; ZHANG YONG
    权利人:WASHINGTON UNIVERSITY ST LOUIS
    摘要:Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutically for a variety of diseases, including cancer and respiratory diseases. Methods of synthesis of the compounds are also disclosed.

    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:US-2022143183-A1
    优先权日:2019-02-23
    标题:Photoswitchable protacs and synthesis and uses thereof
    发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE
    权利人:UNIV NEW YORK
    摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.

    专利号:CN-108821968-A
    优先权日:2018-06-28
    标题:Preparation method of in-situ acid resin catalyzed synthesis of higher carbon alkyl acrylate

    专利号:CN-111575006-A
    优先权日:2020-03-11
    标 题 :A kind of alloy quantum dot synthesis method
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    主要参考文献


    1: Davis T, Brook AJ, Rokicki MJ, Bagley MC, Kipling D. Evaluating the Role of p38 MAPK in the Accelerated Cell Senescence of Werner Syndrome Fibroblasts. Pharmaceuticals (Basel). 2016 Apr 28;9(2). pii: E23. doi: 10.3390/ph9020023. doi: 10.3233/JAD-150277. doi: 10.1016/j.ejpb.2015.03.017. Epub 2015 Mar 30. doi: 10.1128/MCB.01691-12. Epub 2013 Aug 26.
    5: Tsai YR, Wang YJ, Lee MR, Hsu MF, Wang JP. p38 Mitogen-activated protein kinase and extracellular signal-regulated kinase signaling pathways are not essential regulators of formyl peptide-stimulated p47(phox) activation in neutrophils. Eur J Pharmacol. 2013 Feb 15;701(1-3):96-105. doi: 10.1016/j.ejphar.2013.01.003. Epub 2013 Jan 21. doi: 10.1107/S090744491201997X. Epub 2012 Jul 17. doi: 10.1021/ml2001455. eCollection 2011 Oct 13.
    8: Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13. doi: 10.1016/j.chembiol.2011.01.015. doi: 10.4155/fmc.10.217. doi: 10.1016/j.intimp.2010.01.007. Epub 2010 Jan 20. doi: 10.1021/jo9017155. doi: 10.1002/art.24264. doi: 10.1186/1476-9255-5-22.
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