CAS: 934353-76-1; (E)-N-(5-Methyl-1H-Pyrazol-3-yl)-6-(4-Methylpiperazin-1-yl)-2-Styrylpyrimidin-4-Amine

该化合物是一个小分子,主要因其潜在的治疗应用,特别是在肿瘤学领域,受到调查,被归类为某些有选择的抑制性动脉,在细胞信号路径中发挥着关键作用,调节细胞生长和扩散;该化合物在临床前研究中显示出其抑制肿瘤生长和在癌症细胞中诱发人口中毒的能力的希望;ENMD-2076的特点是它与目标动脉有具体结合,这可能有助于其破坏癌症细胞信号的效果;此外,还评估了它的药理动力特性,包括吸收,分布,代谢和排泄(ADME),这对于确定其是否适合作为治疗剂至关重要;与许多研究药物一样,正在进行的研究旨在进一步阐明其行动机制,优化其配制,并评估其在临床环境中的安全性和有效性.

结构式图片

合成工艺路线路线简述

  • 934353-75-0 = 934353-76-1
    反应条件:1.1 Reagents: Lithium Aluminum Hydride Solvents: Tetrahydrofuran; 0 °C; 12 H,0 °C -> Rt; Rt -> 0 °C1.2 Reagents: Methanol
    标题:Preparation Of Substituted Pyrazole Compounds As Protein Kinase Inhibitors
    参考文献:World Intellectual Property Organization
📜6-(4-Methylpiperazin-1-yl)-N-(3-Methyl-1H-Pyrazol-5-yl)-2-(Phenylethynyl)Pyrimidin-4-Amine置于lithium Aluminium Tetrahydride,Potassium Tartrate体系中,用 四氢呋喃,甲醇,水 作为反应溶剂,化学反应 12.0H,以61%的收率获得产物6-(4-甲基-1-哌嗪基)-N-(5-甲基-1H-吡唑-3-基)-2-[(1E)-2-苯乙烯基]-4-嘧啶胺
参考文献: Substituted Pyrazole Compounds[fr] Composes Pyrazole Substitues
标题: Substituted Pyrazole Compounds[fr] Composes Pyrazole Substitues

海关参考信息

专利信息


专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

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-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

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: Shiomitsu K, Sajo E, Rubin C, Sehgal I. The radiosensitizing effect of the aurora kinase inhibitors, ENMD-2076, on canine mast cell tumours in vitro. Vet Comp Oncol. 2013 Jun 13. doi: 10.1111/vco.12046. [Epub ahead of print]
2: Diamond JR, Eckhardt SG, Tan AC, Newton TP, Selby HM, Brunkow KL, Kachaeva MI, Varella-Garcia M, Pitts TM, Bray MR, Fletcher GC, Tentler JJ. Predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor ENMD-2076 in preclinical breast cancer models. Clin Cancer Res. 2013 Jan 1;19(1):291-303. doi: 10.1158/1078-0432.CCR-12-1611. Epub 2012 Nov 7.
3: Cao H, Li M, Qian WB. [Killing effect of aurora kinase inhibitor ENMD-2076 on acute myelogenous leukemia cells]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2012 Sep;41(5):479-84. Chinese. doi: 10.1016/j.ejca.2012.07.020. Epub 2012 Aug 21. doi: 10.1517/13543784.2012.668882. Epub 2012 Mar 8. Review. doi: 10.1517/13543784.2011.584869. Epub 2011 May 26. Review. doi: 10.1158/1535-7163.MCT-10-0574. Epub 2010 Dec 21. doi: 10.1158/1078-0432.CCR-10-2144. Epub 2010 Dec 3.

合成参考文献


参考文献:10.1517/13543784.2011.584869
摘要:Zhang S, Farag SS. From cell biology to therapy: ENMD-2076 in the treatment of multiple myeloma. Expert Opinion on Investigational Drugs. 2011 May 26;20(7):1015–28. doi: 10.1517/13543784.2011.584869.
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