CAS: 1403254-99-8; N-((4,6-Dimethyl-2-Oxo-1,2-Dihydropyridin-3-yl)Methyl)-5-(Ethyl(Tetrahydro-2H-Pyran-4-yl)Amino)-4-Methyl-4'-(Morpholinomethyl)-[1,1'-Biphenyl]-3-Carboxamide

该化合物是以其化学名称而著称的,是一个小分子抑制剂,主要针对的是酶EZH2(Zeste同族体2的增生器),这是聚氯抑制综合体2(PRC2)的一个关键组成部分.该复合体在肿瘤学中具有潜在的治疗用途,特别是在治疗以突变为EZH2基因特征的某些类型的癌症方面.EPZ-6438展示了EZH2的选择性抑制剂,导致因淋巴27(H3K27me3)的丙酮H3甲基化而沉默的肿瘤抑制基因的恢复.该复合体在临床前和临床环境中进行了研究,展示了淋巴瘤和其他恶性肿瘤模型的功效,其药理学特征包括有利的生物利用率和可管理的安全特征,使其成为目标癌症疗法进一步发展的候选体.与任何调查药物一样,进行中的研究对于充分阐明其行动机制,治疗潜力和任何相关副作用至关重要.

结构式图片

物理性质

MSDS等安全信息

上下游产品

Tetrahydro-4H-pyran-4-one 5-bromo-2-methyl-3-nitro-benzoic acid 5-bromo-2-methyl-3-nitrobenzoic acid methyl ester 2-methyl-3-nitrobenzic acidN-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)[1,1'-biphenyl]-3-carboxamide hydrobromide N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-thiopyran-4-yl)amino)-4,4'-dimethyl-[1,1'-biphenyl]-3-carboxamide

合成工艺路线路线简述

  • 合成目标产物 Tazemetostat (Epz-6438) 主要起始原料 5-Bromo-N-((4,6-Dimethyl-2-Oxo-1,2-Dihydropyridin-3-yl)Methyl)-3-(Ethyl(Tetrahydro-2H-Pyran-4-yl)Amino)-2-Methylbenzamide And 4-[4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Benzyl]Morpholine
  • (文献来源)合成步骤主要原料 5-Bromo-N-((4,6-Dimethyl-2-Oxo-1,2-Dihydropyridin-3-yl)Methyl)-3-(Ethyl(Tetrahydro-2H-Pyran-4-yl)Amino)-2-Methylbenzamide 和 4-[4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Benzyl]Morpholine
📜2-甲基-3-硝基苯甲酸置于1,3-二溴-5,5-二甲基海因,硫酸,水,铁粉,Sodium Carbonate,氯化铵,溶剂黄146,Sodium Hydroxide体系中,用 1,4-二氧六环,乙醇,水,二甲基亚砜,1,2-二氯乙烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 34.2H,反应生成N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-5-[乙基(四氢-2H-吡喃-4-基)氨基]-4-甲基-4'-(4-吗啉基甲基)-[1,1'-联苯]-3-甲酰胺
参考文献: Combination Therapy For Treating Cancer[fr] Polythérapie Anticancéreuse
标题: Combination Therapy For Treating Cancer[fr] Polythérapie Anticancéreuse
摘要:本发明涉及包含人类组蛋白甲基转移酶ezh2抑制剂和一种或多种其他治疗药物的组合物,特别是抗癌药物如泼尼松,以及用于治疗癌症的组合治疗方法,用于给予需要的受试者.

海关参考信息

专利信息


专利号:WO-2024115549-A1
优先权日:2022-11-30
标题:Aryl- and heteroaryl-sulfonamide derivatives as ccr8 modulators
发明人：AISSAOUI HAMED; CORMINBOEUF OLIVIER; DIETHELM STEFAN; REMEN LUBOS; RICHARD-BILDSTEIN SYLVIA
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR8 receptor modulators in medicine.

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主要参考文献


1: Xia C, Liu J, Hu L, Chen J, Zhang L. Post-Marketing Safety of Tazemetostat in Antitumor Therapy: A Real-World Pharmacovigilance Study of the FDA Adverse Event Reporting System. Cancer Invest. 2025 Dec
19:1-9. doi: 10.1080/07357907.2025.2598038. Epub ahead of print. 9(1):331. doi: 10.1038/s41698-025-01113-2.
3: Cao J, Chen G, Qiu L, Zhang L, Jiang M, Cheng Y, Zhang Q, Liu L, Li P, Shuang Y, Wang H, Xue H, Wu H, Zheng M, Zhou K, Li Z, Jing H, Yang W, Zhu Z, Li W, Wangwu J, Huang H, Jia Q, Chen D, Fan S, Shi MM, Su W. Efficacy and safety of tazemetostat, an EZH2 inhibitor, in Chinese patients with relapsed/refractory follicular lymphoma: a multicentre, single-arm, phase 2 study. EClinicalMedicine. 2025 Aug 18;87:103399. doi: 10.1016/j.eclinm.2025.103399.

合成参考文献


参考文献:10.1016/j.bbrc.2019.06.093
摘要:Chen J, Chen X, Yao J, Li M, Yang X. The combination of Decitabine and EPZ-6438 effectively facilitate adipogenic differentiation of induced pluripotent stem cell-derived mesenchymal stem cells. Biochemical and Biophysical Research Communications. 2019 Aug;516(1):307–12. doi: 10.1016/j.bbrc.2019.06.093.
参考文献:10.1038/s41568-020-0288-4
摘要:Nacev BA, Jones KB, Intlekofer AM, Yu JSE, Allis CD, Tap WD, Ladanyi M, Nielsen TO. The epigenomics of sarcoma. Nature Reviews Cancer. 2020 Aug 11;20(10):608–23. doi: 10.1038/s41568-020-0288-4.
参考文献:10.1186/s13045-022-01249-9
摘要:Zhuang Y, Che J, Wu M, Guo Y, Xu Y, Dong X, Yang H. Altered pathways and targeted therapy in double hit lymphoma. Journal of Hematology & Oncology. 2022 Mar 18;15(1):26. doi: 10.1186/s13045-022-01249-9.
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