CAS: 1415823-73-2; 1-(4-(((6-Amino-5-(4-Phenoxyphenyl)Pyrimidin-4-yl)Amino)Methyl)Piperidin-1-yl)Prop-2-En-1-One
该化合物是用于治疗自动免疫疾病,特别是多发性硬化症(MS)的高度选择性,小分子布鲁顿(BTK)抗体抑制剂. 它的主要优势在于其共价约束机制,它确保了持续的目标接触和长期的药理动力效应. Evobrutib表现出了高度的能量和特质,最大限度地减少了目标外的相互作用并减少了潜在的不利影响. 临床和临床研究已经证明它有能力调节B细胞和近距离细胞信号,解决了自动免疫病理学的关键路径. 该化合物的有利药用植物特征,包括口腔生物利用率和血液阻隔热作用,进一步支持了其治疗潜力. Evobrutinib是免疫中性障碍的有希望的调查剂.
- 英文名称1-(4-(((6-Amino-5-(4-Phenoxyphenyl)Pyrimidin-4-yl)Amino)Methyl)Piperidin-1-yl)Prop-2-En-1-One
- 中文名称依伏替尼
- IUPAC名称1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one
- 其它别名1-(4-(((6-Amino-5-(4-Phenoxyphenyl)-4-Pyrimidinyl)Amino)Methyl)-1-Piperidinyl)-2-Propen-1-One; 1-[4-[[[6-Amino-5-(4-Phenoxyphenyl)-4-Pyrimidinyl]Amino]Methyl]-1-Piperidinyl]-2-Propen-1-One; Ev
- CAS编号1415823-73-2
- MFCD编号:MFCD30502975
- EINECS号:853-472-2
- FDA UNII编号:ZA45457L1K
- 分子式:C25H27N5O2分子量:429.52
- 产品CID: 635026
- 产品分类Protein Tyrosine Kinase/RTK → BTK
物理性质
MSDS等安全信息
欧盟法规
C&L通报合成工艺路线路线简述
海关参考信息
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专利信息
专利号:WO-2025101716-A1
优先权日:2023-11-07
标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds
发明人：LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH
权利人:H LEE MOFFITT CANCER CT & RES
摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes described.
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主要参考文献
1: Montalban X, Vermersch P, Arnold DL, Bar-Or A, Cree BAC, Cross AH, Kubala Havrdova E, Kappos L, Stuve O, Wiendl H, Wolinsky JS, Dahlke F, Le Bolay C, Shen Loo L, Gopalakrishnan S, Hyvert Y, Javor A, Guehring H, Tenenbaum N, Tomic D; evolutionRMS investigators. Safety and efficacy of evobrutinib in relapsing multiple sclerosis (evolutionRMS1 and evolutionRMS2): two multicentre, randomised, double-blind, active-controlled, phase 3 trials. Lancet Neurol. 2024 Nov;23(11):1119-1132. doi: 10.1016/S1474-4422(24)00328-4. Epub 2024 Sep 19. 94(1):1-9. doi: 10.1136/jnnp-2022-328799. Epub 2022 Nov 23.
3: Arnold DL, Elliott C, Martin EC, Hyvert Y, Tomic D, Montalban X. Effect of Evobrutinib on Slowly Expanding Lesion Volume in Relapsing Multiple Sclerosis: A Post Hoc Analysis of a Phase 2 Trial. Neurology. 2024 Mar 12;102(5):e208058. doi: 10.1212/WNL.0000000000208058. Epub 2024 Feb 9.
4: Scheible H, Schieferstein H, Schmidt R, Pusecker K, Gradhand U, Gopalakrishnan S, Iqbal K, Dong J, Jones R, Meli C, Bolleddula J, Dyroff M, Georgi K. Evobrutinib pathway to its major metabolite M463-2 and insights from a biotransformation and DDI perspective. Xenobiotica. 2023 Dec;53(8-9):547-558. doi: 10.1080/00498254.2023.2272180. Epub 2023 Nov 26. 23(11):1068-1070. doi: 10.1016/S1474-4422(24)00391-0. Epub 2024 Sep 19. 15(12):2899-2908. doi: 10.1111/cts.13417. Epub 2022 Oct 17.
合成参考文献
参考文献:10.1007/978-981-16-7200-2_6
摘要:Mok CC. Biologics in Systemic Lupus Erythematosus (SLE). 2022. In: Handbook of Biologics for Rheumatological Disorders.
参考文献:10.1007/s15202-023-5671-z
参考文献:10.1007/s11055-023-01430-8
摘要:Boyko AN. Tyrosine Kinases: Targets for Epigenetic Influences and a New Direction in the Treatment of Multiple Sclerosis. Neurosci Behav Physi. 2023 Mar;53(3):333–6. doi: 10.1007/s11055-023-01430-8.
参考文献:10.1007/s15005-023-3290-z
参考文献:10.1007/164_2021_545
摘要:Thompson KK, Tsirka SE. Immunosuppression in Multiple Sclerosis and Other Neurologic Disorders. Handb Exp Pharmacol. 2022;272():245–65. doi: 10.1007/164_2021_545.
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