CAS: 1655504-04-3; 6-(1-Acryloylpiperidin-4-yl)-2-(4-Phenoxyphenyl)Nicotinamide
物理性质
- 沸点646.3±55.0 °C(预测)
- 密度1.213±0.06 g/cm3(预测)
- pKa:14.80±0.50(预测)
- LogP:3.6
- 外观形态白色至类白色固体
- 储存条件Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
- 产品应用该化合物是一个高度选择性的,不可逆转的布鲁顿的暴风杆菌(BTK)抑制剂,它具有亚纳米化生化能(IC50~1-3 NM)和广红动脉板中最小离目标活动. 在B细胞类的实验中,它抑制BT-K自发性呼吸系统(TYR2223)和下游PLC2,NF-B和MAPK信号,抑制恶性B细胞在低纳米分子浓度下的扩散和生存. 在体内,口服管理使周边血液单核细胞和淋巴组织持续使用BT K(>90%) . 在淋巴细胞模型中,它可以减少肿瘤负担并延长存活时间. 临床药理学研究证实耐久性BTK抑制剂具有有利的选择性和有限的非目标类酶效应.
上下游产品
2-(4-Phenoxyphenyl)-6-(Piperidin-4-yl)Nicotinamide合成工艺路线路线简述
📜2,6-二氯烟酰胺置于盐酸,Bis-Triphenylphosphine-Palladium(II) Chloride,Tris-(Dibenzylideneacetone)Dipalladium(0),Pd(Oh)2/c,20%,氢气,碳酸氢钠,Sodium Carbonate体系中,用 四氢呋喃,甲醇,乙醇,水,乙酸乙酯 用作溶剂,-2.0~85.0 °C,200.0 Kpa 条件下,反应 25.5H,反应生成奥布替尼
参考文献: Process For Preparing 6-(1-Acryloylpiperidin-4-yl)-2-(4-Phenoxyphenyl) Nicotinamide[fr] Procédé De Préparation De 6-(1-Acryloylpipéridin-4-yl)-2-(4-Phénoxyphényl) Nicotinamide
标题: Process For Preparing 6-(1-Acryloylpiperidin-4-yl)-2-(4-Phenoxyphenyl) Nicotinamide[fr] Procédé De Préparation De 6-(1-Acryloylpipéridin-4-yl)-2-(4-Phénoxyphényl) Nicotinamide
摘要:公开了制备6-(1-丙烯酰基哌啶-4-基)-2-(4-苯氧基苯基)烟酰胺(化合物i)的过程,可在1千克以上的大规模下进行.该过程提供了非常好的收率和至少95%的终产品纯度,并提供可控和安全的反应.
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2912110000-甲醛
2912120000-乙醛 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Dhillon S. Orelabrutinib: First Approval. Drugs. 2021 Mar;81(4):503-507. doi: 10.1007/s40265-021-01482-5. Epub 2021 Mar 11. 23(18):1979-1986. doi: 10.1080/14656566.2022.2144218. Epub 2022 Nov 11. 98(4):571-579. doi: 10.1002/ajh.26826. Epub 2023 Jan 22. 7(16):4349-4357. doi: 10.1182/bloodadvances.2022009168.
5: Deng L, Li Z, Zhang H, Huang H, Hu J, Liu L, Liu T, Jin J, Zhu Z, Li W, Huang Z, Huang W, Zhou K, Yang H, Zhang M, Ding K, Zhou H, Hu Y, Shuang Y, Cao J, Gao S, Li D, Sun Z, Zhang Q, Yi S, Ji C, Zhang L, Hou C, Du Y, Wang W, Zhao R, Song Y, Zhu J. Orelabrutinib for the treatment of relapsed or refractory marginal zone lymphoma: A phase 2, multicenter, open-label study. Am J Hematol. 2023 Nov;98(11):1742-1750. doi: 10.1002/ajh.27064. Epub 2023 Aug 30. 206(4):1186-1199. doi: 10.1111/bjh.20045. Epub 2025 Mar 11. 18(10):1065-1076. doi: 10.1080/17460441.2023.2236547. Epub 2023 Jul 13. 45(5):599-605. doi: 10.1097/FTD.0000000000001106. Epub 2023 May 5. 40(3):650-659. doi: 10.1007/s10637-022-01219-5. Epub 2022 Feb 9. 102(27):e33880. doi: 10.1097/MD.0000000000033880.
12: Yang C, Cui Y, Ren X, Li M, Yu K, Shen S, Jiang H, Li M, Zhang X, Zhao X, Zhu Q, Lin S. Orelabrutinib Combined With Lenalidomide and Immunochemotherapy for Relapsed/Refractory Primary Central Nervous System Lymphoma: A Retrospective Analysis of Case Series. Front Oncol. 2022 Jun 16;12:901797. doi: 10.3389/fonc.2022.901797.
合成参考文献
参考文献:10.1021/acs.jmedchem.2c01938
摘要:Guo Y, Hu N, Liu Y, Zhang W, Yu D, Shi G, Zhang B, Yin L, Wei M, Yuan X, Luo L, Wang F, Song X, Xin L, Wei Q, Li Y, Guo Y, Chen S, Zhang T, Zhang S, Zhou X, Zhang C, Su D, Liu J, Cheng Z, Zhang J, Xing H, Sun H, Li X, Zhao Y, He M, Wu Y, Guo Y, Sun X, Tian A, Zhou C, Young S, Liu X, Wang L, Wang Z. Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases. J Med Chem. 2023 Mar 23;66(6):4025–44. doi: 10.1021/acs.jmedchem.2c01938.
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