CAS: 1847461-43-1; Isopropyl 2-((5-Acrylamido-4-((2-(Dimethylamino)Ethyl)(Methyl)Amino)-2-Methoxyphenyl)Amino)-4-(1-Methyl-1H-Indol-3-yl)Pyrimidine-5-Carboxylate

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Isopropyl 2-Chloro-4-(1-Methyl-1H-Indol-3-yl)Pyrimidine-5-Carboxylate

📜2,4-二氯嘧啶-5-甲酸异丙酯置于aluminum (III) Chloride,Palladium 10% On Activated Carbon,氢气,N,N-二异丙基乙胺,三氟乙酸体系中,用 四氢呋喃,乙二醇二甲醚,异丙醇 用作溶剂,90.0 °C,101.33 Kpa 条件下,反应 7.0H,反应生成莫博替尼/tak-788
参考文献:用野生型保留抑制剂对表皮生长因子受体靶向外显子 20 插入突变的洞察
标题:用野生型保留抑制剂对表皮生长因子受体靶向外显子 20 插入突变的洞察
摘要:尽管表皮生长因子受体 (Egfr) 抑制剂具有临床疗效,但一部分非小细胞肺癌患者在 Egfr 和 Her2 的外显子 20 中显示插入突变,治疗选择有限.在这里,我们介绍了基于 1 H-Pyrrolo [2,3-B的新型共价抑制剂 Ldc8201 和 Ldc0496 的开发和表征.]吡啶支架.它们表现出对 Egfr 和 Her2 外显子 20 插入突变的强烈抑制效力,以及对野生型 Egfr 和激酶组内的选择性.具有抑制剂和生化和细胞靶向活性的复杂晶体结构证明了它们有利的结合特性.最终,我们在 Ldc8201 治疗期间观测到移植了患者来源的 Egfr-H773_v774Insnph 突变细胞的小鼠的肿瘤缩小.总之,这些结果突出了共价吡咯并吡啶作为靶向外显子20插入突变抑制剂的潜力.
Doi:10.1021/acs.Jmedchem.1C02080

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.

专利号:CN-116655599-A
优先权日:2023-05-17
标题:Synthesis and application of a class of EGFR allosteric inhibitors

专利号:CN-118652239-A
优先权日:2024-05-29
标题 :Synthesis and application of EGFR allosteric inhibitors