CAS: 1899921-05-1; N-(5-((4-(1-Cyclopropyl-1H-Indol-3-yl)Pyrimidin-2-yl)Amino)-2-((2-(Dimethylamino)Ethyl)(Methyl)Amino)-4-Methoxyphenyl)Acrylamide

📜3-(2-氯-嘧啶-4-基)-1H-吲哚置于n,N-二甲基乙酰胺,Palladium On Activated Charcoal,氢气,Sodium Hydride,对甲苯磺酸,N,N-二异丙基乙胺,苯胺体系中,用 四氢呋喃,甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 19.5H,反应生成阿美替尼
参考文献:Osimertinib 吲哚和嘧啶环的结构修饰导致对 L858R/t790M 双突变酶的高选择性和有效的抗肿瘤活性
标题:Osimertinib 吲哚和嘧啶环的结构修饰导致对 L858R/t790M 双突变酶的高选择性和有效的抗肿瘤活性
摘要:Egfr抑制剂是治疗非小细胞肺癌的一个重要里程碑,然而,它们存在获得性耐药性.利用奥希替尼作为先导化合物,这项工作探索了奥希替尼的吲哚和嘧啶环的结构修饰,以产生新的奥希替尼衍生物.在体外酶活性和细胞的研究表明,具有衍生物朝双突变的egfr和有效的抗肿瘤活性的高选择性.特别是,活性最强的化合物6B-1对双突变egfr(ic 50 = 0.18 Nm)和野生型egfr(ic 50 = 2.89 Nm)以及h1975细胞(ic 50 = 1.44 Nm).蛋白质印迹分析表明,6B-1完全抑制双突变 Egfr 和 Erk 磷酸化.使用异种移植模型的体内试验表明,化合物6B-1比奥希替尼具有更好的抗肿瘤功效.更重要的是,6B-1在药代动力学研究中显示出许多优势,包括更好的口服生物利用度和代谢特性.
Doi:10.1016/j.Bmc.2021.116094

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: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.