CAS: 1254036-71-9; 2-(6-(1H-Indol-4-yl)-1H-Indazol-4-yl)-5-((4-Isopropylpiperazin-1-yl)Methyl)Oxazole

该化合物是用于治疗呼吸道疾病(包括慢性阻塞性肺病(COPD)和哮喘)的一种强效和选择性的磷酸盐3-K-肝炎酯(PI3K)抑制剂,对PI3K的高度选择性将治疗性效果降低到非目标效果,提高了治疗性精确度. Nemiralisib通过调节免疫细胞活化和减少空气炎,表现出很强的抗炎特性. 临床和临床研究表明,可以使用有利的药理活性,包括良好的口服生物利用率和持续的目标接触. 它的行动机制针对中微营养素炎的关键路径,为管理严重呼吸道疾病提供了潜在好处. 化合物的精密安全特征支持了其在长期呼吸道疗法中的调查用途.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

6-(1H-Indol-4-yl)-4-(5-{[4-(1-Methylethyl)-1-Piperazinyl]Methyl}-1,3-Oxazol-2-yl)-1-(Phenylsulfonyl)-1H-Indazole 1364802-72-1
6-Chloro-4-(5-{[4-(1-Methylethyl)-1-Piperazinyl]Methyl}-1,3-Oxazol-2-yl)-1-(Phenylsulfonyl)-1H-Indazole 1254036-86-6
{2-[6-Chloro-1-(Phenylsulfonyl)-1H-Indazol-4-Yl]-1,3-Oxazol-5-Yl}Methanol 1254036-83-3
(5-Bromomethyl)-2-(6-Chloro-1-(Phenylsulfonyl)-1H-Indazol-4-yl)Oxazole 1254036-84-4
Methyl 2-[6-Chloro-1-(Phenylsulfonyl)-1H-Indazol-4-Yl]-1,3-Oxazole-5-Carboxylate 1254036-82-2
Ethyl 2-[6-Chloro-1-(Phenylsulfonyl)-1H-Indazol-4-Yl]-1,3-Oxazole-5-Carboxylate 1254036-81-1

合成工艺路线路线简述

    📜(2-(6-(1H-Indol-4-yl)-1-(Tetrahydro-2H-Pyran-2-yl)-1H-Indazol-4-yl)Oxazol-5-yl)(4-Isopropylpiperazin-1-yl)Methanone置于aluminum (III) Chloride,Lithium Aluminium Tetrahydride,甲醇,三甲基氯硅烷,三乙胺体系中,用 四氢呋喃,乙酸乙酯 用作溶剂,化学反应 3.5H,以81%的收率获得奈米利塞
    参考文献: Processes To Make Indazole Derivatives[fr] Procédés Pour Fabriquer Des Dérivés D'Indazole
    标题: Processes To Make Indazole Derivatives[fr] Procédés Pour Fabriquer Des Dérivés D'Indazole
    摘要:本发明提供了制备化合物(iv)及其盐的新工艺,新中间体,以及新的盐和其多晶形式.

    海关参考信息

    专利信息


    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    专利号:US-2022411407-A1
    优先权日:2019-11-15
    标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
    发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
    权利人:UNIV NORTH CAROLINA CHAPEL HILL
    摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Begg M, Edwards CD, Hamblin JN, Pifani E, Wilson R, Gilbert J, Vitulli G, Mallett D, Morrell J, Hingle MI, Uddin S, Ehtesham F, Marotti M, Harell A, Newman C, Fernando D, Clark J, Cahn A, Hessel EM. Translation of inhaled drug optimization strategies into clinical pharmacokinetics and pharmacodynamics using GSK2292767A, a novel inhaled PI3Kδ inhibitor. J Pharmacol Exp Ther. 2019 Apr 2. pii: jpet.119.257311. doi: 10.1124/jpet.119.257311. [Epub ahead of print] doi: 10.1002/cpdd.614. Epub 2018 Oct 10. doi: 10.1124/jpet.118.249516. Epub 2018 Sep 14. doi: 10.1016/j.clinthera.2018.06.011. Epub 2018 Jul 25.

    合成参考文献


    参考文献:10.1007/978-981-33-6827-9_5
    摘要:Bhatt S, Kanoujia J, Nagappa AN, Pai KSR. Targeting Molecular and Cellular Mechanisms in Chronic Obstructive Pulmonary Disease. 2021. In: Targeting Cellular Signalling Pathways in Lung Diseases.
    参考文献:10.1055/s-0040-1719732
    摘要:Synthesis of Nemiralisib. Synfacts. 2021 May 18;17(06):0609. doi: 10.1055/s-0040-1719732.
    参考文献:10.1186/s43094-025-00859-7
    摘要:Salva C, Galla R. A bioanalytical method development and validation of leniolisib by reverse phase high-performance liquid chromatography in rat plasma and its application in pharmacokinetic studies. Futur J Pharm Sci. 2025 Aug 01;11(1). doi: 10.1186/s43094-025-00859-7.
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