CAS: 957054-30-7; 4-(2-(1H-Indazol-4-yl)-6-((4-(Methylsulfonyl)Piperazin-1-yl)Methyl)Thieno[3,2-D]Pyrimidin-4-yl)Morpholine

该化合物是磷酸丁二醇3-皮肤(PI3K)的一种有选择性的小型分子抑制剂,专门针对p110α异形,对PI3Kα(PI3Kα)有高度的抑制性活动,PI3K/AKT/mtor信号路径是PI3K/AKT/mtor信号路径的一个关键组成部分,经常对癌症进行控制. Pictilisib展示了有利的药用植物基因特性,包括口服生物利用率和持续的目标接触,使其适合临床前科和临床研究.其特性和精细化的行动机制使它成为研究PI3K驱动的肿瘤发源和评估肿瘤治疗战略的宝贵工具.该化合物被广泛用于研究抗药机制和复方疗法,强调其在癌症研究中的实用性.

结构式图片

上下游产品

CAS号885618-33-7 1H-吲唑-4-硼酸频哪醇酯 | CAS号885675-66-1 2-氯-6-(4-甲烷磺酰基-... | CAS号16234-15-4 2-氯-4-(4-吗啉基)噻吩... | CAS号55289-36-6 2-甲基-3-溴苯胺 | CAS号73183-34-3 双戊酰二硼 | CAS号186407-74-9 4-溴吲唑 | CAS号16233-51-5 2,4-二羟基噻吩并[3,2-D]嘧啶 | CAS号22288-78-4 3-氨基-2-噻吩甲酸甲酯 | CAS号16234-14-3 2,4-二氯噻吩并[3,2-D]嘧啶 | CAS号885618-31-5 2-氯-4-吗啉代噻吩并[3,...

合成工艺路线路线简述

    📜2,4-二氯噻吩并[3,2-D]嘧啶置于titanium(Iv) Isopropylate,Bis-Triphenylphosphine-Palladium(II) Chloride,碳酸氢钠,三乙胺,Lithium Diisopropyl Amide体系中,用 四氢呋喃,甲醇,正己烷,氯仿,水,甲苯 作为反应溶剂,化学反应 26.0H,反应生成 4-羟基-2,6-二甲基苯甲腈
    参考文献:Treatment Of Cancers Having K-Ras Mutations
    标题:Treatment Of Cancers Having K-Ras Mutations
    摘要:本发明提供了一种治疗与k-Ras突变相关的癌症的方法,适用于需要该方法的受试者.该方法包括以下步骤:(1)识别患有与k-Ras突变相关的癌症的受试者;和(2)向受试者施用(i)pi3激酶抑制剂和(II)hdac抑制剂,其中pi3激酶抑制剂和hdac抑制剂以联合治疗有效的剂量进行施用.

    海关参考信息

    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-12441733-B2
    优先权日:2018-03-26
    标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
    发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
    权利人:NOVARTIS AG
    摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

    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-10772971-B2
    优先权日:2017-06-22
    标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
    发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
    权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
    摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

    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: De Wolf E, De Wolf C, Richardson A. ABT-737 and pictilisib synergistically enhance pitavastatin-induced apoptosis in ovarian cancer cells. Oncol Lett. 2018 Feb;15(2):1979-1984. doi: 10.3892/ol.2017.7516. Epub 2017 Dec 5.
    2: Keegan NM, Gleeson JP, Hennessy BT, Morris PG. PI3K inhibition to overcome endocrine resistance in breast cancer. Expert Opin Investig Drugs. 2018 Jan;27(1):1-15. doi: 10.1080/13543784.2018.1417384. Epub 2018 Jan 6. Review. doi: 10.1038/s41389-017-0004-8. doi: 10.1016/j.ejca.2017.08.027. Epub 2017 Oct 6. doi: 10.18632/oncotarget.19194. eCollection 2017 Sep 8.
    7: Chen J, Guo J, Cui X, Dai Y, Tang Z, Qu J, Raj JU, Hu Q, Gou D. The Long Noncoding RNA LnRPT Is Regulated by PDGF-BB and Modulates the Proliferation of Pulmonary Artery Smooth Muscle Cells. Am J Respir Cell Mol Biol. 2018 Feb;58(2):181-193. doi: 10.1165/rcmb.2017-0111OC. doi: 10.1158/1078-0432.CCR-17-0033. Epub 2017 Aug 14.

    合成参考文献


    参考文献:10.1007/s11912-011-0187-7
    摘要:Schatz JH. Targeting the PI3K/AKT/mTOR pathway in non-Hodgkin's lymphoma: results, biology, and development strategies. Curr Oncol Rep. 2011 Oct;13(5):398–406. doi: 10.1007/s11912-011-0187-7.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知