CAS: 1217486-61-7; (S)-N1-(4-Methyl-5-(2-(1,1,1-Trifluoro-2-Methylpropan-2-yl)Pyridin-4-yl)Thiazol-2-yl)Pyrrolidine-1,2-Dicarboxamide

该化合物是磷酸丁酯3-kinase(PI3K)路径的选择性抑制物,具体针对PI3K的α异形.它主要用于治疗某些类型的乳腺癌,特别是荷尔蒙受体阳性并具有PIK3CA基因突变的乳腺癌.Alpelisib功能通过干扰促进癌症细胞生长和生存的信号路径,从而抑制肿瘤的生长.该化合物是口服的,并经常与内分泌疗法等其他疗法结合使用,以提高其功效.其药用植物活性半衰期表明中度的半衰期,允许一次性服用.常见副作用可能包括高血糖,皮疹和胃肠紊乱,需要在治疗期间进行监测.Alpolisib的发育代表了定向癌症疗法的重大进步,提供了基于肿瘤基因特征分析的更个性化治疗方法.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

2,4-lutidine 2-acetyl-4-methylpyridine L-prolinamide

合成工艺路线路线简述

    2,4-二甲基吡啶置于吡啶,N-溴代丁二酰亚胺(Nbs),正丁基锂,Sulfur Tetrafluoride,氢氟酸,Sodium Hydroxide,Lithium Diisopropyl Amide体系中,用 四氢呋喃,2-甲基四氢呋喃,乙醇,水,甲苯 用作溶剂,化学反应 29.59H,反应生成阿培利司
    参考文献: Synthesis Of 2-Carboxamide Cycloamino Urea Derivatives[fr] Synthèse De Dérivés De 2-Carboxamidocycloaminourée
    标题: Synthesis Of 2-Carboxamide Cycloamino Urea Derivatives[fr] Synthèse De Dérivés De 2-Carboxamidocycloaminourée
    摘要:本文提供了用于制备公式(x)的2-羧酰胺环氨基脲衍生物的过程和中间化合物,以及其有用的中间体.

    海关参考信息

    专利信息


    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-9776966-B2
    优先权日:2011-03-03
    标 题:Synthesis of 2-carboxamide cycloamino urea derivatives
    发明人:ERB BERNHARD; GALLOU ISABELLE SYLVIE; KLEINBECK FLORIAN KARL
    权利人:NOVARTIS AG
    摘要:Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.

    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:WO-2025019775-A1
    优先权日:2023-07-19
    标题 :Endoxifen compositions and methods of use thereof and synthesis thereof
    发明人:QUAY STEVEN
    权利人:ATOSSA THERAPEUTICS INC
    摘要:Described herein are endoxifen compositions comprising novel compounds and methods of use thereof. Methods of synthesis for the compositions are described herein. The endoxifen compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The endoxifen compositions described herein may be useful in the treatment of a condition in a subject, such as cancer.

    专利号:US-2023391824-A1
    优先权日:2021-02-08
    标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
    发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
    权利人:NARENDRAN ARUMUGAVADIVEL
    摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
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    主要参考文献


    1: Holzhauser S, Lukoseviciute M, Papachristofi C, Vasilopoulou C, Herold N, Wickström M, Kostopoulou ON, Dalianis T. Effects of PI3K and FGFR inhibitors alone and in combination, and with/without cytostatics in childhood neuroblastoma cell lines. Int J Oncol. 2021 Jan 5. doi: 10.3892/ijo.2021.5167. Epub ahead of print.
    3: Zhao M, Scott S, Evans KW, Yuca E, Saridogan T, Zheng X, Wang H, Korkut A, Cruz Pico CX, Demirhan ME, Kirby B, Kopetz S, Diala I, Lalani AS, Piha-Paul S, Meric-Bernstam F. Combining neratinib with CDK4/6, mTOR and MEK inhibitors in models of HER2-positive cancer. Clin Cancer Res. 2021 Jan
    7:clincanres.3017.2020. doi: 10.1158/1078-0432.CCR-20-3017. Epub ahead of print.

    合成参考文献


    参考文献:10.1007/s40265-019-01155-4
    摘要:McCann KE, Hurvitz SA, McAndrew N. Advances in Targeted Therapies for Triple-Negative Breast Cancer. Drugs. 2019 Jul;79(11):1217–30. doi: 10.1007/s40265-019-01155-4.
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