CAS: 1650550-25-6; 2-Methyl-1-((4-(6-(Trifluoromethyl)Pyridin-2-yl)-6-((2-(Trifluoromethyl)Pyridin-4-yl)Amino)-1,3,5-Triazin-2-yl)Amino)Propan-2-Ol Methanesulfonate

该化合物是一种小分子抑制剂,主要用于治疗具有特定基因突变的急性流状白血病(AML),它有选择性地抑制二类氢气酶(IDH2)酶,在细胞代谢和分化中起着关键作用;通过抑制二类细胞内的新陈代谢途径,抑制二类细胞内的新陈代谢途径,导致白化素的累积,促进对白化细胞的区分; 环状盐形式增加其溶解性和稳定性,便利其管理; 环状盐通常通过口服方式施用,并具有有利的药性植物基因特征,允许一次性施用; 常见的副作用可能包括恶心,疲劳和潜在的分化综合症,这需要监测; 它的发展代表了定向癌症疗法的重大进步,特别是染有二类白化细胞的病人,提供了更个性化的治疗方法. 与任何药物一样,其使用应该以保健专业为导向,考虑到具体的临床和病人特点.

结构式图片

合成工艺路线路线简述

    6-(三氟甲基)吡啶-2-甲酸置于氯化亚砜,乙醇,五氯化磷,Sodium,碳酸氢钠体系中,用 四氢呋喃,丙酮,三氯氧磷 用作溶剂,化学反应 25.17H,反应生成Ag221甲磺酸盐
    参考文献: Crystalline Forms Of Therapeutically Active Compounds And Use Thereof[fr] Formes Cristallines De Composés Thérapeutiquement Actifs Et Utilisation Associée
    标题: Crystalline Forms Of Therapeutically Active Compounds And Use Thereof[fr] Formes Cristallines De Composés Thérapeutiquement Actifs Et Utilisation Associée
    摘要:提供了2-甲基-1-[(4-[6-(三氟甲基)吡啶-2-基]-6-{[2-(三氟甲基)吡啶-4-基]氨基}-1,3,5-三嗪-2-基)氨基]丙醇(Compound 3),2-甲基-1-[(4-[6-(三氟甲基)吡啶-2-基]-6-{[2-(三氟甲基)吡啶-4-基]氨基}-1,3,5-三嗪-2-基)氨基]丙醇甲磺酸盐(Compound 1)的结晶形式及其用途.

    海关参考信息

    专利信息


    专利号:US-2022118094-A1
    优先权日:2019-02-21
    标题:Synthesis of biomimetic cell wall structure
    发明人:WANG YONG; SHI PENG
    权利人:PENN STATE RES FOUND
    摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

    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.

    专利号:WO-2025137620-A1
    优先权日:2023-12-21
    标题:Methods for high quality and high accuracy methylation sequencing
    发明人:KENNEDY ANDREW
    权利人:GUARDANT HEALTH INC
    摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.

    专利号:EP-4288444-A1
    优先权日:2021-02-08
    标题:Rationale, design, synthesis and validation of a small molecule anticancer agent

    专利号:WO-2022165606-A1
    优先权日:2021-02-08
    标 题:Rationale, design, synthesis and validation of a small molecule anticancer agent

    专利号:CA-3207354-A1
    优先权日:2021-02-08
    标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
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    主要参考文献


    1: Dittakavi S, Hallur G, Purra BR, Kiran V, Zakkula A, Mullangi R. Validated LC-MS/MS Method for Simultaneous Quantitation of Enasidenib and its Active Metabolite, AGI-16903 in Small Volume Mice Plasma: Application to a Pharmacokinetic Study. Drug Res (Stuttg). 2019 Oct 25. doi: 10.1055/a-1024-3623. [Epub ahead of print] Available from http://www.ncbi.nlm.nih.gov/books/NBK548492/ doi: 10.2147/CMAR.S162784. eCollection 2019.
    4: Del Principe MI, Paterno G, Palmieri R, Maurillo L, Buccisano F, Venditti A. An evaluation of enasidenib for the treatment of acute myeloid leukemia. Expert Opin Pharmacother. 2019 Nov;20(16):1935-1942. doi: 10.1080/14656566.2019.1654456. Epub 2019 Aug 27. doi: 10.1002/bmc.4658. Epub 2019 Sep 2. doi: 10.2147/CE.S172912. eCollection 2019.
    7: Pollyea DA, Tallman MS, de Botton S, Kantarjian HM, Collins R, Stein AS, Frattini MG, Xu Q, Tosolini A, See WL, MacBeth KJ, Agresta SV, Attar EC, DiNardo CD, Stein EM. Enasidenib, an inhibitor of mutant IDH2 proteins, induces durable remissions in older patients with newly diagnosed acute myeloid leukemia. Leukemia. 2019 Nov;33(11):2575-2584. doi: 10.1038/s41375-019-0472-2. Epub 2019 Apr 9. doi: 10.2147/CPAA.S192687. eCollection 2019.

    合成参考文献


    参考文献:10.1007/978-981-99-9183-9_11
    摘要:Sengupta T, Khan A, Nambiar M, Nishana M. Targeting the Epigenetic Landscape for Cancer Therapy. 2024. In: Drugs from Nature: Targets, Assay Systems and Leads.
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