CAS: 783355-60-2; 3-((Dimethylamino)Methyl)-N-(2-(4-(Hydroxycarbamoyl)Phenoxy)Ethyl)Benzofuran-2-Carboxamide

该化合物是脑膜脱氧核糖核酸(HDACs)的强大,小分子抑制剂, 具体针对HDAC第一,二和四级. 它在基因表达中表现出通过诱导直肠高血压增生性激素来调节基因表达的广谱性活动,导致细胞循环停止,恶性细胞的吸附性. Abexinostat在肝脏恶性肿瘤和固态肿瘤的临床和临床前期研究中表现出效力, 特别是在复发或复发环境中. 它的口服生物利用率和有利的药用动能特征增强了它的治疗潜力. 复合体与其他抗癌剂(如DNA成形药物和免疫疗法)的合成能力进一步凸显了它在生殖系统上的效用. 持续的研究继续探索其机械深度和临床应用.

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上下游产品

abexinostat methyl 4-hydroxylbenzoate 4-(2-tert-butoxycarbonylaminoethoxy)benzoic acid methyl ester o-hydroxyacetophenone

合成工艺路线路线简述

    📜Methyl 4-(2-((Tert-Butoxycarbonyl)Amino)Ethoxy)Benzoate置于盐酸,Hatu,羟胺,溶剂黄146,三乙胺体系中,用 四氢呋喃,甲醇,乙酸乙酯 作为反应溶剂,化学反应 6.0H,反应生成 3-[(二甲基氨基)甲基]-N-[2-[4-[(羟基氨基)羰基]苯氧基]乙基]-2-苯并呋喃羧酰胺
    参考文献:一种制备艾贝司他的方法,中间体及中间体的制备方法
    标题:一种制备艾贝司他的方法,中间体及中间体的制备方法
    摘要:本发明提供一种艾贝司他的制备方法,包括如下步骤:(1)将第一中间体3‑((二甲氨基)甲基)苯并呋喃‑2‑羧酸和第二中间体4‑(2‑氨基乙氧基)苯甲酸甲酯经酰胺缩合后制得第三中间体4‑[2‑(3‑二甲基氨基苯并呋喃‑2‑基‑羰基氨基)乙氧基]苯甲酸甲酯;(2)将第三中间体脱酯后再经酸调制备得到艾贝司他.该方法原料易得,工艺简洁,反应条件温和,操作方便,收率高,成本低,易于工业化生产.本发明还提供制备艾贝司他的第一中间体和第二中间体及其制备方法.

    海关参考信息

    专利信息


    专利号:US-11286271-B2
    优先权日:2018-07-31
    标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
    发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
    权利人:UNIV HONG KONG
    摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    专利号:US-10370455-B2
    优先权日:2014-12-05
    标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists
    发明人:MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL
    权利人:IMMUNEXT INC
    摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    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.

    专利号:US-2018371021-A1
    优先权日:2017-05-11
    标 题 :Peptidomimetic macrocycles and uses thereof
    发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
    权利人:AILERON THERAPEUTICS INC
    摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

    专利号:US-2025064840-A1
    优先权日:2021-12-16
    标 题 :Drug delivery systems based on endoperoxides useful in diagnosis and therapy, and methods thereof
    发明人:SILVA MAGALHAES DIOGO; MOREIRA RUI; LOPES FRANCISCA; RODRIGUES CECILIA; MARQUES VANDA
    权利人:FACULDADE DE FARMACIA DA UNIV DE LISBOA
    摘要:The present invention relates to novel drug delivery systems based on endoperoxide moieties such as 1,2,4,5-tetraoxanes, namely compounds of formula I, appropriately modified to release active pharmaceutical ingredients (API) in the presence of higher levels of Fe (II), in a subject, whereinIron metabolism dysregulation occurs in diseases such as malaria and cancer. Therefore, the present invention also relates to biomarkers comprising said compounds of formula I.Another aspect, the present invention relates to a process of synthesis of compounds of formula I and respective intermediaries.Further, the present invention also relates to a process for labelling, detection, and identification of tumours in a tissue sample.The present invention is thus applicable to the medical and pharmacological areas, in related to particular the ones cancer detection and treatment, and malaria treatment.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: De Souza C, Chatterji BP. HDAC Inhibitors as Novel Anti-Cancer Therapeutics. Recent Pat Anticancer Drug Discov. 2015;10(2):145-62. doi: 10.2174/1574892810666150317144511. 8(34):56210-56227. doi: 10.18632/oncotarget.14813.
    3: Ali D, Hamam R, Alfayez M, Kassem M, Aldahmash A, Alajez NM. Epigenetic Library Screen Identifies Abexinostat as Novel Regulator of Adipocytic and Osteoblastic Differentiation of Human Skeletal (Mesenchymal) Stem Cells. Stem Cells Transl Med. 2016 Aug;5(8):1036-47. doi: 10.5966/sctm.2015-0331. Epub 2016 May 18.
    4: Choy E, Flamand Y, Balasubramanian S, Butrynski JE, Harmon DC, George S, Cote GM, Wagner AJ, Morgan JA, Sirisawad M, Mani C, Hornicek FJ, Duan Z, Demetri GD. Phase 1 study of oral abexinostat, a histone deacetylase inhibitor, in combination with doxorubicin in patients with metastatic sarcoma. Cancer. 2015 Apr 15;121(8):1223-30. doi: 10.1002/cncr.29175. Epub 2014 Dec 23.

    合成参考文献


    参考文献:10.1007/s12253-012-9592-y
    摘要:Du X, Zhao H, Zang L, Song N, Yang T, Dong R, Yin J, Wang C, Lu J. Overexpression of Histone Deacetylase 2 Predicts Unfavorable Prognosis in Human Gallbladder Carcinoma. Pathology & Oncology Research. 2012 Dec 16;19(3):397–403. doi: 10.1007/s12253-012-9592-y.
    参考文献:10.1007/s10637-014-0118-1
    摘要:Chalret du Rieu Q, Fouliard S, White-Koning M, Kloos I, Chatelut E, Chenel M. Pharmacokinetic/Pharmacodynamic modeling of abexinostat-induced thrombocytopenia across different patient populations: application for the determination of the maximum tolerated doses in both lymphoma and solid tumour patients. Invest New Drugs. 2014 Oct;32(5):985–94. doi: 10.1007/s10637-014-0118-1.
    参考文献:10.1007/s11914-020-00616-0
    摘要:Cakouros D, Gronthos S. Epigenetic Regulators of Mesenchymal Stem/Stromal Cell Lineage Determination. Current Osteoporosis Reports. 2020 Aug 13;18(5):597–605. doi: 10.1007/s11914-020-00616-0.
    参考文献:10.1186/1756-8722-3-5
    摘要:Tan J, Cang S, Ma Y, Petrillo RL, Liu D. Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents. Journal of Hematology & Oncology. 2010 Feb 04;3(1):5. doi: 10.1186/1756-8722-3-5.
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