CAS: 497833-27-9; (6-((Diethylamino)Methyl)Naphthalen-2-yl)Methyl (4-(Hydroxycarbamoyl)Phenyl)Carbamate

该化合物是一个小分子抑制剂,主要因其作为直肠脱乙酰酶抑制剂的作用而得到承认,被归入了遗传变异器类别,这意味着通过改变染色体结构影响基因表达方式,Givinostat由于能够诱发细胞循环停止细胞循环和癌症细胞中流行性疾病等各种条件下的潜在治疗应用,因此已经研究过它可能用于治疗,包括癌症和炎症,该化合物在有机溶剂中表现出中等至高溶性,通常在药物配方中施用.其行动机制包括抑制HDAC酶,导致乙酰激素激素激素和随后基因表达方式的调节.Givinostat经过临床试验,表明它有可能治疗特定血清恶性肿瘤和固态肿瘤.然而,与许多调查药物一样,其安全和功效简介也在不断研究中评估.

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合成工艺路线路线简述

    📜[6-(Diethylaminomethyl)Naphthalen-2-Yl]Methyl N-(4-Carbonochloridoylphenyl)Carbamate置于羟胺体系中,用 四氢呋喃,水 作为反应溶剂,以107 G的收率获得产物[4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯
    参考文献: Process For Preparing {6-[(Diethylamino)Methyl]Naphthalen-2-Yl}Methyl [4-(Hydroxycarbamoyl)Phenyl]Carbamate Having High Purity[fr] Procédé De Préparation De {6-[(Diéthylamino)Méthyl]Naphthalen-2-Yl}Méthyl[4-(Hydroxycarbamoyl)Phényl]Carbamate De Haute Pureté
    标题: Process For Preparing {6-[(Diethylamino)Methyl]Naphthalen-2-Yl}Methyl [4-(Hydroxycarbamoyl)Phenyl]Carbamate Having High Purity[fr] Procédé De Préparation De {6-[(Diéthylamino)Méthyl]Naphthalen-2-Yl}Méthyl[4-(Hydroxycarbamoyl)Phényl]Carbamate De Haute Pureté

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    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-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.

    专利号:US-11885012-B2
    优先权日:2015-08-14
    标题 :Graphene synthesis
    发明人:SEO DONG HAN; PINEDA SHAFIQUE; HAN ZHAO JUN; OSTRIKOV KOSTYANTYN
    权利人:COMMW SCIENT IND RES ORG; COMMONWEALTH SCIENT AND INDUSTRIAL RESEARCH ORGANIZATION
    摘要:The invention relates to methods for the production of high quality graphene. In particular, the invention relates to single-step thermal methods which can be carried out in an ambient-air or vacuum environment using renewable biomass as a carbon source. Specifically, the invention comprises heating a metal substrate and carbon source in a sealed ambient environment to a temperature which produces carbon vapour from the carbon source such that the vapour comes into contact with the metal substrate, maintaining the temperature for a time sufficient to form a graphene lattice and then cooling the substrate at a controlled rate to form a deposited graphene.

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    主要参考文献


    1: Zappasodi R, Cavanè A, Iorio MV, Tortoreto M, Guarnotta C, Ruggiero G, Piovan C, Magni M, Zaffaroni N, Tagliabue E, Croce CM, Zunino F, Gianni AM, Di Nicola M. Pleiotropic antitumor effects of the pan-HDAC inhibitor ITF2357 against c-Myc-overexpressing human B-cell non-Hodgkin lymphomas. Int J Cancer. 2014 Nov 1;135(9):2034-45. doi: 10.1002/ijc.28852. Epub 2014 Mar 26. doi: 10.2119/molmed.2011.00058. Epub 2011 Feb 11.
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    4: Li S, Fossati G, Marchetti C, Modena D, Pozzi P, Reznikov LL, Moras ML, Azam T, Abbate A, Mascagni P, Dinarello CA. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. doi: 10.1074/jbc.M114.618454. Epub 2014 Dec 1.

    合成参考文献


    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.
    参考文献:10.1038/nchembio.313
    摘要:Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. Chemical phylogenetics of histone deacetylases. Nature Chemical Biology. 2010 Feb 07;6(3):238–43. doi: 10.1038/nchembio.313.
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