CAS: 209783-80-2; Pyridin-3-Ylmethyl 4-((2-Aminophenyl)Carbamoyl)Benzylcarbamate

该化合物是一个小分子,主要作为直肠脱乙酰酶抑制剂,其特点是能够改变直ones的胃状态,从而调节基因表达,这可能导致静默基因的恢复,特别是肿瘤抑制中的静脉瘤;Entinostat经常在癌症治疗方面进行研究,因为它表明它有可能提高其他抗癌剂的功效和治疗各种恶性病,包括乳腺癌和乳腺瘤;该化合物一般是口服的,具有相对有利的药用皮质特征,允许系统分布;其行动机制不仅涉及HDACs的抑制,而且还涉及各种信号路径的调节,从而导致其抗肿瘤效应;此外,对entinostat进行了免疫性特性的调查,使它成为肿瘤综合疗法的候选对象;与许多治疗剂一样,其使用可能伴随着副作用,在治疗期间需要仔细监测.

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CAS号95-54-5 邻苯二胺(OPD) | CAS号241809-79-0 4-(((吡啶-3-基甲氧基)... | CAS号80-73-9 1,3-二甲基-2-咪唑啉酮 | CAS号100-55-0 3-吡啶甲醇 | CAS号212632-27-4 pyrid-3-ylmethy... | CAS号255894-58-7 1-{4-[N-(pyridi... | CAS号1353003-29-8

合成工艺路线路线简述

    Pyridin-3-Ylmethyl N-[[4-[[2-[(2-Methylpropan-2-yl)Oxycarbonylamino]Phenyl]Carbamoyl]Phenyl]Methyl]Carbamate置于盐酸体系中,用 甲醇 用作溶剂,化学反应 3.0H,反应生成恩替诺特
    参考文献: Crystalline Forms Of Entinostat[fr] Formes Cristallines D'Entinostat
    标题: Crystalline Forms Of Entinostat[fr] Formes Cristallines D'Entinostat
    摘要:Entinostat是一种正在临床调查中的组蛋白去乙酰化酶抑制剂,用于多种固体肿瘤,如乳腺癌和血液肿瘤.提供了entinostat的结晶形态d和e以及高结晶纯度的结晶形态a.结晶形态d可以在高化学纯度下获得,具有改善的水溶性,并允许高效地纯化entinostat并去除有色杂质.还提供了制备这些结晶形态和具有改善化学和结晶纯度的a形态的工艺.

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    专利信息


    专利号:US-2025235415-A1
    优先权日:2022-02-23
    标 题:Modulation of human breast milk composition
    发明人:ROSS MICHAEL G; DESAI MINA
    权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER
    摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.

    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:WO-2009076206-A1
    优先权日:2007-12-07
    标题 :Synthesis methods of histone deacetylase inhibitors (hdacis)
    发明人:NJAR VINCENT C O; GEDIYA LALJI K
    权利人:UNIV MARYLAND; NJAR VINCENT C O; GEDIYA LALJI K
    摘要:Simple and efficient procedures for the synthesis of histone deacetylase inhibitors. The procedure may provide MS-275 in 72% overall yields.

    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-2023202980-A1
    优先权日:2019-08-30
    标题:N-(2-Aminophenyl)-Prop-2-Enamide Derivatives, and Uses Thereof in the Treatment of Cancer
    发明人:RADHAKRISHNAN SRIDHAR; TENEN DANIEL G; LIU BEE HUI; VU LE KIM ANH; GO MEI LIN; CHAI LI; GAO CHONG; KAMAL AHMED; SUNKARI SATISH; AYINAMPUDI VENKATA SUBBARAO; SYED RIYAZ; LIU MIAO
    权利人:NAT UNIV SINGAPORE; THE BRIGHAM AND WOMEN’S HOSPITAL INC; INDIAN INSTITUTE OF CHEMICAL TECH
    摘要:Provided herein are N-(2-aminophenyl)-prop-2-enamide derivatives, such as those of Formula (I), methods for the synthesis thereof, and uses thereof in the treatment of cancer, such as SALL4-expressing cancer, in a cell or subject in need thereof.

    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.
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    主要参考文献


    1: Trapani D, Esposito A, Criscitiello C, Mazzarella L, Locatelli M, Minchella I, Minucci S, Curigliano G. Entinostat for the treatment of breast cancer. Expert Opin Investig Drugs. 2017 Aug;26(8):965-971. doi: 10.1080/13543784.2017.1353077. Epub 2017 Jul 24. 10(5):656-669. doi: 10.1158/2326-6066.CIR-21-0170.
    3: Gupta VG, Hirst J, Petersen S, Roby KF, Kusch M, Zhou H, Clive ML, Jewell A, Pathak HB, Godwin AK, Wilson AJ, Crispens MA, Cybulla E, Vindigni A, Fuh KC, Khabele D. Entinostat, a selective HDAC1/2 inhibitor, potentiates the effects of olaparib in homologous recombination proficient ovarian cancer. Gynecol Oncol. 2021 Jul;162(1):163-172. doi: 10.1016/j.ygyno.2021.04.015. Epub 2021 Apr 16.
    4: Kiany S, Harrison D, Gordon N. The Histone Deacetylase Inhibitor Entinostat/Syndax 275 in Osteosarcoma. Adv Exp Med Biol. 2020;1257:75-83. doi: 10.1007/978-3-030-43032-0_7. 24(8):1101-9. doi: 10.1517/13543784.2015.1056779. Epub 2015 Jun 22. 20(10):1455-67. doi: 10.1517/13543784.2011.613822. Epub 2011 Sep 2. 28(3):1456. doi: 10.3390/molecules28031456.

    合成参考文献


    参考文献:10.1111/j.1600-0765.2011.01392.x
    摘要:Cantley MD, Bartold PM, Marino V, Fairlie DP, Le GT, Lucke AJ, Haynes DR. Histone deacetylase inhibitors and periodontal bone loss. J Periodontal Res. 2011 Dec;46(6):697–703. doi: 10.1111/j.1600-0765.2011.01392.x.
    参考文献:10.1155/2011/514261
    摘要:Miller CP, Singh MM, Rivera-Del Valle N, Manton CA, Chandra J. Therapeutic strategies to enhance the anticancer efficacy of histone deacetylase inhibitors. J Biomed Biotechnol. 2011;2011():514261.
    参考文献:10.1016/j.exphem.2011.07.002
    摘要:Jóna Á, Khaskhely N, Buglio D, Shafer JA, Derenzini E, Bollard C, Medeiros LJ, Illés Á, Ji Y, Younes A. The histone deacetylase inhibitor entinostat (SNDX-275) induces apoptosis in Hodgkin lymphoma cells and synergizes with Bcl-2 family inhibitors. Experimental Hematology. 2011 Oct;39(10):1007–1017.e1. doi: 10.1016/j.exphem.2011.07.002.
    参考文献:10.1093/brain/awr155
    摘要:Engmann O, Hortobágyi T, Pidsley R, Troakes C, Bernstein HG, Kreutz MR, Mill J, Nikolic M, Giese KP. Schizophrenia is associated with dysregulation of a Cdk5 activator that regulates synaptic protein expression and cognition. Brain. 2011 Aug;134(Pt 8):2408–21.
    参考文献:10.1007/s10637-011-9718-1
    摘要:Hwang JJ, Kim YS, Kim T, Kim MJ, Jeong IG, Lee JH, Choi J, Jang S, Ro S, Kim CS. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL. Invest New Drugs. 2012 Aug;30(4):1434–42. doi: 10.1007/s10637-011-9718-1.
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