CAS: 1239908-20-3; (R)-2,2'-(2-(1-(2-(2,5-Dichlorobenzamido)Acetamido)-3-Methylbutyl)-5-Oxo-1,3,2-Dioxaborolane-4,4-Diyl)Diacetic Acid

该化合物是一种主要用于治疗多种骨髓瘤的小分子蛋白抑制剂,其特点是能够破坏蛋白质的功能,导致培养癌症细胞中的骨质疏松症的调控蛋白质的积累;该化合物通过口服施用,提供了与传统静脉注射疗法相比方便的行政管理途径;Ixazomob 柠檬酸盐经常与其他物剂,如Lenalomide和dexamethason,结合使用,以提高治疗效果;其行动机制包括抑制26S蛋白质,这是对有辱人格的活性蛋白质负责的复合物,从而影响到各种细胞过程,包括细胞循环调节和人口囊肿症;该物质经过广泛的临床试验,表明其对于复发或再生多子细胞瘤患者的有效性和安全性.此外,Ixazomomib 柠檬因其有利的药效特性而引人注目,包括可控副作用,有助于其在现代癌症治疗中发挥作用.

结构式图片

欧盟法规

C&L通报

上下游产品

艾沙佐米 Ixazomib 1072833-77-2
N,N',N''-[2,4,6-Boroxintriyltris[[(1R)-3-Methylbutylidene]Imino(2-Oxo-2,1-Ethanediyl)]]Tris(2,5-Dichlorobenzamide) 1201903-03-8

合成工艺路线路线简述

    2,5-二氯苯甲酸置于o-(Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Tetrafluoroborate,Lithium Hydroxide体系中,用 四氢呋喃,二氯甲烷,水,乙酸乙酯,丙酮 用作溶剂,化学反应 1.33H,反应生成枸橼酸艾沙佐米
    参考文献:一种含硼化合物的制备方法
    标题:一种含硼化合物的制备方法
    摘要:本发明公开了一种含硼化合物mln9708的制备方法.本发明公布的制备mln9708的方法包括采用方便易得的原料iv合成制备得到一种能够重结晶纯化的中间体ii,然后采用柠檬酸进行硼酸酯交换反应,得到含硼化合物mln9708.该合成工艺路线,对生产设备没有特殊的要求,反应条件温和,所有的原料均为市售产品,该工艺路线非常适合工业化生产.

    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-11542283-B2
    优先权日:2018-05-28
    标题 :Synthesis of peptide borate ester compound and use thereof
    发明人:QIN YANRU
    权利人:JIANGSU CHIA TAI FENGHAI PHARMACEUTICAL CO LTD
    摘要:Provided are a peptide borate ester compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, and pharmaceutical use thereof. The peptide borate ester compound or pharmaceutically acceptable salt thereof has a structure as shown in Formula (I), and is useful in the preparation of proteasome inhibitors to treat solid tumors and hematoma.

    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-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-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:CN-118922420-A
    优先权日:2022-03-25
    标题 :Synthesis of TYK2 inhibitors and their intermediates
    南通嘉星泰生物科技有限公司
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    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548002/ doi: 10.1136/esmoopen-2019-000570. eCollection 2019. Review.
    3: Armoiry X, Spath HM, Clarke A, Connock M, Sutcliffe P, Dussart C. Comparison of health technology assessment for new medicines in France and England: an example based on ixazomib for patients with relapsed or refractory multiple myeloma. J Mark Access Health Policy. 2019 Jul 30;7(1):1648971. doi: 10.1080/20016689.2019.1648971. eCollection 2019. Review.
    4: Smolewski P, Rydygier D. Ixazomib: an investigational drug for the treatment of lymphoproliferative disorders. Expert Opin Investig Drugs. 2019 May;28(5):421-433. doi: 10.1080/13543784.2019.1596258. Epub 2019 Apr 13. Review. doi: 10.1080/14656566.2018.1528229. Epub 2018 Nov 13. Review. doi: 10.1080/17474086.2018.1518129. Review. doi: 10.1007/s40262-018-0702-1. Review.

    合成参考文献


    参考文献:10.1186/1747-1028-7-26
    摘要:Rastogi N, Mishra DP. Therapeutic targeting of cancer cell cycle using proteasome inhibitors. Cell Div. 2012 Dec 26;7(1):26.
    参考文献:10.1007/s11899-017-0365-2
    摘要:Green DJ, Bensinger WI. A View from the Plateau: Is There a Role for Allogeneic Stem Cell Transplantation in the Era of Highly Effective Therapies for Multiple Myeloma Current Hematologic Malignancy Reports. 2017 Jan 31;12(1):61–7. doi: 10.1007/s11899-017-0365-2.
    参考文献:10.1038/s41375-018-0098-9
    摘要:Avet-Loiseau H, Facon T. Front-line therapies for elderly patients with transplant-ineligible multiple myeloma and high-risk cytogenetics in the era of novel agents. Leukemia. 2018 Mar 28;32(6):1267–76. doi: 10.1038/s41375-018-0098-9.
    参考文献:10.1038/s41375-018-0040-1
    摘要:Ludwig H, Delforge M, Facon T, Einsele H, Gay F, Moreau P, Avet-Loiseau H, Boccadoro M, Hajek R, Mohty M, Cavo M, Dimopoulos MA, San-Miguel JF, Terpos E, Zweegman S, Garderet L, Mateos MV, Cook G, Leleu X, Goldschmidt H, Jackson G, Kaiser M, Weisel K, van de Donk NWCJ, Waage A, Beksac M, Mellqvist UH, Engelhardt M, Caers J, Driessen C, Bladé J, Sonneveld P. Prevention and management of adverse events of novel agents in multiple myeloma: a consensus of the European Myeloma Network. Leukemia. 2018 Jul;32(7):1542–60.
    参考文献:10.1007/s00277-019-03739-2
    摘要:Spicka I, Ocio EM, Oakervee HE, Greil R, Banh RH, Huang S, D’Rozario JM, Dimopoulos MA, Martínez S, Extremera S, Kahatt C, Alfaro V, Carella AM, Meuleman N, Hájek R, Symeonidis A, Min C, Cannell P, Ludwig H, Sonneveld P, Mateos MV. Randomized phase III study (ADMYRE) of plitidepsin in combination with dexamethasone vs. dexamethasone alone in patients with relapsed/refractory multiple myeloma. Annals of Hematology. 2019 Jun 25;98(9):2139–50. doi: 10.1007/s00277-019-03739-2.
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