CAS: 108852-90-0; Nemorubicin

该化合物是一种主要用于癌症治疗,特别是抗肿瘤特性的炭疽抗生素,主要用于抗癌治疗,它源于天然产物达诺丁辛,以其能相互授精DNA,从而抑制DNA和RNA合成,最终导致细胞死亡.内莫罗比辛的化学结构包括一个四环系统,其特征是炭疽环,有助于其生物活动.它展示了多种针对各种癌症的活动,包括白血病和固态肿瘤.它也因其潜在的心毒性而得到注意,一种与炭疽衍生物相关的共同副作用,需要在治疗期间进行仔细监测.此外,对甲虫菌素进行了有关其致癌学学的研究,其中包括吸收,分布,新陈代谢和体内排泄.研究继续探索其功效和安全特征,以及与其他治疗剂进行可能的结合,以加强其抗癌作用,同时尽量减少不良反应.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    📜Doxorubicin Hydrochloride,2-[(1S)-1-Methoxy-2-Oxoethoxy]Acetaldehyde置于doxorubicin Hydrochloride体系中,用55的收率获得奈莫柔比星
    参考文献:Morpholino Derivatives Of Daunorubicin And Doxorubicin
    标题:Morpholino Derivatives Of Daunorubicin And Doxorubicin
    摘要:通式(a)的蒽环类糖苷:##str1## 其中x是氢或羟基,R是氢,甲基或羟甲基;及其药学上可接受的盐,可用作抗肿瘤剂.

    专利信息


    专利号:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    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-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Broggini M. Nemorubicin. Top Curr Chem. 2008;283:191-206. doi: 10.1007/128_2007_6. 1860(6):1129-38. doi: 10.1016/j.bbagen.2016.02.011. Epub 2016 Feb 23. 30(2):614-624. doi: 10.1021/acs.chemrestox.6b00362. Epub 2017 Jan 25. 11(4):1608-17. doi: 10.1158/1078-0432.CCR-04-1845. 20(24):6979-88. doi: 10.1016/j.bmc.2012.10.033. Epub 2012 Nov 3. 30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28. 76(6):784-95. doi: 10.1016/j.bcp.2008.07.003. Epub 2008 Jul 11.
    9:2. doi: 10.20517/cdr.2025.151.
    9: Fraier D, Frigerio E, Brianceschi G, James CA. LC-MS-MS determination of nemorubicin (methoxymorpholinyldoxorubicin, PNU-152243A) and its 13-OH metabolite (PNU-155051A) in human plasma. J Pharm Biomed Anal. 2002 Oct 15;30(3):377-89. doi: 10.1016/s0731-7085(02)00222-4. 30(3):oyae267. doi: 10.1093/oncolo/oyae267.

    合成参考文献


    参考文献:10.1023/a:1014415205955
    摘要:Leontieva OV, Preobrazhenskaya MN, Bernacki RJ. Partial circumvention of P-glycoprotein-mediated multidrug resistance by doxorubicin-14-O-hemiadipate. Invest New Drugs. 2002 Feb;20(1):35–48. doi: 10.1023/a:1014415205955.
    参考文献:10.1007/128_2007_4
    摘要:Koch TH, Barthel BL, Kalet BT, Rudnicki DL, Post GC, Burkhart DJ. Anthracycline-formaldehyde conjugates and their targeted prodrugs. Top Curr Chem. 2008;283():141–70. doi: 10.1007/128_2007_4.
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