CAS: 89778-27-8; Toremifene Citrate

该化合物是一种选择性雌激素受体调节器(SERM),主要用于治疗乳腺癌,特别是绝经后的妇女,其功能是约束雌激素受体,从而抑制雌激素对乳腺组织的影响,这有助于减缓或阻止依赖雌激素的肿瘤的生长.该化合物的特点是其化学结构,包括三苯乙烯脊椎,有助于其选择性地调节雌激素活动的能力.托雷米芬内氏血清通常通过口述方式施用,并因其相对优于其他激素疗法的副作用而闻名.它也可能对骨骼和脂肪新陈代谢产生一些不耐性影响,在某些情况下可能有所助益.该物质通常在胃肠道中沉浸,其新陈代谢主要发生在肝脏中.与任何药物一样,治疗期间,对潜在副作用的监测,如热闪光或血栓血症等,是必不可少的.总的来说,托雷米内氏体是一个重要的治疗选择.

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citric acid toremifene

合成工艺路线路线简述

    柠檬酸,托瑞米芬 以 丙酮 作为反应溶剂,化学反应生成 枸橼酸托瑞米芬
    参考文献:Polymorphic Form Of Toremifene Citrate And Process For Its Preparation
    标题:Polymorphic Form Of Toremifene Citrate And Process For Its Preparation
    摘要:本发明提供了托瑞米芬柠檬酸盐的多晶型及其制备方法.它还涉及一种改进的托瑞米芬基z异构体的制备方法,不含e异构体,以及其药学上可接受的盐.

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    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    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.
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    主要参考文献


    1: Gerken P. Toremifene citrate (Fareston). Clin J Oncol Nurs. 2004 Oct;8(5):529-30. doi: 10.1188/04.CJON.529-530. 14(1):1-9. doi: 10.1016/j.clbc.2013.10.014. Epub 2013 Oct 31. 25(8):955-9. doi: 10.1081/ddc-100102257. 195(1-2):219-27. doi: 10.1016/s0378-5173(99)00403-2. 136(3):467-72. doi: 10.1039/c0an00487a. Epub 2010 Nov 29. 4(3):147-52. doi: 10.1097/SPC.0b013e32833bd913. 181(2):181-91. doi: 10.1016/s0378-5173(99)00022-8. 63(4):187-94. doi: 10.18926/AMO/31816.
    95:107181. doi: 10.1016/j.ijscr.2022.107181. Epub 2022 May 11.
    10: Toimela T, Salminen L, Tähti H. Effects of tamoxifen, toremifene and chloroquine on the lysosomal enzymes in cultured retinal pigment epithelial cells. Pharmacol Toxicol. 1998 Dec;83(6):246-51. doi: 10.1111/j.1600-0773.1998.tb01477.x. 27(2):245-9. Japanese. 212(1):121-30. doi: 10.1016/s0378-5173(00)00601-3. 94(10):4809-4819. doi: 10.1002/jmv.27951. Epub 2022 Jul 1.

    合成参考文献


    摘要:
    摘要:Oyo Yakuri. Pharmacometrics., 44(351), 1992
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