CAS: 443913-73-3; N-(4-Bromo-2-Fluorophenyl)-6-Methoxy-7-((1-Methylpiperidin-4-yl)Methoxy)Quinazolin-4-Amine

该化合物是一种主要用于治疗甲状腺癌的微分子气旋性激素抑制剂,主要用于治疗甲状腺癌,针对多种受体性气旋性激素抑制剂,包括血管内分泌增生受体(VeGFR),上皮生长因受体(EGFR)和在移植过程中重新排列,这涉及到肿瘤的生长和血管产生.Vandetanib的化学配方为C22H24N4O2S,分子重量约为396.52克/摩尔.这种复合物通常通过口服,表现出中度到高的生物利用率.Vandetanib因潜在的副作用而闻名,其中可能包括腹泻,高血压,疲劳和皮肤皮疹等,其行动机制包括抑制肿瘤细胞扩散和减少对肿瘤的血液供应,使其成为重要的肿瘤治疗选择.与任何药物一样,医疗专业人员应密切监测其使用情况,以管理任何不良效果和确保功效.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号50-00-0 甲醛 | CAS号338992-12-4 N-(4-溴-2-氟苯基)-6... | CAS号338992-20-4 4-((4-(4-溴-2-氟苯... | CAS号367-24-8 4-溴-2-氟苯胺 | CAS号264208-72-2 4-氯-6-甲氧基-7-[(1... | CAS号162364-72-9 7-苄氧基-4-氯-6-甲氧基喹唑啉 | CAS号196603-96-0 4-(4-溴-2-氟苯胺基)-... | CAS号768350-54-5 7-(苄氧基)-4-(4-溴-...

合成工艺路线路线简述

    7-苄氧基-4-氯-6-甲氧基喹唑啉置于盐酸,Sodium Triacetoxyborohydride,Potassium Carbonate,溶剂黄146,三氟乙酸体系中,用 甲醇,二氯甲烷,水,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 7.0H,反应生成 凡德他尼
    参考文献:Radiosynthesis Of [11C]Vandetanib And [11C]Chloro-Vandetanib As New Potential Pet Agents For Imaging Of Vegfr In Cancer
    标题:Radiosynthesis Of [11C]Vandetanib And [11C]Chloro-Vandetanib As New Potential Pet Agents For Imaging Of Vegfr In Cancer
    摘要:Vandetanib (Zd6474) And Its Chlorine Analogue Chloro-Vandetanib Are Potent And Selective Vascular Endothelial Growth Factor Receptor (Vegfr) Tyrosine Kinase Inhibitors With Low Nanomolar Ic50 Values. [c-11]Vandetanib And [c-11]Chloro-Vandetanib,New Potential Pet Agents For Imaging Of Vegfr In Cancer,Were First Designed,Synthesized And Labeled At Nitrogen And Oxygen Positions From Their Corresponding N-And O-Des-Methylated Precursors,In 40-50% Decay Corrected Radiochemical Yield And 370-555 Gbq/mu Mol Specific Activity At End Of Bombardment (Eob). (C) 2011 Elsevier Ltd. All Rights Reserved.
    DOI:10.1016/j.Bmcl.2011.04.049

    海关参考信息

    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-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    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-11155562-B2
    优先权日:2014-06-30
    标 题 :Synthesis of halichondrin analogs and uses thereof
    发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
    权利人:HARVARD COLLEGE
    摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.

    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.
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    主要参考文献


    1: Mormando M, Lauretta R, Puliani G, Bianchini M, Spoltore ME, Appetecchia M. Treatment Outcomes and Toxicities of Multiple Tyrosin Kinase Inhibitors for Metastatic Medullary Thyroid Cancer: A Case Series. Biomedicines. 2024 Dec 23;12(12):2923. doi: 10.3390/biomedicines12122923. 24(1):1569. doi: 10.1186/s12885-024-13345-9.
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    合成参考文献


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    参考文献:10.4061/2011/678357
    摘要:Prazeres H, Torres J, Rodrigues F, Couto JP, Vinagre J, Sobrinho-Simões M, Soares P. How to Treat a Signal Current Basis for RET-Genotype-Oriented Choice of Kinase Inhibitors for the Treatment of Medullary Thyroid Cancer. Journal of Thyroid Research. 2011;2011():1–10. doi: 10.4061/2011/678357.
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