CAS: 59917-39-4; Methyl (5S,7S,9S)-9-((3Ar,3A1R,4R,5S,5Ar,10Br)-5-Carbamoyl-3A-Ethyl-4,5-Dihydroxy-8-Methoxy-6-Methyl-3A,3A1,4,5,5A,6,11,12-Octahydro-1H-Indolizino[8,1-Cd]Carbazol-9-yl)-5-Ethyl-5-Hydroxy-1,4,5,6,7,8,9,10-Octahydro-2H-3,7-Methano[1]Azacycloundecino[5,4-B]Indole-9-Carboxylate Sulfate

该化合物是一种主要用作化疗中抗乳粉剂的合成松脂碱性碱性碱性衍生物,它通过对管状素捆绑,抑制微囊形成,干扰线性脊椎组装,从而在G2/M阶段阻止细胞分解,从而在G2/M阶段对迅速扩散的癌症细胞有效.硫酸二甲酯因其中度和毒性特征而与其他氯碱性碱性物质相比特别突出,它提供了功效与可管理的副作用之间的平衡.它通常用于治疗白血病,淋巴瘤和某些固态肿瘤.硫酸盐形式可以增强溶性性和稳定性,便于临床应用中的精确剂量.

结构式图片

欧盟法规

C&L通报REACH预注册

合成工艺路线路线简述

    海关参考信息

    专利信息


    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: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-10342858-B2
    优先权日:2015-01-24
    标题 :Glycan conjugates and methods of use thereof
    发明人:WONG CHI-HUEY; WU CHUNG-YI
    权利人:ACADEMIA SINICA
    摘要:The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series 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 globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. 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.

    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.
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    主要参考文献


    1: Cersosimo RJ, Bromer R, Licciardello JT, Hong WK. Pharmacology, clinical efficacy and adverse effects of vindesine sulfate, a new vinca alkaloid. Pharmacotherapy. 1983 Sep-Oct;3(5):259-74. doi: 10.1002/j.1875-9114.1983.tb03269.x. 26(5-6):497-506. doi: 10.3109/10428199709050886. 39(3):12. doi: 10.1097/01.NURSE.0000347050.21740.8c. 28(23):3739-45. doi: 10.1200/JCO.2009.24.5050. Epub 2010 Jul 12. 85(2):433-441. doi: 10.1007/s00280-019-03972-6. Epub 2019 Nov 5. 44(6):875-882. doi: 10.1111/jcpt.13007. Epub 2019 Sep 17. 52(3):369-75. doi: 10.1038/bjc.1985.203.
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    合成参考文献


    摘要:L1022: Wikipedia. Vindesine. Last Updated 2 April 2009.
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    参考文献:10.1007/bf02913474
    摘要:Masaki Y, Gomibuchi M, Tanaka S. Carcinoma positive for Epstein-Barr virus staining. Mediastinal lymph node origination Jpn J Thorac Cardiovasc Surg. 2002 Mar;50(3):122–4. doi: 10.1007/bf02913474.
    参考文献:10.1007/bf02982552
    摘要:Maeda T, Yamada Y, Tawara M, Yamasaki R, Yakata Y, Tsutsumi C, Onimaru Y, Kamihira S, Tomonaga M. Successful Treatment With a Chimeric Anti-CD20 Monoclonal Antibody (IDEC-C2B8, Rituximab) for a Patient With Relapsed Mantle Cell Lymphoma Who Developed a Human Anti-Chimeric Antibody. International Journal of Hematology. 2001 Jul 01;74(1):70–5. doi: 10.1007/bf02982552.
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