CAS: 16506-27-7; 4-(5-(Bis(2-Chloroethyl)Amino)-1-Methyl-1H-Benzo[d]Imidazol-2-yl)Butanoic Acid

该化合物是一种双功能烷基剂,具有纯正的苯并环,结合了烷基组的特性和纯仿的特性,主要用于治疗慢性淋巴细胞白血病(CLL),非Hodgkin 淋巴瘤(NHL)的B细胞非Hodgkin 淋巴瘤(NHL)和多种血肿.该化合物的独特结构使得它与其他烷基剂交叉抗争最小化,提高了其在复发性或复发性病例中的效力.本德穆斯因通过碱性接触和断线,破坏细胞复制,诱发DNA损伤.其有利的毒性特征,包括减少我的乳房抑制,使其在特定治疗疗法中成为首选选择.临床研究支持它在单一疗法和组合疗法中的作用.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜盐酸苯达莫司汀置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应生成宾达氮芥
    参考文献: Novel Forms Of Bendamustine Free Base[fr] Nouvelles Formes De Base Libre De Bendamustine
    标题: Novel Forms Of Bendamustine Free Base[fr] Nouvelles Formes De Base Libre De Bendamustine
    摘要:本发明涉及苯达莫司缓释剂型的新型多晶型,包括非晶态苯达莫司缓释剂型,六种无水晶型,四种水合晶型和五种溶剂晶型,同时还描述了它们的制备和使用方法.

    海关参考信息

    专利信息


    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.

    专利号:US-8828984-B2
    优先权日:2012-11-19
    标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
    发明人:CHE CHI MING; ZOU TAOTAO
    权利人:UNIV HONG KONG; UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

    专利号:US-10577387-B1
    优先权日:2018-08-09
    标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
    发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng
    权利人:UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Alrifai T, Grant Szymanski K, Venugopal P, Mahon B, Okwuosa T, Karmali R. Bendamustine and Rituximab: Complete Response in a 62-Year-Old Female with an Aggressive Lymphoma and an Ejection Fraction of 20. Chemotherapy. 2017;62(2):140-146. doi: 10.1159/000452756. Epub 2016 Dec 14. Review. doi: 10.3109/10428194.2015.1110748. Epub 2015 Dec 23. Review. doi: 10.3109/10428194.2015.1099647. Epub 2015 Nov 23. Review.
    4: Gentile M, Vigna E, Recchia AG, Morabito L, Mendicino F, Giagnuolo G, Morabito F. Bendamustine in multiple myeloma. Eur J Haematol. 2015 Nov;95(5):377-88. doi: 10.1111/ejh.12609. Epub 2015 Jul 14. Review. doi: 10.1007/s00280-015-2727-6. Epub 2015 Apr 1. Review.
    6: Kuno M, Inoue A, Aimoto M, Nakao T, Kameda K, Yoshida M, Kanashima H, Hirai M, Yamane T. [Alleviated anemia by bendamustine in cold agglutinin disease associated with small lymphocytic lymphoma]. Rinsho Ketsueki. 2015 Feb;56(2):204-9. doi: 10.11406/rinketsu.56.204. Review. Japanese. doi: 10.3109/10428194.2014.915545. Epub 2014 Jun 27. Review. doi: 10.1016/j.hemonc.2014.04.001. Epub 2014 Apr 29. Review. doi: 10.1007/s12032-014-0944-1. Epub 2014 Apr 22. Review.

    合成参考文献


    参考文献:10.1186/2047-783x-15-1-13
    摘要:Michael M, Bruns I, Bölke E, Zohren F, Czibere A, Safaian NN, Neumann F, Haas R, Kobbe G, Fenk R. Bendamustine in patients with relapsed or refractory multiple myeloma. European Journal of Medical Research. 2010 Jan 29;15(1):13. doi: 10.1186/2047-783x-15-1-13.
    参考文献:10.1007/s11912-011-0187-7
    摘要:Schatz JH. Targeting the PI3K/AKT/mTOR pathway in non-Hodgkin's lymphoma: results, biology, and development strategies. Curr Oncol Rep. 2011 Oct;13(5):398–406. doi: 10.1007/s11912-011-0187-7.
    参考文献:10.1007/s11912-011-0188-6
    摘要:Riches JC, Ramsay AG, Gribben JG. Chronic lymphocytic leukemia: an update on biology and treatment. Curr Oncol Rep. 2011 Oct;13(5):379–85. doi: 10.1007/s11912-011-0188-6.
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