CAS: 149003-01-0; (S)-4,4'-(Propane-1,2-Diyl)Bis(Piperazine-2,6-Dione) Xhydrochloride

该化合物是一种心血管保护剂和托波异构体酶II抑制剂,主要用于降低癌症化学治疗中炭碱诱发的心毒性风险,其机制包括切除无铁,防止形成反应性氧物种,从而减少对心脏组织的氧化损害.该化合物化学稳定,水溶性,并具有可预测的药理动因,确保治疗结果一致. 盐酸甲酸甲酯符合标准静脉注射管理规程,在临床环境中表现出效力,使其成为关键的肿瘤治疗辅助剂.其特征清晰的安全概况进一步支持其在高风险患者群中的使用.

结构式图片

合成工艺路线路线简述

    (S)-1,2-Diaminopropane-N,N,N',N'-Tetraacetic Acid Methyl Ester 反应生成右雷佐生盐酸盐
    参考文献:用于制备4,4'-(1-甲基-1,2-乙二基)-双-(2,6-哌嗪二酮)的新方法
    标题:用于制备4,4'-(1-甲基-1,2-乙二基)-双-(2,6-哌嗪二酮)的新方法
    摘要:本发明涉及通过在氨和甲酰胺的存在下式(II)四乙酸烷基酯的环化来制备式(I)化合物的新方法,以及在该方法中使用的式(II)化合物.

    海关参考信息

    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-2022118094-A1
    优先权日:2019-02-21
    标题:Synthesis of biomimetic cell wall structure
    发明人:WANG YONG; SHI PENG
    权利人:PENN STATE RES FOUND
    摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

    专利号:US-2018140724-A1
    优先权日:2015-05-27
    标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer
    发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A
    权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA
    摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.

    专利号:US-9868767-B2
    优先权日:2013-05-23
    标 题:Chemical synthesis and screening of bicyclic peptide libraries
    发明人:PEI DEHUA; UPADHYAYA PUNIT; LIAN WENLONG; TRINH THI
    权利人:OHIO STATE INNOVATION FOUNDATION
    摘要:Disclosed herein are bicyclic peptide compounds, compositions comprising same, methods for making same, and libraries comprising same. The disclosed compounds, in various aspects, are useful for treating a variety of disorders, including inflammatory disorders, autoimmune disorders, and disorders of uncontrolled cellular proliferation. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:US-8372881-B2
    优先权日:2005-06-20
    标题 :Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use
    发明人:ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A
    权利人:XENOPORT INC; ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A
    摘要:Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.
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    主要参考文献


    1: Henriksen PA. Anthracycline cardiotoxicity: an update on mechanisms, monitoring and prevention. Heart. 2018 Jun;104(12):971-977. doi: 10.1136/heartjnl-2017-312103. Epub 2017 Dec 7. Review. doi: 10.1007/s11897-017-0353-9. Review. doi: 10.1080/17425255.2017.1351547. Epub 2017 Jul 13. Review. doi: 10.1016/j.biopha.2017.04.033. Epub 2017 Apr 26. Review. doi: 10.1007/s10557-016-6711-0. Review.
    6: Henninger C, Fritz G. Statins in anthracycline-induced cardiotoxicity: Rac and Rho, and the heartbreakers. Cell Death Dis. 2017 Jan 19;8(1):e2564. doi: 10.1038/cddis.2016.418. Review.
    7: Fojtu M, Gumulec J, Stracina T, Raudenska M, Skotakova A, Vaculovicova M, Adam V, Babula P, Novakova M, Masarik M. Reduction of Doxorubicin-Induced Cardiotoxicity Using Nanocarriers: A Review. Curr Drug Metab. 2017;18(3):237-263. doi: 10.2174/1389200218666170105165444. Review. doi: 10.1152/ajpheart.00646.2016. Epub 2016 Dec 6. Review. Epub 2016 Oct 17. Review.
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