CAS: 103222-11-3; 13-((1H-Indol-3-yl)Methyl)-N-(1-Amino-3-(1H-Indol-3-yl)-1-Oxopropan-2-yl)-19-(2-Amino-3-Phenylpropanamido)-10-(4-Aminobutyl)-16-(4-Hydroxybenzyl)-7-Isopropyl-6,9,12,15,18-Pentaoxo-1,2-Dithia-5,8,11,14,17-Pentaazacycloicosane-4-Carboxamide

该化合物是一种环状虫酸,其特点是一种独特的氨酸安排,它由peptide结合,并通过细胞残留物之间的脱硫桥而稳定.这种化合物具有循环结构的特点,它比线性peptine更具稳定性和生物活性.芳香氨酸,如锥虫和苯丙胺,的存在,有助于它与生物目标的潜在相互作用,可能影响...

结构式图片

MSDS等安全信息

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-12351573-B2
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; CHENG KAI FAN
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

    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-2023159450-A1
    优先权日:2020-05-08
    标 题 :Dimers for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

    专利号:WO-2023148680-A1
    优先权日:2022-02-04
    标 题 :Methods for large scale synthesis of radionuclide complexes
    发明人:BARBATO DONATO; BO MICHELE; ROSSETTO MATTIA; TEDESCO MATTIA; VALERIO FEDERICO
    权利人:ADVANCED ACCELERATOR APPLICATIONS
    摘要:The present disclosure relates to methods of large scale synthesis of radionuclide complex solutions having a high activity for diagnostic and/or therapeutic purposes, their use in the commercial production of radioactive drug substances, and to respective solutions as well as containers comprising said solutions.

    专利号:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

    专利号:US-2009162290-A1
    优先权日:2005-09-09
    标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof
    发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN
    权利人:THERAPHARM GMBH
    摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
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    主要参考文献


    1: Saha S, Sharma A, Bhowmik D, Kumar D. Investigation into in silico and in vitro approaches for inhibitors targeting MCM10 in Leishmania donovani: a comprehensive study. Mol Divers. 2024 May 9. doi: 10.1007/s11030-024-10876-y. Epub ahead of print. 43(3):e202300284. doi: 10.1002/minf.202300284. Epub 2024 Feb 6. 60(2):152-159. doi: 10.4103/ijc.IJC_280_21. 40(6):1824-1837. doi: 10.1007/s12640-022-00588-2. Epub 2022 Nov 15. 20(8):1770-1778. doi: 10.1016/j.pan.2020.10.043. Epub 2020 Oct 22. 16(3):508-518. doi: 10.5114/aoms.2020.94567.
    7: Abdellatif AAH. A plausible way for excretion of metal nanoparticles via active targeting. Drug Dev Ind Pharm. 2020 May;46(5):744-750. doi: 10.1080/03639045.2020.1752710. Epub 2020 Apr 15. 31(3):035603. doi: 10.1088/1361-6528/ab4836. Epub 2019 Sep 26. 43(7):1788-1801. doi: 10.1007/s00268-019-04956-6. 26(8):1162-1169. doi: 10.1016/j.jsps.2018.07.004. Epub 2018 Jul 20.
    11: Zhu R, Li Y, Zhang X, Bian K, Yang M, Cong C, Cheng X, Zhao S, Li X, Gao D. Vapreotide-mediated hierarchical mineralized Ag/Au nanoshells for photothermal anti-tumor therapy. Nanotechnology. 2019 Feb 1;30(5):055602. doi: 10.1088/1361-6528/aaf0db.

    合成参考文献


    摘要:A2442: Betoin F, Advenier C, Fardin V, Wilcox G, Lavarenne J, Eschalier A: In vitro and in vivo evidence for a tachykinin NK1 receptor antagonist effect of vapreotide, an analgesic cyclic analog of somatostatin. Eur J Pharmacol. 1995 Jun 12;279(2-3):241-9.
    参考文献:10.1053/paor.1999.0176
    摘要:Zalatnai A. Epidermal growth factor receptor, somatostatin and bcl-2 in human pancreatic tumor xenografts. An immunohistochemical study. Pathol Oncol Res. 1999;5(2):146–51. doi: 10.1053/paor.1999.0176.
    参考文献:10.1021/bc980121c|10.1021/bc9900688
    摘要:Decristoforo C, Mather SJ. Preparation, 99mTc-Labeling, and in Vitro Characterization of HYNIC and N3S Modified RC-160 and [Tyr3]Octreotide. Bioconjugate Chem. 1999 Mar 31;10(3):431–8. doi: 10.1021/bc980121c.
    参考文献:10.1053/snuc.2002.31020
    摘要:Warner RR, O'dorisio TM. Radiolabeled peptides in diagnosis and tumor imaging: clinical overview. Semin Nucl Med. 2002 Apr;32(2):79–83. doi: 10.1053/snuc.2002.31020.
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