CAS: 130308-48-4; ((2S,3As,7As)-1-((R)-2-(((S)-2-(2-((2S,4R)-1-(D-Arginyl-L-Arginyl-L-Prolyl)-4-Hydroxypyrrolidine-2-Carboxamido)Acetamido)-3-(Thiophen-2-yl)Propanoyl)-L-Seryl)-1,2,3,4-Tetrahydroisoquinoline-3-Carbonyl)Octahydro-1H-Indole-2-Carbonyl)-L-Arginine

该化合物是一种合成的peptide和一种选择性的bradykinin B2受体对抗剂,主要用于治疗遗传性血管肿肿,这是经常出现严重肿胀的症状.它的操作机制包括阻止粘膜基宁的影响,它是一种促进血管血管扩张和增加血管渗透性的peptide,从而减轻与血管肿有关的症状.Icatibant是通过下皮注射进行,并因其迅速行动而闻名.该物质有较短的半衰期,需要小心地服用以保持治疗水平.在化学结构方面,Icatibant是一种非pitite,它有助于其特性和效果,能够针对胸膜基因受体,它的安全性一般是有利的,其常见的副作用包括注射场反应和胃肠扰动.

结构式图片

上下游产品

N-(fluoren-9-ylmethoxycarbonyl)glycine Fm°C-Pro-OH Fm°C-Ser(tBu)-OH (2S,4R)-4-tert-butoxy-1-(9H-fluoren-9-ylmethoxycarbonyl)pyrrolidine-2-carboxylic acid

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    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-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:US-2020247841-A1
    优先权日:2017-09-27
    标 题 :Synthesis of icatibant
    发明人:RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha
    权利人:BIOCON LTD
    摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.

    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-2004110228-A1
    优先权日:2002-04-01
    标 题:Combinatorial organic synthesis of unique biologically active compounds
    发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
    摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
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    主要参考文献


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    合成参考文献


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    参考文献:10.1007/s10140-014-1242-0
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    参考文献:10.1007/s12576-015-0397-0
    摘要:Mizumura K, Taguchi T. Delayed onset muscle soreness: Involvement of neurotrophic factors. The Journal of Physiological Sciences. 2015 Oct 14;66(1):43–52. doi: 10.1007/s12576-015-0397-0.
    参考文献:10.1186/s13023-018-0815-5
    摘要:Aygören-Pürsün E, Magerl M, Maetzel A, Maurer M. Epidemiology of Bradykinin-mediated angioedema: a systematic investigation of epidemiological studies. Orphanet Journal of Rare Diseases. 2018 May 04;13(1):73. doi: 10.1186/s13023-018-0815-5.
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