CAS: 396091-73-9; Pasireotide

该化合物是一种合成环己酸盐和一种somatostatin模拟物,经过三氟乙酸(TFA)抗药性改造,以提高溶性性和稳定性,对索马图血受体(SSTS)具有高度的亲近性,特别是SSTR1,2,3和5,使它成为研究内分泌紊乱,包括昆虫病和库辛病的宝贵工具.TFA盐形式确保改进处理和储存特性,同时保持生物活动.它对生长激素和胰岛素类似生长因子-1(IGF-1)的强效抑制性影响突出它在临床前和临床研究中的效用.该化合物的供应具有高纯度,适合药理学和生物化学应用.

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欧盟法规

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上下游产品

2-CH2-NH-B°C)-Phg-D-Trp(B°C)-Lys(B°C)-Tyr(Bzl)-Phe]cyclo[Pro(4-°CO-NH-CH2-CH2-NH-B°C)-Phg-D-Trp(B°C)-Lys(B°C)-Tyr(Bzl)-Phe] bis(trichloromethyl) carbonate N-B°C-1,2-diaminoethane

合成工艺路线路线简述

    Cyclo[pro(4-oco-Nh-Ch2-Ch2-Nh-Boc)-Phg-D-Trp(Boc)-Lys(Boc)-Tyr(Bzl)-Phe]置于三异丙基硅烷,三氟乙酸体系中,用 水 用作溶剂,化学反应 1.0H,反应生成帕瑞肽
    参考文献: Novel Process For The Preparation Of Pasireotide[fr] Nouveau Procédé De Préparation De Pasiréotide
    标题: Novel Process For The Preparation Of Pasireotide[fr] Nouveau Procédé De Préparation De Pasiréotide
    摘要:本发明涉及一种用于制备化学式11的帕西瑞肽的新型工艺.该发明还涉及一种化学式8的新型中间化合物及其制备工艺,该中间化合物用于制备化合物11.

    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-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-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-10919882-B2
    优先权日:2019-05-09
    标题:Compounds for use in synthesis of peptidomimetics

    专利号:CA-2551859-C
    优先权日:2003-12-30
    标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

    专利号:JP-2025506322-A
    优先权日:2022-02-04
    标题 :Methods for the large scale synthesis of radionuclide complexes.
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    主要参考文献


    1: Silverstein JM. Hyperglycemia induced by pasireotide in patients with Cushing's disease or acromegaly. Pituitary. 2016 Oct;19(5):536-43. doi: 10.1007/s11102-016-0734-1. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK349174/ doi: 10.2147/DDDT.S77999. eCollection 2016 Jan 11. Review.
    4: Wildemberg LE, Gadelha MR. Pasireotide for the treatment of acromegaly. Expert Opin Pharmacother. 2016;17(4):579-88. doi: 10.1517/14656566.2016.1146688. Epub 2016 Feb 17. Review. doi: 10.1007/s40265-015-0413-y. Review. doi: 10.2147/TCRM.S37314. eCollection 2015 Mar 17. Review.
    7: Ben-Shlomo A. Pharmacotherapy for acromegaly: future role for pasireotide? Endocrinol Metab Clin North Am. 2015 Mar;44(1):35-41. doi: 10.1016/j.ecl.2014.10.004. Epub 2014 Nov 4. Review. doi: 10.1055/s-0034-1376988. Epub 2014 Jul 8. Review. doi: 10.1007/s11102-014-0582-9. Review. doi: 10.4158/EP13127.RA. Review. doi: 10.1007/s40265-013-0052-0. Review. doi: 10.1007/s11102-013-0483-3. Review.

    合成参考文献


    参考文献:10.1159/000094325
    摘要:Labeur M, Theodoropoulou M, Sievers C, Paez-Pereda M, Castillo V, Arzt E, Stalla GK. New aspects in the diagnosis and treatment of Cushing disease. Front Horm Res. 2006;35():169–78. doi: 10.1159/000094325.
    摘要:From The Merck Index.
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