CAS: 65807-02-5; (S)-N-((6S,9S,12R,15S,18S,21S,24S)-21-((1H-Indol-3-yl)Methyl)-1-Amino-12-(Tert-Butoxymethyl)-6-((S)-2-(2-Carbamoylhydrazine-1-Carbonyl)Pyrrolidine-1-Carbonyl)-15-(4-Hydroxybenzyl)-18-(Hydroxymethyl)-25-(1H-Imidazol-4-yl)-1-Imino-9-Isobutyl-8,11,14,17,20,23-Hexaoxo-2,7,10,13,16,19,22-Heptaazapentacosan-24-yl)-5-Oxopyrrolidine-2-Carboxamide

该化合物是一种合成的peptide 类比性激素(GnRH),主要用于治疗前列腺癌,乳腺癌和内分泌性硬化等对激素敏感的病症.它作为GnRH的激动剂,最初刺激润滑性激素(LH)和泡泡激素(FSH)的释放,随后通过负面反馈机制导致性激素产量下降.Goserelin 是通过亚皮层植入来施用,长期释放该药物.它的化学结构包括一系列氨基酸,它模拟自然激素,使其有效与GnRH受体结合.该物质的特点在于它能够抑制淋热性激素(LH)和泡泡泡激素(FSH)的产生,因此对管理因性激素而加剧的条件很有价值.常见的副作用可能包括热闪光,减少性激素,以及长期抑制激素的潜在骨密度损失.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-11873305-B2
    优先权日:2020-06-30
    标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
    发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
    权利人:GENENTECH INC; HOFFMANN LA ROCHE
    摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

    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:EP-0443532-B1
    优先权日:1990-02-20
    标题:Temporary minimal protection synthesis of LH-RH analogs
    发明人:NESTOR JOHN J JR; MCCLURE NATALIE L
    权利人:SYNTEX INC
    摘要:A solid phase synthesis of LH-RH analogs in which the amino acids serine and histidine, if present, are side chain protected during the synthesis with groups labile to selected alpha -amino or deprotecting agents.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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
    杭州阿诺生物医药科技有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.adlainortye.com
    电话: 0571-28918366👤
    📞杭州阿诺生物医药科技有限公司 ⚠️参考联系方式

    销售电话:0571-28918366
    邮箱:info@adlainortye.com
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    四川吉晟生物医药有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.jsjpharm.cn
    电话: 0833-2598983👤
    📞四川吉晟生物医药有限公司 ⚠️参考联系方式

    销售电话:0833-2598983
    邮箱:marketing@jsjpharm.cn
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    浙江湃肽生物股份有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.peptide-china.com
    电话: 0571-89197072; 18668118770👤
    📞浙江湃肽生物股份有限公司 ⚠️参考联系方式

    销售电话:0571-89197072; 18668118770
    邮箱:linda@peptide-china.com
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别 ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    第 1 / 1 页
    现货

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548740/ Available from http://www.ncbi.nlm.nih.gov/books/NBK547863/ doi: 10.3892/mco.2019.1913. Epub 2019 Aug 20.
    5: Maguire MJ, Nevitt SJ. Treatments for seizures in catamenial (menstrual-related) epilepsy. Cochrane Database Syst Rev. 2019 Oct 14;10:CD013225. doi: 10.1002/14651858.CD013225.pub2. [Epub ahead of print] Review. doi: 10.1055/s-0039-1695737. Epub 2019 Sep 23. Adding Ovarian Suppression to Tamoxifen for Premenopausal Breast Cancer: A Randomized Phase III Trial. J Clin Oncol. 2019 Sep
    16:JCO1900126. doi: 10.1200/JCO.19.00126. [Epub ahead of print] doi: 10.2217/cer-2019-0038. Epub 2019 Aug 23. doi: 10.4111/icu.2019.60.4.244. Epub 2019 May 21.

    合成参考文献


    摘要:Ikeda K, Ogawa Y, Nagahara H, Xiang Z, Sakurai K, Fukuoka T, Tokunaga S, Nishiguchi Y. [Evaluation of pain reduction upon injecting goserelin acetate using an ice pack]. Gan To Kagaku Ryoho. 2010 Feb;37(2):291–3.
    参考文献:10.1007/s10549-005-9039-1
    摘要:Eichbaum MH, Kaltwasser M, Bruckner T, de Rossi TM, Schneeweiss A, Sohn C. Prognostic factors for patients with liver metastases from breast cancer. Breast Cancer Res Treat. 2006 Mar;96(1):53–62. doi: 10.1007/s10549-005-9039-1.
    参考文献:10.1056/nejmoa1012348
    摘要:Jones CU, Hunt D, McGowan DG, Amin MB, Chetner MP, Bruner DW, Leibenhaut MH, Husain SM, Rotman M, Souhami L, Sandler HM, Shipley WU. Radiotherapy and short-term androgen deprivation for localized prostate cancer. N Engl J Med. 2011 Jul 14;365(2):107–18. doi: 10.1056/nejmoa1012348.
    参考文献:10.1590/s1806-37132011000300015
    摘要:Baldi BG, Medeiros Junior P, Pimenta SP, Lopes RI, Kairalla RA, Carvalho CR. Evolution of pulmonary function after treatment with goserelin in patients with lymphangioleiomyomatosis. J Bras Pneumol. 2011 May;37(3):375–9. doi: 10.1590/s1806-37132011000300015.
    参考文献:10.1200/jco.2011.36.9850
    摘要:Blumenfeld Z. ZORO study: discrepancy between the conclusion and the results. J Clin Oncol. 2011 Aug 20;29(24):3340; author reply 3341–2. doi: 10.1200/jco.2011.36.9850.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知