CAS: 96346-61-1; (8S,11R,13R,14S,17S)-11-[4-(Dimethylamino)Phenyl]-17-Hydroxy-17-(3-Hydroxypropyl)-13-Methyl-1,2,6,7,8,11,12,14,15,16-Decahydrocyclopenta[a]Phenanthren-3-One

该化合物是一种合成类固醇和选择性丙酮受体调节器(SPRM),其主要特征是它能够抑制丙酮的动作,使它成为生殖健康和癌症研究,特别是治疗依赖蛋白酮的肿瘤的研究对象; 石对丙酮受体具有高度的亲近性,导致它有可能用于管理内分泌和子宫纤维等情况; 化合物以其独特的作用机制而著称,这可能会对某些组织产生抗生素效应; 就物理特性而言,Onapristone通常在室内温度上作为固体出现,在有机溶剂中可溶性; 其药理学特征表明它可能具有治疗效益和副作用,这是临床应用中的重要考虑因素; 持续的研究继续探索其在不同医学环境,特别是肿瘤和妇科方面的效力和安全.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    📜(5'R,8'S,11'R,13'R,14'S,17'S)-11'-[4-(Dimethylamino)Phenyl]-13'-Methyl-17'-[3-(Oxan-2-Yloxy)Propyl]Spiro[1,3-Dioxolane-2,3'-2,4,6,7,8,11,12,14,15,16-Decahydro-1H-Cyclopenta[a]Phenanthrene]-5',17'-Diol置于吡啶,硫酸体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,反应生成 奥那司酮
    参考文献:Methods For Onapristone Synthesis Dehydration And Deprotection
    标题:Methods For Onapristone Synthesis Dehydration And Deprotection
    摘要:本发明提供了使用酸性水解和硫酸在酒精溶液中脱水制备onapristone(ona)的方法和系统.

    海关参考信息

    专利信息


    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

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    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-10308676-B2
    优先权日:2015-09-25
    标题 :Methods of making onapristone intermediates
    发明人:TILSTAM ULF; PRONIUK STEFAN; BINDERNAGEL HOLGER; WERNER SILVIA; RAUTER HOLGER
    权利人:CONTEXT BIOPHARMA INC
    摘要:Methods and systems for making intermediates in the synthesis of onapristone are provided. Aspects include the photoconversion of onapristone synthesis intermediates using a narrow band frequency light source.

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    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: Rezai K, Chassard D, Denot C, Proniuk S, Zukiwski A, Gilles E, Ramos HL, Patat A, Bexon A, Lokiec F. A single-dose PK study of onapristone including the effect of food on absorption. Cancer Chemother Pharmacol. 2015 Jul;76(1):171-7. doi: 10.1007/s00280-015-2754-3. Epub 2015 May 26. doi: 10.1016/j.theriogenology.2015.03.024. Epub 2015 Apr 1. doi: 10.14670/HH-29.949. Epub 2014 Feb 6. doi: 10.1016/j.mce.2013.06.001. Epub 2013 Jun 7. doi: 10.1016/j.jsbmb.2009.05.013. Epub 2009 Jun 14. doi: 10.1371/journal.pone.0124756. eCollection 2015 Apr 21.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    参考文献:10.1074/jbc.274.31.21544
    摘要:Lin HH, Zentner MD, Ho HL, Kim KJ, Ann DK. The gene expression of the amiloride-sensitive epithelial sodium channel alpha-subunit is regulated by antagonistic effects between glucocorticoid hormone and ras pathways in salivary epithelial cells. J Biol Chem. 1999 Jul 30;274(31):21544–54. doi: 10.1074/jbc.274.31.21544.
    参考文献:10.1016/j.anireprosci.2008.02.004
    摘要:Pereira RM, Marques CC, Baptista MC, Vasques MI, Horta AE. Embryos and culture cells: a model for studying the effect of progesterone. Anim Reprod Sci. 2009 Mar;111(1):31–40. doi: 10.1016/j.anireprosci.2008.02.004.
    参考文献:10.1016/s1474-4422(03)00636-7
    摘要:Bradbury J. Antiprogesterone hope for inherited neuropathy. Lancet Neurol. 2004 Jan;3(1):6. doi: 10.1016/s1474-4422(03)00636-7.
    参考文献:10.1016/s0960-0760(96)00090-8
    摘要:Schubert C, Donath J, Michna H, Nishino Y. The antiovulatory activity of progesterone antagonists is not correlated to their antiprogestational potency in the rat. The Journal of Steroid Biochemistry and Molecular Biology. 1996 Sep;59(1):75–82. doi: 10.1016/s0960-0760(96)00090-8.
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