CAS: 183552-38-7; Abarelix

该化合物是一种合成激素和抗蛋激素激素,主要用于治疗前列腺癌.其行动机制包括抑制垂垂垂地格地的GNR受体,导致润滑激素(LH)和泡泡刺激激素(FSH)的分泌减少.这导致睾丸生产量减少,而睾丸生产量对于前列腺癌细胞的生长至关重要.巴列利克斯的特征是,它有能力在不与GNRH诱导剂相关的初始激增的情况下,迅速抑制睾酮水平.它通过亚乳性注射进行控制,以其相对短的半衰期为人所知,需要小心下药.普通的副作用可能包括注射点反应,热闪光和利皮多的变化.作为浸泡剂,其结构由氨酸的具体序列组成,有助于其生物活动及其在GNRRH-R-S反应中采用的方法的特性.

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    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-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-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.

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    主要参考文献


    1: Tombal B. New treatment paradigm for prostate cancer: abarelix initiation therapy for immediate testosterone suppression followed by a luteinizing hormone-releasing hormone agonist. BJU Int. 2012 Mar;109(6):E16; author reply E16-7. doi: 10.1111/j.1464-410X.2012.10983.x. doi: 10.1111/j.1464-410X.2011.10708.x. Epub 2011 Nov 16. doi: 10.1111/j.1365-2125.2010.03730.x.
    4: Retraction statement: Reconstitution of Plenaxis® (Abarelix) 100 mg for injection is more effective with a vortex-like mixer than when performed manually. J Pharm Pract. 2010 Feb;23(1):78. doi: 10.1177/0897190009360369. doi: 10.1111/j.1464-410X.2009.08924.x. Review. Review. Dose-escalated abarelix in androgen-independent prostate cancer: a phase I study. Anticancer Drugs. 2006 Oct;17(9):1075-9. Review.

    合成参考文献


    参考文献:10.1007/s00404-012-2672-0
    摘要:Figueiredo JBP, Nastri CO, Vieira ADD, Martins WP. Clomiphene combined with gonadotropins and GnRH antagonist versus conventional controlled ovarian hyperstimulation without clomiphene in women undergoing assisted reproductive techniques: systematic review and meta-analysis. Archives of Gynecology and Obstetrics. 2012 Dec 19;287(4):779–90. doi: 10.1007/s00404-012-2672-0.
    参考文献:10.1016/j.urology.2003.10.029
    摘要:Marks LS. Luteinizing hormone-releasing hormone agonists in the treatment of men with prostate cancer: timing, alternatives, and the 1-year implant. Urology. 2003 Dec 22;62(6 Suppl 1):36–42. doi: 10.1016/j.urology.2003.10.029.
    参考文献:10.1016/j.eururo.2004.05.006
    摘要:Weckermann D, Harzmann R. Hormone therapy in prostate cancer: LHRH antagonists versus LHRH analogues. Eur Urol. 2004 Sep;46(3):279–83; discussion 283. doi: 10.1016/j.eururo.2004.05.006.
    参考文献:10.2165/00024677-200504060-00002
    摘要:Amory JK. Male hormonal contraceptives: current status and future prospects. Treat Endocrinol. 2005;4(6):333–41. doi: 10.2165/00024677-200504060-00002.
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