CAS: 3562-63-8; Megestrol

该化合物是一种合成蛋白质,是一种模仿 progneroone(一种月经周期和怀孕过程中的自然激素)效应的激素,主要用于医疗环境,治疗厌食症,缓冲症,慢性病患者体重下降等症状,以及某些类型的癌症,特别是乳腺癌和内脏癌;Megestrol的特征是其刺激食欲和促进体重增长的能力;化学学上,它是一种17-羟丙酮的衍生物,具有类固醇结构,典型的是蛋白质;该物质通常以口服悬浮或药片的形式施用,其药理效应包括调控各种生理过程,例如对月经周期的调控和妊娠的保持;与任何药物一样,Megestrol可以产生副作用,其使用应当由保健专业人员加以监测.

结构式图片

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CAS号595-33-5 醋酸甲地孕酮 | CAS号520-85-4 甲羟孕酮 | CAS号71-58-9 安宫黄体酮

合成工艺路线路线简述

    醋酸甲羟孕酮置于sodium Methylate,四氯苯醌体系中,化学反应生成甲地孕酮
    参考文献:De Ruggieri Et Al.,Annali Di Chimica,1959,Vol. 49,P. 1371,1376
    标题:De Ruggieri Et Al.,Annali Di Chimica,1959,Vol. 49,P. 1371,1376

    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-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-7816544-B2
    优先权日:2004-03-23
    标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species
    发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A
    权利人:UNIV BOSTON
    摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-8404088-B2
    优先权日:2006-05-22
    标 题:Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids
    发明人:PORCO JR JOHN A; GERARD BAUDOUIN
    权利人:PORCO JR JOHN A; GERARD BAUDOUIN; UNIV BOSTON
    摘要:The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

    专利号:US-2024209029-A1
    优先权日:2021-04-21
    标题:Adiponectin glycopeptides and compositions and methods of use thereof
    发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
    权利人:UNIV HONG KONG
    摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.
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    主要参考文献


    1: Schacter L, Rozencweig M, Canetta R, Kelley S, Nicaise C, Smaldone L. Megestrol acetate: clinical experience. Cancer Treat Rev. 1989 Mar;16(1):49-63. doi: 10.1016/0305-7372(89)90004-2. 10(3):141-57. doi: 10.1016/0305-7372(83)90029-4. 194(5):700-2. 158(5):241-242. English, Spanish. doi: 10.1016/j.medcli.2021.04.019. Epub 2021 May 29. 35(10):1208-10. doi: 10.1345/aph.10197. 28(6):644-645. doi: 10.1016/j.jagp.2020.01.188. Epub 2020 Feb 2. 131(6):623-629.e1. doi: 10.1016/j.amjmed.2017.12.028. Epub 2018 Mar 6.
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    合成参考文献


    参考文献:10.1007/s10552-010-9513-x
    摘要:Beasley JM, Coronado GD, Livaudais J, Angeles-Llerenas A, Ortega-Olvera C, Romieu I, Lazcano-Ponce E, Torres-Mejía G. Alcohol and risk of breast cancer in Mexican women. Cancer Causes & Control. 2010 Feb 13;21(6):863–70. doi: 10.1007/s10552-010-9513-x.
    参考文献:10.1016/j.contraception.2010.11.017
    摘要:van Diepen HA, Lam TW, Kuil CW. Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey. Contraception. 2011 Aug;84(2):199–204. doi: 10.1016/j.contraception.2010.11.017.
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