CAS: 2920-86-7; Prednisolone Succinate

该化合物是一种该化合物是一种合成溶液,其关键优势在于溶液溶性增强,有助于静脉注射或肌肉内管理,以迅速系统交付.杂交会提高生物利用率,同时保留母化合物的抗炎,免疫抑制和代谢效应.在需要迅速采取行动的急性治疗环境中,这种衍生物特别有用,如严重过敏反应或炎热条件.其酯联系使活性水解高效,释放活性前硝酮.该化合物因其可靠的药用基因特征和与液体配方的兼容性,在临床和研究应用中被广泛使用.

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CAS号108-30-5 丁二酸酐 | CAS号50-24-8 泼尼松龙 | CAS号570370-45-5 (5-nitrothien-2... | CAS号50-24-8 泼尼松龙

合成工艺路线路线简述

    📜丁二酸酐,泼尼松龙置于吡啶,盐酸体系中,用 水 用作溶剂,化学反应 24.0H,以63%的收率获得泼尼松龙半琥珀酸酯
    参考文献:泼尼松龙-α-环糊精-星形peg聚伪轮烷,具有受控的药物递送特性† ‡
    标题:泼尼松龙-α-环糊精-星形peg聚伪轮烷,具有受控的药物递送特性† ‡
    摘要:的反应 α-氨基-ω-甲氧基聚(乙二醇)[ M = 5000]或星号α-氨基聚乙二醇[ M = 20 000],半个学期泼尼松龙 二元羧酸(琥珀酸,戊二酸,己二酸,邻苯二甲酸)已用于制备相应的缀合物.共轭物的酯酶催化水解速率由聚乙二醇的分子量和之间的连接基团的长度控制泼尼松龙和聚(乙二醇)(τ 1/2〜5-0.5小时).酶促水解在与己二酸和邻苯二甲酸衍生的接头偶联时最迅速进行.合成的共轭物与α-环糊精其通过2D Noesy NMR光谱,粉末x射线衍射图以及在一种情况下还通过stm显微镜进行表征.在具有由以下物质衍生的连接基的聚假轮烷中己二酸,酶促释放进行约.慢五倍泼尼松龙从相应的结合物中释放.以...的速率泼尼松龙 从载体中的释放可通过三个因素控制:聚合物载体与聚合物之间的连接基的特性. 泼尼松龙,聚乙二醇的分子量和与 α-环糊精.合成的聚伪轮烷代表了新的有望用于靶标释放的转运系统泼尼松龙
    Doi:10.1039/c0Ob00039F

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    专利信息


    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:WO-9709067-A1
    优先权日:1995-09-05
    标 题 :Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids
    发明人：BURCHARDT ELMAR-REINHOLD; MUELLER-PEDDINGHAUS REINER
    权利人:BAYER AG; BURCHARDT ELMAR REINHOLD; MUELLER PEDDINGHAUS REINER
    摘要:The combination is disclosed of 5-lipoxygenase inhibitors as direct action lipoxygenase inhibitors (LOI) or of leukotriene synthesis inhibitors (LSI) with glucocorticosteroids (GCS). This combination is suitable for treating and preventing various acute and chronic inflammatory processes, in particular of the respiratory tract, and may therefore be used as a medicament, in particular for treating asthma.

    专利号:US-10239856-B2
    优先权日:2008-01-15
    标题:Synthesis of resorcylic acid lactones useful as therapeutic agents

    专利号:CN-101990399-B
    优先权日:2008-01-15
    标 题:Synthesis of dihydroxybenzoic acid lactones as therapeutic agents

    专利号:US-2011217335-A1
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents

    专利号:US-2016075677-A1
    优先权日:2008-01-15
    标 题:Synthesis of resorcylic acid lactones useful as therapeutic agents

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    合成参考文献


    摘要:KNICK B, WAGNER HJ. [Therapeutic studies with ACTH, cortisone & prednisolone (solu-decortin H) in acute alcoholic intoxication; observations on the treatment of full drunkenness in youngsters, clinical tests & animal experiments with alcoholic intoxication]. Arztl Wochensch. 1958 Dec 12;13(50):1110–4.
    摘要:Su J, Bachmann G, Tang A, Zumegen C, Michel O, Wittekindt C. [The different levels of prednisolone in perilymph after local and systemic treatment]. Lin Chuang Er Bi Yan Hou Ke Za Zhi. 2003 Oct;17(10):615–7.
    参考文献:10.1021/jm0102811
    摘要:Farr CD, Tabet MR, Ball WJ, Fishwild DM, Wang X, Nair AC, Welsh WJ. Three-dimensional quantitative structure-activity relationship analysis of ligand binding to human sequence antidigoxin monoclonal antibodies using comparative molecular field analysis. J Med Chem. 2002 Jul 18;45(15):3257–70. doi: 10.1021/jm0102811.
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