CAS: 38821-49-7; Carbidopa Monohydrate

该化合物是一种主要用于治疗帕金森病及其症状的药物化合物,它的作用是作为多帕除虫菊酯抑制剂,它防止在外围组织组织组织中将叶伏多巴转化为多巴胺,从而增加脑部的叶伏多巴的食用量,从而增强列伏多巴的治疗效应,同时尽量减少与外围多巴胺生产有关的副作用.单水合物形式表明,该化合物含有一种可影响其溶性与稳定性的卡宾洛巴分子的水分子.氨基多巴甲虫酸酯通常与异伏多巴结合使用,以优化治疗结果.其特征是白色和非白色晶体外的外观和水溶性,有利于口服剂量制剂的配制.该化合物一般都受到很好的调制,但在某些病人中可能会产生如恶心,眩晕和躁郁症等副作用.

结构式图片

欧盟法规

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L-DOPA ethyl ester (S)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid hydrobromide

合成工艺路线路线简述

    2(S)-氨基-3-(3,4-二羟基苯基)丙酸乙酯 反应生成 卡比多巴单水合物
    参考文献:Dual Release Formulation Comprising Levodopa Ethyl Ester And A Decarboxylase Inhibitor In Immediate Release Layer With Levodopa Ethyl Ester And A Decarboxylase Inhibitor In A Controlled Release Core
    标题:Dual Release Formulation Comprising Levodopa Ethyl Ester And A Decarboxylase Inhibitor In Immediate Release Layer With Levodopa Ethyl Ester And A Decarboxylase Inhibitor In A Controlled Release Core
    摘要:一种药片,包括:内部核心,用于控制释放,包括以下混合物:(a)去羧化酶抑制剂和表面活性剂的颗粒混合物,以及(b)左旋多巴乙酯或其衍生物或其药学上可接受的盐;以及封装内部核心的外层,用于立即释放,包括以下混合物:去羧化酶抑制剂和左旋多巴乙酯或其衍生物或其药学上可接受的盐的颗粒混合物.本发明还涵盖了通过给予本发明的药物组合物治疗帕金森病或相关疾病的患者的方法.此外,本发明还提供了制造本发明药片的方法.

    海关参考信息

    专利信息


    专利号:US-2004110228-A1
    优先权日:2002-04-01
    标 题:Combinatorial organic synthesis of unique biologically active compounds
    发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
    摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-5401844-A
    优先权日:1983-04-11
    标 题 :Regulation of enzymes which utilize tetrahydrobiopterin or tetrahydrofolate cofactors with 6,6-disubstituted-tetrahydropteridines
    发明人:AYLING JUNE E; BAILEY STEVEN W
    权利人:UNIV SOUTH ALABAMA
    摘要:6-[2'-Amino-2',2'-disubstituted-ethylamino]-pyrimidines of the structure: ##STR1## in which X=H, NH 2 or NO 2 , which are novel intermediates in the synthesis of quinoid 6,6-disubstituted-dihydro- and 6,6-disubstituted-tetrahydro-pteridines, are claimed.

    专利号:US-8697888-B2
    优先权日:2012-01-06
    标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:US-7799829-B2
    优先权日:2006-07-28
    标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
    发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

    专利号:WO-2005102340-A1
    优先权日:2003-05-30
    标题 :Piperazine melanocortin-specific compounds
    发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
    权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
    摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
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    主要参考文献


    1: Polonini HC, Silva SL, Cunha CN, Brandão MA, Ferreira AO. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions. Pharmazie. 2016 Apr;71(4):185-91.
    6: Bayes M, Rabasseda X, Prous JR. Gateways to Clinical Trials. June 2002. Methods Find Exp Clin Pharmacol. 2002 Jun;24(5):291-327. Review.

    合成参考文献


    摘要:Toxicology and Applied Pharmacology., 29(181), 1974 []
    参考文献:10.1016/j.bmc.2011.01.046
    摘要:Lohse B, Kristensen JL, Kristensen LH, Agger K, Helin K, Gajhede M, Clausen RP. Inhibitors of histone demethylases. Bioorg Med Chem. 2011 Jun 15;19(12):3625–36. doi: 10.1016/j.bmc.2011.01.046.
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