CAS: 100427-26-7; 3-(1-((3,3-Diphenylpropyl)(Methyl)Amino)-2-Methylpropan-2-yl) 5-Methyl 2,6-Dimethyl-4-(3-Nitrophenyl)-1,4-Dihydropyridine-3,5-Dicarboxylate

该化合物是一种主要用于治疗高血压的钙管阻塞器,它属于二氢正丙烯类的钙对抗者,通过抑制钙离子流入血管滑动肌肉和心血管细胞,导致血管变异和减少血压,Lercanidipine的特点是其亲脂性,这增加了其吸收能力,允许一次剂量.该物质有相对较长的半衰期,有助于其持续的抗血压效应.它通常以盐盐的形式进行施用,其药用皮肤科动物可能受到食物摄入的影响,建议将其用空腹来进行最佳吸收.常见的副作用可能包括周围的红肿,头痛和冲洗,尽管通常都具有良好的温度.Lercanidipine选择血管滑动肌肉来取代心脏组织,最大限度地减少对心脏速的有害影响,从而在管理高血压时,特别是病人的随身状况下,它更愿意选择.

结构式图片

欧盟法规

C&L通报

上下游产品

CAS号132866-11-6 盐酸乐卡地平 | CAS号28075-29-8 N-甲基-3,3-二苯基丙胺 | CAS号74936-72-4 乐卡地平母核 | CAS号100442-33-9 2,N-二甲基-N-(3,3-... | CAS号100427-51-8 1,1,N-trimethyl... | CAS号88712-56-5 1,4-dihydro-2,6... | CAS号100427-53-0 1,1,N-trimethyl... | CAS号21731-17-9 β-氨基巴豆酸甲酯 | CAS号210579-45-6 1-((3,3-dipheny... | CAS号132866-11-6 盐酸乐卡地平

合成工艺路线路线简述

    盐酸乐卡地平置于sodium Hydroxide体系中,用 甲醇,水 用作溶剂,化学反应生成乐卡地平
    参考文献:Solid Lercanidipine Free Base
    标题:Solid Lercanidipine Free Base
    摘要:本发明提供了基本纯度为至少95%,优选至少97%,更优选至少99%,还更优选至少99.5%的左旋卡尼地平游离基.本发明的左旋卡尼地平游离基以非晶态固体形式形成,易于处理,特别适用于制药组合物的制备.

    专利信息


    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-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

    专利号:US-7708989-B2
    优先权日:1999-10-29
    标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
    发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
    权利人:NITROMED INC
    摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

    专利号:EP-3967330-A1
    优先权日:2020-09-10
    标 题:Methods for the synthesis of bioactivated metal nanocluster and their medical application
    发明人:MARCHI VALÉRIE; CHIECHIO REGINA MARIA; EVEN-HERNANDEZ PASCALE
    权利人:UNIV RENNES; CENTRE NAT RECH SCIENT; INSTITUT NAT DES SCIENCES APPLIQUEES DE RENNES; ECOLE NAT SUPERIEURE DE CHIMIE DE RENNES
    摘要:The present invention relates to a bioactivated metal nanocluster comprising a mixture of ligands linked to a fluorescent metallic nanocluster, their synthesis methods, and their medical applications.

    专利号:US-2024368164-A1
    优先权日:2021-04-28
    标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof
    发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH
    权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH
    摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

    专利号:US-7384976-B2
    优先权日:2001-05-02
    标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC
    摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Tabidze GA, Gezeli TD, Tsibadze TA, Dolidze NM. [Clinical efficacy of calcium channel blockers slow the third generation of lercanidipine in the treatment of patients with arterial hypertension and metabolic disorders (review)]. Georgian Med News. 2015 Feb;(239):51-6. Review. Russian. Review. Russian. doi: 10.1185/03007995.2013.842891. Epub 2013 Sep 27. Review. Review. Russian. Review. Russian. Review. Russian. Review. Russian. doi: 10.5301/JN.2011.6271. Review. doi: 10.2165/11584470-000000000-00000. Review. Erratum in: Clin Drug Investig. 2011;31(8):572. doi: 10.1517/14656560903055087. Review. doi: 10.1517/17425250903085135. Review. Review. Review. Review. Review. doi: 10.1586/14779072.7.2.115. Review. Review.
    18: Pruijm MT, Maillard MP, Burnier M. Patient adherence and the choice of antihypertensive drugs: focus on lercanidipine. Vasc Health Risk Manag. 2008;4(6):1159-66. Review.
    19: Beckey C, Lundy A, Lutfi N. Lercanidipine in the treatment of hypertension. Ann Pharmacother. 2007 Mar;41(3):465-73. Epub 2007 Mar 6. Review. Review.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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