CAS: 82586-52-5; (3S)-2-[(2S)-2-[[(2S)-1-Ethoxy-1-Oxo-4-Phenylbutan-2-Yl]Amino]Propanoyl]-6,7-Dimethoxy-3,4-Dihydro-1H-Isoquinoline-3-Carboxylic Acid,Hydrochloride

该化合物是一种主要用于治疗高血压的抗酶抑制剂(ACE),是一种主要用于治疗高血压的抗酶激素抑制剂,是一种在身体中转化成活性形态的抗药剂,莫exiprilat,它通过阻止将血管I转化为血管II,导致血管变异和血压降低,从而产生药理效应.甲基盐酸甲酯的化学配方包括一种复杂的结构,其成分是有利于其功效和特性的分泌衍生物.它一般是口服的,以相对长的半衰期为人所知,允许一次剂量.常见副作用包括头晕,咳嗽和高钾含量等.与其他ACE抑制剂一样,它被与以前的ACE抑制剂疗法有关的有血管肿史的病人所侵入,应当谨慎地用于肾脏损伤的个人.

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CAS号82586-51-4 [3S-[2[R*(R*)]]... | CAS号103775-14-0 莫昔普利拉 | CAS号103733-51-3 莫西普利二酮哌嗪

合成工艺路线路线简述

    [3S-[2[r*(R*)]],3R*]-2-[2-[[1-(Ethoxycarbonyl)-3-Phenylpropyl]Amino]-1-Oxopropyl]-1,2,3,4-Tetrahydro-6,7-Dimethoxy-3-Isoquinolinecarboxylic Acid,Phenylmethyl Ester,Hydrochloride置于palladium On Activated Charcoal 氢气体系中,用 四氢呋喃 作为反应溶剂,以88%的收率获得产物盐酸莫昔普利
    参考文献:新型血管紧张素转化酶抑制剂奎纳普利及其相关化合物的合成.非巯基和巯基类型的结构活性关系存在差异.
    标题:新型血管紧张素转化酶抑制剂奎纳普利及其相关化合物的合成.非巯基和巯基类型的结构活性关系存在差异.
    摘要:据报道奎纳普利(ci-906,22),其活性二酸(ci-928,33)和其二甲氧基类似物(ci-925,25)的合成和血管紧张素转化酶(ace)抑制活性.这些四氢-3-异喹啉羧酸衍生物具有与依那普利相当的体外效能和体内功效.具有相同结构变化的巯基类似物也非常有效.相反,四氢-1-异喹啉羧酸和同源异吲哚啉-1-羧酸类似物在两种类型的效力上显示出惊人的差异,巯基类似物基本上是无活性的,而非巯基类似物与脯氨酸原型是等效的.这是第一个证据表明小分子ace抑制剂的两个主要结构类别可能存在其他结合模式.
    DOI:10.1021/jm00160A026

    海关参考信息

    专利信息


    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-9757463-B2
    优先权日:2012-06-15
    标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
    发明人:HARTH EVA M; BEEZER DAIN B; LI GUANGZHAO; SPEARS BENJAMIN R; STEVENS DAVID M
    权利人:UNIV VANDERBILT
    摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. 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-9745419-B2
    优先权日:2014-01-24
    标 题 :Aqueous polyglycidol synthesis with ultra-low branching
    发明人:HARTH EVA M; SPEARS BENJAMIN R
    权利人:UNIV VANDERBILT
    摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for a variety of applications, including, but not limited to, drug delivery. 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:WO-2024097977-A1
    优先权日:2022-11-04
    标题:Silk nanoparticle synthesis: tuning size, dispersity, and surface chemistry for drug delivery
    发明人:SHAIDANI SAWNAZ; FALCUCCI THOMAS; FOSTER OLIVIA; SAHOO JUGAL KISHORE; HASTURK ONUR; KAPLAN DAVID L; JACOBUS CHARLOTTE S
    权利人:TUFTS COLLEGE
    摘要:Methods disclosed herein relate to generating silk nanoparticles with a low polydispersity index (PDI). Methods include adding a silk solution dropwise into a volatile solvent that is miscible with water, thereby forming a precipitate-bearing solution and applying shear forces to the precipitate-bearing solution for a length of time sufficient to achieve evaporation of at least 95% of the volatile solvent, thereby producing a population of silk fibroin nanoparticles in water having a polydispersity index (PDI) of 0.35 or less, including but not limited to, a PDI of 0.330 or less, 0.325 or less, 0.315 or less, 0.310 or less, 0.30 or less, 0.275 or less, 0.250 or less, 0.225 or less, or 0.200 or less. Parameters related to silk fibroin molecular weight, silk fibroin concentration, shear force application, and temperature may all be modified to achieve silk nanoparticles of a particular size exhibiting particular PDIs.

    专利号:US-2016206743-A1
    优先权日:2012-06-15
    标题 :Linear Polyester and Semi-Linear Glycidol Polymer Systems: Formulation and Synthesis of Novel Monomers and Macromolecular Structures

    专利号:US-2014005278-A1
    优先权日:2012-06-15
    标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures
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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Moexipril. 2024 Nov 15. 2012–. Moexipril. 2018 Feb 11. 31(11). doi: 10.1002/bmc.4004. Epub 2017 Jun 7. 69(9):648-54.
    133:300-6. doi: 10.1016/j.saa.2014.05.061. Epub 2014 Jun 5. 85(9):1297-305. doi: 10.1016/j.bcp.2013.02.026. Epub 2013 Mar 5.
    7: Stanisz B, Regulska K, Ratajczak T. First order derivative spectrophotometric and HPLC methods for determination of moexipril hydrochloride in the pure form, pharmeceutical formulations and evaluation of its stability. Acta Pol Pharm. 2012 May-Jun;69(3):389-95. 26(12):1552-8. doi: 10.1002/bmc.2731. Epub 2012 Mar 14. 81(1-2):25-9. doi: 10.1016/j.talanta.2009.11.031. Epub 2009 Nov 13. 55(2):476-83. doi: 10.1007/s10620-009-0744-1. Epub 2009 Mar 3. 47(8):44-8. Russian. 3(1):23-30.

    合成参考文献


    参考文献:10.1007/s10557-011-6316-6
    摘要:Opie LH. Inhibition of the cerebral renin-angiotensin system to limit cognitive decline in elderly hypertensive persons. Cardiovasc Drugs Ther. 2011 Aug;25(4):277–9. doi: 10.1007/s10557-011-6316-6.
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