CAS: 26844-12-2; N-[1-[2-(1H-Indol-3-yl)Ethyl]Piperidin-4-Yl]Benzamide

该化合物是一种化学化合物,主要被确认为用作抗血压剂,属于被称为阿尔法-1肾上腺对抗剂的化合物,其作用是阻止甲型-甲型-肾上腺受体的无肾上腺素作用,导致血管通缩,并随后降低血压;Indoramin的分子结构包括一个管状环,有助于其药理特性;它通常以口服形式进行,并研究其对心血管健康的影响;Indoramin展示中度的亲脂性,影响体内的吸收和分布;此外,它具有相对较长的半衰期,允许在临床环境中每天一次服用;虽然它有效管理高血压,但潜在的副作用可能包括眩晕,疲劳和胃肠扰动;与任何药物一样,在开开用Indoramin药时必须考虑个别病人因素和潜在的药物相互作用.

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CAS号26844-47-3 N-[1-[2-(1H-ind...

合成工艺路线路线简述

    📜4-Benzamido-1-[2-(3-Indolyl)Ethyl]-Pyridinium Bromide置于sodium Borohydrid体系中,用 仲丁醇 用作溶剂,化学反应生成吲哚拉明
    参考文献:Process For Preparing 3-[(Benzamidopiperid-1-yl)Alkyl] Indoles
    标题:Process For Preparing 3-[(Benzamidopiperid-1-yl)Alkyl] Indoles
    摘要:本发明提供了一种制备吲哚的新工艺,其中使用特殊溶剂将4-酰胺基-1-[3-吲哚基-亚烯基]吡啶化合物或相应的四氢吡啶化合物还原为相应的哌啶化合物.

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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-6469065-B1
    优先权日:1996-02-02
    标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
    发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

    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-RE41998-E
    优先权日:1990-02-26
    标题 :Compositions and methods of treatment of sympathetically maintained pain
    发明人:CAMPBELL JAMES N
    权利人:ARCLON THERAPEUTICS INC
    摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

    专利号:US-9556123-B2
    优先权日:2004-07-19
    标题:Synthesis of triethylenetetramines
    发明人:JONAS MARCO; VAULONT IRENE; SOI ANTONIO; SCHMIDT GUNTHER
    权利人:PHILERA NEW ZEALAND LTD
    摘要:Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

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    主要参考文献


    1: Nelson RL, Thomas K, Morgan J, Jones A. Non surgical therapy for anal fissure. Cochrane Database Syst Rev. 2012 Feb 15;(2):CD003431. doi: 10.1002/14651858.CD003431.pub3. Review. Review. Review. Erratum in: Drugs 1986 Oct;32(4):preceding 291. Review. doi: 10.3389/fphys.2016.00320. eCollection 2016. Review.
    9: Bennett JM, Weich DJ, Schoeman HS. Double-blind study comparing indoramin and propranolol in the treatment of black patients with hypertension. S Afr Med J. 1988 Dec 17;74(12):619-21.
    12: Pierce V, Shepperson NB, Todd MH, Waterfall JF. Investigation into the cardioregulatory properties of the alpha 1-adrenoceptor blocker indoramin. Br J Pharmacol. 1986 Feb;87(2):433-41.

    合成参考文献


    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    参考文献:10.1023/a:1007739421023
    摘要:Usui K, Tanabe T, Handa S, Shinozaki Y, Mori H. Disproportional response between refractory period and blood flow to alpha 1- and beta-adrenoceptor blockade in canine ischemic myocardium. Cardiovasc Drugs Ther. 1998 Dec;12(6):561–71. doi: 10.1023/a:1007739421023.
    参考文献:10.1007/bf03239966|10.1016/j.gassur.2006.01.006
    摘要:MacLean A. Chemical Sphincterotomy in the Treatment of Anal Fissure. Journal of Gastrointestinal Surgery. 2006 May;10(5):629–30. doi: 10.1016/j.gassur.2006.01.006.
    参考文献:10.2515/therapie/2012075
    摘要:Villa AF, Hong HT, Lee HM, Chataigner D, Garnier R. [Not Available]. Therapie. 2012 Nov;67(6):523–7. doi: 10.2515/therapie/2012075.
    参考文献:10.2165/00003088-199223020-00005
    摘要:Murray M. P450 enzymes. Inhibition mechanisms, genetic regulation and effects of liver disease. Clin Pharmacokinet. 1992 Aug;23(2):132–46. doi: 10.2165/00003088-199223020-00005.
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