CAS: 6452-71-7; 1-(2-Allyloxyphenoxy)-2-Hydroxy-3-Isopropylaminopropane

该化合物是一种非选择性的乙型肾上腺激素对抗物,通常用于治疗高血压和某些心脏状况,其作用是阻止乙型肾上腺素等乙型肾上腺素在乙型肾上腺受体上作用,导致心率和血压下降.化学特征是其结构,包括一个苯丙醇氢氧基和一种丙烯胺,有助于其药用活动.Oxprenolol表现出适度的亲脂性,允许其有效跨过生物膜.它通常通过口服,其半衰期较短,需要全天多剂量才能产生持续治疗效果.该物质还可能表现出某种内在的同感性活动,这可能导致与其他乙型阻塞剂相比,心脏病的发病率下降得不太明显.与许多药物一样,潜在的副作用包括疲劳,眩晕和胃肠扰动,在具有呼吸道状况的病人中应谨慎使用,因为其非选择性的心血管疾病管理具有重要的选择.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

3-(o-Allyloxyphenoxy)-2-hydroxy-1-chlorpropan isopropylamine BA 42154 allyl bromide2-(2-allyloxyphenoxy)acetic acid -1,2-propanediol3--1,2-propanediol 1-[2-(allyloxy)phenoxy]-3-(isopropylamino)propan-2-ol (-)-Oxprenolol

合成工艺路线路线简述

    📜[2-(Oxiran-2-Ylmethoxy)Phenyl] 4-Methylbenzenesulfonate 反应生成 氧烯洛尔
    参考文献:Yamada,Jositsugu
    标题:Yamada,Jositsugu

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    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-2003050305-A1
    优先权日:2000-05-22
    标题:Thromboxane inhibitors, compositions and methods of use
    发明人:TEJADA INIGO SAENZ DE
    摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

    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-6436997-B1
    优先权日:1998-06-01
    标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension
    发明人:DE TEJADA INIGO SAENZ
    权利人:NITROMED INC
    摘要:The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides methods of promoting vasorelaxation and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, at least one vasoactive agent and/or thromboxane A2 receptor antagonist. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions resulting from an abnormally high level of arginase activity, such as, heart disease, systemic hypertension, pulmonary hypertension, sexual dysfunction, autoimmune disease, chronic renal failure and cerebral vasospasm. The present invention also provides methods for treating clinical conditions associated with a deficient nitric oxide pathway by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Azizi K, Koli MG. Molecular dynamics simulations of Oxprenolol and Propranolol in a DPPC lipid bilayer. J Mol Graph Model. 2016 Mar;64:153-64. doi: 10.1016/j.jmgm.2016.01.009. Epub 2016 Jan 28. doi: 10.1016/j.ejpb.2014.03.013. Epub 2014 Mar 28. German. Hungarian.
    20: Fraeyman NF, Dello CD, Belpaire FM. Alpha 1-acid glycoprotein concentration and molecular heterogeneity: relationship to oxprenolol binding in serum from healthy volunteers and patients with lung carcinoma or cirrhosis. Br J Clin Pharmacol. 1988 Jun;25(6):733-40.

    合成参考文献


    摘要:Polish Journal of Pharmacology and Pharmacy., 25(145), 1973
    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    摘要:HANSCH,C ET AL. (1995)
    参考文献:10.1007/bf00297587
    摘要:Montagna M, Groppi A. Fatal sotalol poisoning. Arch Toxicol. 1980 Jan;43(3):221–6. doi: 10.1007/bf00297587.
    参考文献:10.1007/bf00561670
    摘要:Svendsen TL, Rasmussen S, Hartling OJ, Nielsen PE, Trap-Jensen J. Acute and long-term effects of labetalol on systemic and pulmonary haemodynamics in hypertensive patients. European Journal of Clinical Pharmacology. 1980 Jan;17(1):5–11. doi: 10.1007/bf00561670.
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