CAS: 59-98-3; 2-Benzyl-4,5-Dihydro-1H-Imidazole

该化合物是一种具有血管性能的线性衍生物,主要作为有竞争力的α-肾上腺受体对立物,在α1和α2受体中表现出选择性的对抗,导致周边血管变异和血压降低.托拉索林在扭转由对流性化学剂引起的血管抑制方面特别有效,使其在管理诸如新生儿肺部高血压等条件方面很有价值.其药理学特征包括轻微的类似甲胺和胆碱性影响,有助于其血管特性.该化合物的结构特征是一无脊髓状腺环,它强化了受体约束的亲和性.托拉索林的快速作用和可逆效应使其适合于需要精确的热动动力调节的急性临床情景.它通常通过静脉注射进行,因为其有利的药理学.

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ECHA物质C&L通报REACH预注册

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CAS号107-15-3 乙二胺 | CAS号645-54-5 2-苯基硫代乙酰胺 | CAS号140-29-4 苯乙腈 | CAS号103-82-2 苯乙酸 | CAS号122-78-1 2-苯基乙醛 | CAS号1011736-08-5 N-nitroso-2-ben... | CAS号7218-04-4 2-乙酰胺-3-氨基丙酸 | CAS号5467-51-6 (5Z)-5-(1H-indo... | CAS号7436-90-0 (2,2-二溴乙烯基)苯 | CAS号5442-34-2 Benzeneethanimi... | CAS号65248-65-9 2-benzyl-1-meth... | CAS号63226-76-6 N-(2-acetamidoe... | CAS号122-78-1 2-苯基乙醛

合成工艺路线路线简述

    📜N-(Cyanomethyl)-2-Phenylacetamide置于镍,异丙醇体系中,125.0 °C,12.75 Mpa 条件下,反应生成 2-苯甲基咪唑啉
    参考文献:De830954
    标题:De830954

    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: Casbeer HC, Knych HK. Pharmacokinetics and pharmacodynamic effects of tolazoline following intravenous administration to horses. Vet J. 2013 Jun;196(3):504-9. doi: 10.1016/j.tvjl.2012.12.006. Epub 2013 Jan 12. doi: 10.2460/ajvr.74.3.395. doi: 10.1016/j.saa.2011.05.041. Epub 2011 May 23. doi: 10.1002/ccd.21811. doi: 10.1111/j.1467-2995.2007.00375.x. Epub 2008 Feb 18.
    19: Wilms G, Stockx L, Baert AL. Optimization of distal artery opacification in peripheral arteriography: comparison between nitroglycerin, tolazoline and buflomedyl. J Belge Radiol. 1993 Oct;76(5):311-3.

    合成参考文献


    参考文献:10.1111/j.1651-2227.1980.tb07038.x
    摘要:Hegyi T, Hiatt IM. Tolazoline and dopamine therapy in neonatal hypoxia and pulmonary vasospasm. Acta Paediatr Scand. 1980 Jan;69(1):101–3. doi: 10.1111/j.1651-2227.1980.tb07038.x.
    摘要:J. Elguero, E. Gonzalez, J.L. Imbach and R. Jacquier. Bull. Soc. Chim. France 1969, 4075.
    参考文献:10.1111/j.1651-2227.1980.tb07105.x
    摘要:Markestad T, Finne PH. Effect of tolazoline in pulmonary hemorrhage in the newborn. Acta Paediatr Scand. 1980 May;69(3):425–6. doi: 10.1111/j.1651-2227.1980.tb07105.x.
    参考文献:10.1001/archsurg.1980.01380050028007
    摘要:Williams RA, Wilson SE. Effect of intra-arterial vasodilators on blood flow in ischemic dog colon. Arch Surg. 1980 May;115(5):602–5. doi: 10.1001/archsurg.1980.01380050028007.
    参考文献:10.1007/bf01728335
    摘要:Muller W, Kachel W, Lasch P, Varnholt V, Konig SA. Inhaled nitric oxide for avoidance of extracorporeal membrane oxygenation in the treatment of severe persistent pulmonary hypertension of the newborn. Intensive Care Med. 1996 Jan;22(1):71–6. doi: 10.1007/bf01728335.
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