CAS: 53267-01-9; Cibenzoline

该化合物是主要用于管理心血管和子脑心律不齐的一种I级抗心律激素,其行动机制包括钠信道阻塞,延长心脏行动潜力,稳定心肌细胞膜.该化合物表现出中度的亲脂性,确保有效的组织渗透和持续的药理活动.主要优势包括其可预测的药理动能,半衰期适合每日两次服用,以及临床使用中具有精细化性的安全特征.Cibenzoline还展示了更多的钾通道阻塞效应,有助于其在骨折性心律不齐方面的效力.其化学稳定性和与标准配方前的兼容性使得它适合口服制板生产.

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CAS号28098-84-2 1-cyano-2,2-dip... | CAS号107-15-3 乙二胺 | CAS号85589-36-2 2-(2,2-diphenyl...

合成工艺路线路线简述

    📜西苯唑啉琥珀酸盐置于sodium Hydroxide体系中,化学反应 0.5H,以30 G的收率获得产物西苯唑啉
    参考文献: Novel Process For The Preparation Of (+)-Cibenzoline Succinate[fr] Nouveau Procédé De Préparation De Succinate (+)-Cibenzoline
    标题: Novel Process For The Preparation Of (+)-Cibenzoline Succinate[fr] Nouveau Procédé De Préparation De Succinate (+)-Cibenzoline
    摘要:本发明涉及(+)-Cibenzoline琥珀酸盐的晶体形态.本发明还涉及一种制备手性纯度大于99.9%的(+)-Cibenzoline琥珀酸盐的方法.本发明还提供了一种制备(+)-Cibenzoline琥珀酸盐及其晶体形态的方法.

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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-5426196-A
    优先权日:1993-12-22
    标题 :Synthesis of diaryl methanes
    发明人：FANG FRANCIS G
    权利人:GLAXO INC
    摘要:The present Invention includes synthetic steps and intermediates involved in the following reaction scheme a of converting compounds of Formula (II) to the diarylmethanes of Formula (I): ##STR1## wherein: Y is oxygen or sulfur; n A, B, C, D, and E are carbon or 1, 2 or 3 of A, B, C, D, and E are independently nitrogen, and the others are carbon; and n wherein n R 1 through R 10 are selected independently from the group consisting of: hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhalo-alkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, heteroaryl, or aryl or heteroaryl, mono, di, or tri substituted with one or more hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhaloalkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, or heteroaryl groups and; n the pharmaceutically acceptable salts and solvates thereof.

    专利号:US-10814013-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-2008107598-A1
    优先权日:2006-10-05
    标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications

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    主要参考文献


    1: Harron DW, Brogden RN, Faulds D, Fitton A. Cibenzoline. A review of its pharmacological properties and therapeutic potential in arrhythmias. Drugs. 1992 May;43(5):734-59. doi: 10.2165/00003495-199243050-00008. 21(1 Pt 1):38-40. doi: 10.1177/10600280870211p104. 7(6):537-9. doi: 10.1016/j.eupc.2005.06.013.

    合成参考文献


    参考文献:10.2165/00002018-199615020-00005
    摘要:Chan JC, Cockram CS, Critchley JA. Drug-induced disorders of glucose metabolism. Mechanisms and management. Drug Saf. 1996 Aug;15(2):135–57. doi: 10.2165/00002018-199615020-00005.
    参考文献:10.1046/j.1540-8167.2004.03402.x
    摘要:Shan Z, Van Der Voort PH, Blaauw Y, Duytschaever M, Allessie MA. Fractionation of electrograms and linking of activation during pharmacologic cardioversion of persistent atrial fibrillation in the goat. J Cardiovasc Electrophysiol. 2004 May;15(5):572–80. doi: 10.1046/j.1540-8167.2004.03402.x.
    参考文献:10.1007/s00380-003-0750-8
    摘要:Hiramatsu M, Wu LM, Hirano Y, Kawano S, Furukawa T, Hiraoka M. Block of HERG current expressed in HEK293 cells by the Na+-channel blocker cibenzoline. Heart Vessels. 2004 May;19(3):137–43. doi: 10.1007/s00380-003-0750-8.
    参考文献:10.1080/15563650701458134
    摘要:Meeus R, Verpooten GA, De Paep R, Paelinck BP, Neels H, Cooreman S, De Doncker M, Jorens PG. Cibenzoline intoxication: effect of combined hemoperfusion-hemodialysis on plasma clearance. Clin Toxicol (Phila). 2008 Apr;46(4):303–6. doi: 10.1080/15563650701458134.
    参考文献:10.1007/bf00241092
    摘要:Sato T, Wu B, Kiyosue T, Arita M. Effects of cibenzoline, a new class Ia antiarrhythmic drug, on various membrane ionic currents and action potentials of guinea-pig ventricular cells. Naunyn Schmiedebergs Arch Pharmacol. 1994 Aug;350(2):167–73. doi: 10.1007/bf00241092.
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