CAS: 108612-45-9; 2-((1-(1-(4-Fluorobenzyl)-1H-Benzo[d]Imidazol-2-yl)Piperidin-4-yl)(Methyl)Amino)Pyrimidin-4(1H)-One

该化合物是一种抗脊髓灰质炎药物,主要用于治疗鼻炎和泌尿病等过敏症,它作为H1类甲胺受体的选择性敌,有效减轻与过敏反应有关的症状.Mizolastine的特点是其相对长的半衰期,允许一次剂量,这可以提高病人的耐药性.与第一代抗脊髓灰质炎相比,该化合物的镇静剂潜力较低,适合需要避免下垂的人.化学上,Mizolastine被归类为管状衍生物,拥有独特的结构,有助于其药用特性.它通常是口服的,在胃肠道中非常有吸收力.该物质还因其抗炎作用而得到注意,这在管理过敏反应方面可能带来额外的治疗好处.与任何药物一样,潜在的副作用可能包括头痛,口干口和胃肠扰动,尽管这些作用一般是轻微的.

结构式图片

上下游产品

1-{1-(4-氟苯基)甲基-1H-苯咪唑-2-基}-N-甲基-4-哌啶胺 1-{1-[(4-Fluorophenyl)Methyl]-1H-Benzimidazol-2-Yl}-N-Methyl-4-Piperidinamine 108635-83-2
1-(4-氟苄基)-2-氯苯并咪唑 2-Chloro-1-(4-Fluorobenzyl)-1H-Benzimidazole 84946-20-3

合成工艺路线路线简述

    2-({1-[1-(4-Fluorobenzyl)-1H-Benzimidazol-2-Yl]-Piperidin-4-Yl}-Aminomethyl)-4-Benzyloxypyrimidine置于氢溴酸,Sodium Hydroxide体系中,用 甲醇,溶剂黄146 用作溶剂,化学反应 12.0H,反应生成咪唑斯汀
    参考文献:Process And Intermediates For Obtaining 1-(1H-Benzimidazol-2-yl)-4-(Pyrimidin-2-Ylamino)Piperidine Derivatives
    标题:Process And Intermediates For Obtaining 1-(1H-Benzimidazol-2-yl)-4-(Pyrimidin-2-Ylamino)Piperidine Derivatives

    专利信息


    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-7919505-B2
    优先权日:2006-07-11
    标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
    发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

    专利号:US-2011003780-A1
    优先权日:2007-07-10
    标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
    发明人:ZHU MAN
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

    专利号:WO-2023096715-A9
    优先权日:2021-10-22
    标 题:Immunomodulatory glycosphingolipids and methods of use thereof
    发明人:KASPER DENNIS; OH SUNGWHAN
    权利人:HARVARD COLLEGE
    摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.

    专利号:US-8697730-B2
    优先权日:2007-10-26
    标题 :5-lipoxygenase activating protein (FLAP) inhibitor
    发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON
    权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC
    摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

    专利号:US-2022125838-A1
    优先权日:2019-02-11
    标题 :Immunomodulatory glycosphingolipids and methods of use thereof
    发明人:OH SUNGWHAN; KASPER DENNIS L; SONG HEEBUM; PARK SEUNG BUM
    权利人:HARVARD COLLEGE; SEOUL NAT UNIV R&DB FOUNDATION
    摘要:Provided herein are a subset of alpha-galactosylceramide (alpha-GC) compounds having improved immunomodulatory activity, particularly with respect to NKT cell number and activity. Also provided herein are methods of use of such compounds, including in the modulation of NKT cells and/or activity in vivo. Further provided are combinatorial synthesis methods for generating alpha-GC compounds of specifically defined structure and thereby generating pure preparations thereof.
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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: Molimard M, Diquet B, Benedetti MS. Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Fundam Clin Pharmacol. 2004 Aug;18(4):399-411. Review. doi: 10.1016/j.biopha.2017.06.008. Epub 2017 Jun 13. Review. Review. Review. doi: 10.3109/02652048.2014.995727. Epub 2014 Dec 24.
    13: Triggiani M, Giannattasio G, Balestrieri B, Granata F, Gelb MH, de Paulis A, Marone G. Differential modulation of mediator release from human basophils and mast cells by mizolastine. Clin Exp Allergy. 2004 Feb;34(2):241-9. doi: 10.1002/14651858.CD006137.pub2. Review.

    合成参考文献


    摘要:United States Patent Document., #4820710
    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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