CAS: 143228-85-7; (S)-Azelastine

该化合物是一种主要被确认为用于抗口炎的手性化合物,特别是在治疗过敏鼻膜炎和结膜炎方面,它属于被称为phthalazinones的化合物类别,其特点是能够有选择地对丙胺H1受体产生对抗,从而减轻过敏症状.(S) ----阿拉斯丁的分子结构具有phthalazine核心的分子结构,有助于其药理特性.它表现出相对较高的亲眼性,允许通过生物膜有效渗透,有利于其治疗效果.此外,(S) ----阿拉斯丁有很长的动作时间,适合在临床环境中一次使用.该化合物通常以鼻涕喷喷剂或眼滴的形式管理,提供局部的缓解,并产生最小的系统性副作用.其安全性特征一般是有利的,尽管一些病人可能经历轻微的副作用,如潜伏性或局部的刺激性,从而具有完全的定向的动作.(S)

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MSDS等安全信息

    上下游产品

    4-[(4-chlorophenyl)methyl]-1(2H)-phthalazinone 2-(2-chloroethyl)-1-methylpyrrolidine hydr°Chloride 2‐(4-chlorophenylacetyl)benzoic acid 2-Benzoyl-1-(hexahydro-1-methyl-1H-azepin-4-yl)hydrazin-hydr°Chlorid azelastine hydr°Chloride

    合成工艺路线路线简述

      📜氮卓斯汀置于mixed Selector Chiral Stationary Phase Prepared With Co-Immobilized Human Serum Albumin And Cellulase On A Poly(Glycidylmethacrylate-Co-Ethylene Glycol Dimethacrylate) Monolith体系中,用 Aq. Phosphate Buffer,异丙醇 用作溶剂,化学反应生成(R)-氮卓斯汀,2-呋喃羧酸,四氢-5-羟基-,甲基酯,(2S-顺)-(9Ci)
      参考文献:毛细管电色谱中基于蛋白质的混合选择剂手性整体固定相†
      标题:毛细管电色谱中基于蛋白质的混合选择剂手性整体固定相†
      摘要:用共固定的人血清白蛋白和纤维素酶在聚(甲基丙烯酸缩水甘油酯-共-乙二醇二甲基丙烯酸酯)(聚(gma-Co-Edma))整体材料及其在手性分离研究中的实用性评价进行了介绍.为了进行比较,还用相应的蛋白质制备了两个单选择手性固定相(csp).通过毛细管电色谱法(cec)与各种外消旋物一起研究了这些csp的对映体分离能力.混合选择器csp的对映选择性比单个选择器大,并且可以分离10种手性分析物,而两个单个选择器csp分别分辨3和8.此外,对于(+/-)-华法林,对映体拆分度在混合选择剂csp上得到了改善.同时,与单一选择器csp相比,在同时固定不同蛋白质时不需要额外的制备阶段或试剂消耗,从经济和实践的角度来看,这是更有利的.因此,通过将hsa和纤维素酶混合在一起,复合柱将两种蛋白质的对映选择性结合在一起,从而在实践上扩大了它们的应用范围.
      Doi:10.1039/c8Nj02309C

      海关参考信息

      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-5760221-A
      优先权日:1993-12-18
      标 题:Method for the preparation of hexahydroazepinones and hexahydroazepinoles
      发明人:OLBRICH ALFRED; ENGEL JUERGEN; KUTSCHER BERNHARD; MOELLER ROLAND
      权利人:ASTA MEDICA AG
      摘要:This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.

      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-2023075715-A1
      优先权日:2021-10-26
      标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids)
      发明人:OYTUN FARUK; CAN EFE
      权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI
      摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.

      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.

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Karpishchenko SA, Kolesnikova OM. [The effectiveness of the combination of azelastine hydrochloride and mometasone furoate for the intranasal application in the patients presenting with seasonal allergic rhinitis]. Vestn Otorinolaringol. 2017;82(5):44-47. doi: 10.17116/otorino201782544-47. Russian. doi: 10.1007/s00405-016-4295-8. Epub 2016 Sep 13. doi: 10.1017/S0022215115002959. Epub 2015 Oct 30.

      合成参考文献


      参考文献:10.2165/00063030-200115070-00004
      摘要:Galant SP, Wilkinson R. Clinical prescribing of allergic rhinitis medication in the preschool and young school-age child: what are the options BioDrugs. 2001;15(7):453–63. doi: 10.2165/00063030-200115070-00004.
      参考文献:10.1002/jps.10091
      摘要:Nakajima M, Tane K, Nakamura S, Shimada N, Yamazaki H, Yokoi T. Evaluation of Approach to Predict the Contribution of Multiple Cytochrome P450s in Drug Metabolism Using Relative Activity Factor: Effects of the Differences in Expression Levels of NADPH–Cytochrome P450 Reductase and Cytochrome b5 in the Expression System and the Differences in the Marker Activities. Journal of Pharmaceutical Sciences. 2002 Apr;91(4):952–63. doi: 10.1002/jps.10091.
      参考文献:10.1097/00004424-200205000-00002
      摘要:Schöber W, Wiskirchen J, Kehlbach R, Gebert R, Rodegerdts E, Betsch A, Johst U, Feuls R, Claussen CD, Duda SD. Antiproliferative effects of the antiallergic agent azelastine on human aortic smooth-muscle cells: an in vitro study. Invest Radiol. 2002 May;37(5):248–53. doi: 10.1097/00004424-200205000-00002.
      参考文献:10.1016/j.jaad.2003.11.048|10.1016/s0190-9622(03)04516-x
      摘要:Lew B, Haw C, Lee M. Cutaneous drug eruption from cetirizine and hydroxyzine. Journal of the American Academy of Dermatology. 2004 Jun;50(6):953–6. doi: 10.1016/j.jaad.2003.11.048.
      参考文献:10.1097/01.moo.0000122310.13359.79
      摘要:Lal D, Corey JP. Vasomotor rhinitis update. Current Opinion in Otolaryngology & Head and Neck Surgery. 2004 Jun;12(3):243–7. doi: 10.1097/01.moo.0000122310.13359.79.
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