CAS: 80012-43-7; 9,13B-Dihydro-1H-Dibenzo[c,F]Imidazo[1,5-A]Azepin-3-Amine

该化合物是一种主要用于治疗过敏结膜炎和其他过敏反应的抗脊髓灰质炎,具有选择性的H1受体抗体对抗性,有效阻塞过敏反应的化合物 ----丙胺 ----一种反应过敏的化合物;乙胺的特征是能够缓解诸如痒痒,红度和与过敏有关的肿胀等症状;该物质通常以眼滴的形式施用,允许最小系统吸收的局部治疗;其化学结构包括一个管状环,有助于其药性特性;乙胺呈现一种有利的安全性特征,其常见副作用是温和短暂的;此外,人们注意到其双重作用是抗口炎和血管稳定剂,有助于防止释放丁胺和其他炎症.

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CAS号127786-29-2 依匹斯汀氢溴酸盐 | CAS号127785-96-0 6-氨甲基-6,11-二氢-5... | CAS号108929-04-0 盐酸依匹斯汀

合成工艺路线路线简述

  • 41218-84-2 = 80012-43-7
    反应条件:1.1 Solvents: Methanol; 14 - 16 H,Rt1.2 Reagents: Sodium Hydroxide Solvents: Tert-Butyl Methyl Ether,Water; Ph 10 - 11
    标题:Synthesis Technology Of Epinastine Hydrochloride
    作者:Guo,Jian-Feng; Zhang,Cai-Xia; Wang,Yan-Li; Sun,Xin-Hui; Guo,Zhen-Hua
    参考文献:Xiandai Yaowu Yu Linchuang 日期:2011 卷标:26(5) 页码:378-380]

    41218-84-2 = 80012-43-7 [标题:Reaction Conditions
    标题:A Modular Approach To Dibenzo-Fused ε-Lactams: Palladium-Catalyzed Bridging-C-H Activation
    作者:Yu,Yinghua; Ma,Liyao; Xia,Jiajin; Xin,Luoting; Zhu,Lei; Et Al
    参考文献:Angewandte Chemie 日期:2020 卷标:59(41) 页码:18261-18266]

    41218-84-2 = 80012-43-7 [标题:Reaction Conditions
    标题:Process For Preparation Of 3-Amino-9,13B-Dihydro-1H-Dibenz[c,F]Imidazo[1,5-A]Azepine Hydrochloride
    参考文献:European Patent Organization
6-(邻苯二甲酰亚胺基甲基)-6,11-二氢-5H-二苯并-[b,E]氮杂卓置于一水合肼体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应 8.0H,反应生成 依匹斯汀
参考文献:一种盐酸依匹斯汀杂质b的合成方法
标题:一种盐酸依匹斯汀杂质b的合成方法
摘要:本发明涉及医药技术领域,尤其涉及一种盐酸依匹斯汀杂质的制备方法.本发明首先以6‑(邻苯二甲酰亚胺基甲基)‑6,11‑二氢‑5H‑二苯并‑[b,E]氮杂为起始原料,用水合肼脱去保护基,再与溴化氰关环得到3‑氨基‑9,13‑二氢‑1H‑二苯并[c,F]‑咪唑并[1,5‑a]氮杂(依匹斯汀),最后与溴单质反应制得盐酸依匹斯汀杂质b.本发明盐酸依匹斯汀杂质b的合成方法,工艺路线简单,操作方便,选择性好,收率高;合成的盐酸依匹斯汀杂质b可作为盐酸依匹斯汀的有关物质检测用对照品,用于盐酸依匹斯汀及其相关制剂的质量控制的应用,控制盐酸依匹斯汀原料药或者其制剂的纯度.

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-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

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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主要参考文献


1: Gumieniczek A, Berecka-Rycerz A, Hubicka U, Żmudzki P, Lejwoda K, Kozyra P. Photodegradation of the H1 Antihistaminic Topical Drugs Emedastine, Epinastine, and Ketotifen and ROS Tests for Estimations of Their Potent Phototoxicity. Pharmaceutics. 2020 Jun 17;12(6):560. doi: 10.3390/pharmaceutics12060560.
2: Jha M, Moshirfar M. Epinastine. 2020 Jun 5. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2020 Jan–. 34(9):e4848. doi: 10.1002/bmc.4848. Epub 2020 Jun 25. 2006–. Epinastine. 2020 Jan 20. 25(1):209. doi: 10.3390/molecules25010209.
6: Iwasa C, Zaima K, Metori K, Harikai N, Tanaka Y, Hamada J, Shinomiya K, Hayashi H. Transfer of epinastine to infants through human breast milk. Pharmazie. 2019 Dec 1;74(12):732-736. doi: 10.1691/ph.2019.9105. 14(1):e0210362. doi: 10.1371/journal.pone.0210362.

合成参考文献


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
参考文献:10.1055/s-0031-1296961
摘要:Shioya T, Satake M, Kagaya M, Sano MA, Watanabe A, Fukui S, Sasaki M. Antitussive effects of the H1-receptor antagonist epinastine in patients with atopic cough (eosinophilic bronchitis). Arzneimittelforschung. 2004;54(4):207–12. doi: 10.1055/s-0031-1296961.
参考文献:10.1385/comp:32:1:43
摘要:Roy H. The red eye. Compr Ther. 2006;32(1):43–6. doi: 10.1385/comp:32:1:43.
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