📜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
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.
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
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