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.
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