1-[4-(1,1-Dimethylethyl)Phenyl]-4-[4-(Diphenylmethoxy)-1-Piperidinyl]-1-Butanone Phosphate置于potassium Hydroxide体系中,用 水,甲苯 作为反应溶剂,化学反应 2.17H,以91.13%的收率获得产物依巴斯汀 参考文献:Process For The Preparation Of 1-[4-(1,1-Dimethylethyl)Phenyl]-4-[4-(Diphenylmethoxy)-1-Piperidinyl]-1-Butanone And Acid Addition Salts Thereof 标题:Process For The Preparation Of 1-[4-(1,1-Dimethylethyl)Phenyl]-4-[4-(Diphenylmethoxy)-1-Piperidinyl]-1-Butanone And Acid Addition Salts Thereof 摘要:该发明描述了制备1-[4-(1,1-二甲基乙基)苯基]-4-[4-(二苯甲氧基)-1-哌啶基]-1-丁酮及其酸盐的过程.
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:US-2003124634-A1 优先权日:1996-04-30 标 题 :Novel proteins involved in the synthesis and assembly of O-antigen in pseudomonas aeruginosa 发明人:LAM JOSEPH S; BURROWS LORI L; CHARTER DEBORAH; KIEVIT TERESA DE 权利人:UNIV GUELPH 摘要:Novel nucleic acid molecules encoding proteins involved in the synthesis and assembly of O-antigen in P. aeruginosa ; and novel proteins encoded by the nucleic acid molecules are described. Methods are disclosed for detecting P.aeruginosa in a sample by determining the presence of the proteins or a nucleic acid molecule encoding the proteins in the sample.
专利号:WO-2024146022-A1 优先权日:2023-01-03 标题:Crystal form and amorphous form of carebastine p-toluenesulfonate 发明人:WANG XIAOYU; ZHANG LI; JIANG JIE; ZHOU NING; MOU XIA 权利人:CHENGDU SHIBEIKANG BIOMEDICAL TECH CO LTD 摘要:Provided are a crystal form and amorphous form of carebastine p-toluenesulfonate, and a preparation method therefor, relating to the field of medicinal chemistry, for use in solving the problems in the prior art that carebastine is unstable, not easy to scale up for synthesis, and difficult to make into a drug and the like. The crystal form and amorphous form of carebastine p-toluenesulfonate have the characteristics of high purity, high stability, high bioavailability, easy scale-up synthesis, and industrial production and the like, and have excellent hygroscopicity for easy storage.
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.
1: Jung HS, Park CH, Park YT, Bae MA, Lee YI, Kang BJ, Jegal Y, Ahn JJ, Lee T. Gynecomastia induced by H1-antihistamine (ebastine) in a patient with idiopathic anaphylaxis. Asia Pac Allergy. 2015 Jul;5(3):187-90. doi: 10.5415/apallergy.2015.5.3.187. Epub 2015 Jul 29. 2: Rapolu R, Pandey AK, Raju ChK, Ghosh K, Srinivas K, Awasthi A, Navalgund SG, Surendranath KV. A novel UV degradation product of Ebastine: isolation and characterization using Q-TOF, NMR, IR and computational chemistry. J Pharm Biomed Anal. 2015 Mar 25;107:488-94. doi: 10.1016/j.jpba.2015.01.039. Epub 2015 Jan 29. 5: Schmidt AH, Molnár I. Using an innovative Quality-by-Design approach for development of a stability indicating UHPLC method for ebastine in the API and pharmaceutical formulations. J Pharm Biomed Anal. 2013 May 5;78-79:65-74. doi: 10.1016/j.jpba.2013.01.032. Epub 2013 Jan 31. doi: 10.1093/chromsci/bms082. Epub 2012 Jun 7. doi: 10.4103/0019-5154.87168.
合成参考文献
摘要:Yakuri to Chiryo. Pharmacology and Therapeutics., 22(1143), 1994 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:10.1007/bf02221755 摘要:Scott DA, Fox JA, Cnaan A, Philip BK, Lind LJ, Palleiko MA, Stelling JM, Philip JH. Resistance to fluid flow in veins. Journal of Clinical Monitoring. 1996 Jul;12(4):331–7. doi: 10.1007/bf02221755.