2-甲基喹啉置于sodium Carbonate Decahydrate,Sodium Carbonate,氯,盐酸体系中,用 水 用作溶剂,化学反应 3.0H,以267.8 G的收率获得2-氯甲基喹啉盐酸盐 参考文献:The Process Development Of Rg 12525 (2-{[4-(Tetrazol-5-Ylmethylphenyl)-Methoxy]Phenoxymethyl}Quinoline) 标题:The Process Development Of Rg 12525 (2-{[4-(Tetrazol-5-Ylmethylphenyl)-Methoxy]Phenoxymethyl}Quinoline) 摘要:This Contribution Describes Process Improvements To Provide A Practical And Cost Effective Synthesis For The Manufacture Of Rg 12525 Which Resulted In A 3-Fold Increase In Overall Yield. Improved Solvent Systems For Chlorination And Azidation Reactions Are Described. Adjustments To The Tetrazole-Forming Step Eliminated Azide Sublimation And Minimised This Risk On Scaleup. A Robust Solvent System Was Found To Control The Polymorphic Form During Crystallisation,Which Had Hitherto Been Difficult Due To The Near-Equivalence Of Melting Points (154 And 157 Degreesc) Of The Two Known Forms. Doi:10.1021/op0000677
专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:US-9040553-B2 优先权日:2010-09-17 标题:Phenoxyisobutyric acid compounds and method of synthesis 发明人:LALEZARI IRAJ; FABRICANT JILL 权利人:LALEZARI IRAJ; FABRICANT JILL; CELL VIABLE CORP 摘要:The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
专利号:US-6166031-A 优先权日:1987-10-19 标 题:Substituted tetralins, chromans and related compounds in the treatment of asthma 发明人:EGGLER JAMES F; MARFAT ANTHONY; MELVIN JR LAWRENCE S 权利人:PFIZER 摘要:Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals; pharmaceutical compositions comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
专利号:US-11976052-B2 优先权日:2019-01-11 标题:Leukotriene synthesis inhibitors 发明人:BURGOYNE DAVID L; DEBRUIN ERIN; FONAREV JULIA; YEE JAMES GEE KEN; LANGLANDS JOHN MICHAEL 权利人:NAEGIS PHARMACEUTICALS INC 摘要:Provided are specific leukotriene synthesis inhibitor compounds and pharmaceutical compositions comprising the compounds and methods of using the compounds and the pharmaceutical compositions in treating, for example, inflammatory diseases or conditions.
专利号:US-10111854-B2 优先权日:2014-02-26 标题 :Synthesis and use of amine-containing flavonoids as potent anti-leishmanial agents 发明人:CHOW LARRY MING-CHEUNG; Chan Tak Hang William; CHAN KIN-FAI; WONG IRIS LAI KING; KAN WING-YIU 权利人:UNIV HONG KONG POLYTECHNIC 摘要:The present invention relates to novel series of amine-containing flavonoids and compositions containing the compounds, as well as the synthesis and the use of the same. The invention also relates to methods of treatment and prevention of diseases, in particular, parasitic infections including Leishmaniasis, comprising administration of the compounds.
专利号:US-8378099-B2 优先权日:1994-10-28 标 题:Boronic ester and acid compounds, synthesis and uses 发明人:ADAMS JULIAN; MA YU-TING; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 权利人:MILLENNIUM PHARMACUETICALS INC; ADAMS JULIAN; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 摘要:Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.