On November 28, 1990, Young, Robert N.; Gauthier, Jacques Yves; Zamboni, Robert; Belley, Michel L. published a patent.Recommanded Product: Isochroman-3-ol The title of the patent was Preparation of diarylstyrylquinoline diacids as leukotriene antagonists. And the patent contained the following:
Title compounds I [R1 = 7-Cl, 7-MeO, 6-F3C, 7-F3C, 6-MeSO2, H, 6,7-Cl2; Y = CH:CH, CH2CH2, CH2O, CHMeCH2; A = HO2C(CH2)2S, Me2NCO(CH2)2S, 3-(HO2C)C6H4S, Me3CNHCO(CH2)2S, 4-carboxy-2-pyridyl, [(1-adamantylamino)carbonylethyl]thio, 1-tetrazol-5-ylmethylthio, etc.; B = 2-(HO2C)C6H4CH2CH2, 3-(HO2C)C6H4, 5-carboxy-2-thiophenyl, HO2CCH2CHMe(CH2)2, 6-carboxy-2-pyridyl, 2-(Me3CNHCO)C6H4S, 3-[(1-tetrazol-5-yl)methyl]phenyl, etc.] and their salts, useful as inhibitors of leukotriene biosynthesis, antiasthmatic, antiallergic, antiinflammatory, and cytoprotective agents (no data, assays described), are prepared I may also be used to treat erosive gastritis, inflammatory bowel disease, prevention of SRA-release (no data). To a suspension of [(7-chloroquinolin-2-yl)methyl]triphenylphosphonium bromide in THF was added BuLi, the reaction mixture was stirred at -78° and Me 2-[3-[2-(methoxycarbonyl)ethylthio]-3-(3-formylphenyl)propyl]benzoate [preparation from 3-(BrCH2)C6H4CN given] added, the mixture warmed to room temperature to give I [R1 = 7-Cl; Y = CH:CH; A = HO2C(CH2)2S; B = 2-(HO2C)C6H4CH2CH2] (II) as the di-Me ester, which in THF and MeOH was saponified to give II.2Na salt. A capsule, injectable suspension and tablet formulations comprising I are given. Pharmaceutical composition of I may comprise an addnl. active ingredient such as nonsteroidal antiinflammatory drug, peripheral analgesic, cyclooxygenase inhibitor, etc. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Recommanded Product: Isochroman-3-ol
The Article related to arylstyrylquinoline diacid preparation leukotriene antagonist, cytoprotection arylstyrylquinoline diacid, eye antiinflammatory arylstyrylquinoline diacid, antiasthmatic arylstyrylquinoline diacid, srsa inhibitor arylstyrylquinoline diacid preparation and other aspects.Recommanded Product: Isochroman-3-ol
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