苯磺酰肼置于ammonium Chloride体系中,用 4-溴肉桂酸,N,N-二甲基甲酰胺 用作溶剂,以3.66 G (73%)的收率获得3-(4-溴苯基)丙酸 参考文献:Inhibitors Of Histone Deacetylase 标题:Inhibitors Of Histone Deacetylase 摘要:这项发明涉及抑制组蛋白去乙酰化酶.该发明提供了抑制组蛋白去乙酰化酶酶活性的化合物和方法.该发明还提供了治疗细胞增殖性疾病和病况的组合物和方法.
专利号:US-9751851-B2 优先权日:2013-09-20 标 题:Molecules and compositions that inhibit gram negative bacteria and their uses 发明人:BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; CONRAD-MILLER LAURA C; O'LOUGHLIN COLLEEN T 权利人:UNIV PRINCETON; BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; MILLER LAURA C; O'LOUGHLIN COLLEEN T 摘要:Antivirulence strategies to combat Pseudomonas aeruginosa , are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.
专利号:US-2009099367-A1 优先权日:2006-03-06 标题 :Process for preparing a leukotriene antagonist 发明人:BESSA BELLMUNT JORDI; RAFECAS JANE LLORENC; PASTO AGUILA MIREIA; VERDAGUER ESPAULELLA XAVIER; GORDO CAMPON ESTHER 权利人:FARMAPROJECTS S A 摘要:Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation.
专利号:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
专利号:US-12304894-B2 优先权日:2019-04-17 标题 :Derivatives of adamantyl oxadiazoles and pharmaceutically acceptable solvates, hydrates and salts thereof, pharmaceutical composition comprising same, synthesis method, suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1) 发明人:FARDELLA BELLO CARLOS ENRIQUE; LAGOS ARÉVALO CARLOS FERNANDO; VECCHIOLA CÃ?RDENAS ANDREA PAOLA; ALLENDE SANZANA FIDEL ALEJANDRO; DIETHELM VARELA BENJAMIN MANUEL; RECABARREN GAJARDO GONZALO IVAN; GONZÃ?LEZ CISTERNA PABLO MARCELO 权利人:UNIV PONTIFICIA CATOLICA CHILE 摘要:The present invention relates to compounds derived from adamantyl oxadiazoles and the pharmaceutically acceptable solvates, hydrates and salts of same. These compounds are suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1), as well as in the production of a drug for treating conditions and diseases such as high blood pressure, obesity, dyslipidaemia, type 2 diabetes, insulin resistance, glaucoma, metabolic syndrome, cognitive disorders, osteoporosis, immune disorders, depression and other conditions. Also provided is a pharmaceutical composition comprising the compounds and a method for preparing said composition.
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries
专利号:US-4992574-A 优先权日:1987-11-06 标题:Benzocycloheptene derivatives 发明人:KLAUS MICHAEL; MOHR PETER 权利人:HOFFMANN LA ROCHE 摘要:A compound of the formula ##STR1## wherein R 1 is hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino; n R 2 is hydrogen, alkyl, akoxy or halogen; n R 3 , R 4 , R 5 , R 6 , R 11 and R 12 independently are hydrogen or lower-alkyl; n R 3 and R 5 taken together are methylene or hydroxymethylene; n R 7 , R 8 , R 9 and R 10 independently are hydrogen or lower-alkyl; n R 11 and R 12 taken together are oxo or spiro-cyclo-lower alkyl; or R 11 is hydrogen and R 12 is hydroxy or acetoxy; and one of the residues R 13 and R 14 is hydrogen and the other is lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I, which can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis, are described. The compounds of the invention can be prepared by the synthesis of the C(R 13 )â•?C(R 14 ) double bond according to Wittig from a corresponding bicyclic component and a corresponding monocyclic component and optional subsequent transformation of functional grous.