2-[二甲基(2-甲基-2-丙基)甲硅烷基]-N,N-二甲基-1H-咪唑-1-磺酰胺置于四丁基氟化铵体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.5H,反应生成 N,N-二甲基咪唑-1-磺酰胺 参考文献:Ngochindo,Raphael I.,Journal Of The Chemical Society. Perkin Transactions I,1990,# 6,P. 1645-1648 标题:Ngochindo,Raphael I.,Journal Of The Chemical Society. Perkin Transactions I,1990,# 6,P. 1645-1648
专利号:US-5359051-A 优先权日:1990-01-11 标题 :Compounds useful in the synthesis of nucleic acids capable of cleaning RNA 发明人:COOK PHILLIP D; GUINOSSO CHARLES J; BRUICE THOMAS 权利人:ISIS PHARMACEUTICALS INC 摘要:Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. In preferred embodiments, the reactive portions comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with and without intervening intercalating moieties and act through phosphorodiester hydrolytic bond cleavage. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided which are useful for elaboration of oligonucleotides for such purposes.
专利号:US-2009118512-A1 优先权日:2006-03-31 标 题:Process for Preparing 6,7-Dihydro-5H-Imidazo[1,5-A]Pyridin-8-One 发明人:MARTIN PIERRE; BOUDIER ANDREAS; QUIRMBACH MICHAEL; MAH ROBERT; JOTTERAND NATHALIE 权利人:MARTIN PIERRE; BOUDIER ANDREAS; QUIRMBACH MICHAEL; MAH ROBERT; JOTTERAND NATHALIE 摘要:6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5-a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.
专利号:WO-9506037-A1 优先权日:1993-08-27 标题 :New imidazole derivatives having agonistic or antagonistic activity on the histamine h3 receptor 发明人:VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK 权利人:VRIJE UNIVERSITEIT; VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK 摘要:The invention relates to new imidazole derivatives of formula (I) having agonistic and antagonistic activity on the histamine H3-receptor. More in particular the invention concerns 4- and 5-substituted aminoalkyl imidazoles and their derivatives. The invention further relates to the synthesis of these compounds, pharmaceutical compositions comprising the said compounds or pharmacological salts thereof, and the use of the compounds as agents having biological activity on the histamine H3-receptor or for the preparation of a pharmaceutical composition.
专利号:CN-104507928-A 优先权日:2012-07-03 标 题:Heterocyclic regulators of lipid synthesis
专利号:KR-20160100329-A 优先权日:2013-12-20 标题 :Heterocyclic modulators of lipid synthesis and combinations thereof
专利号:CN-106061963-A 优先权日:2013-12-20 标题 :Heterocyclic modulators of lipid synthesis and combinations thereof
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2004). 摘要:Gribble, G. W., Science of Synthesis, (2006) 8, 381. 摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 492. 摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 474. 摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 480.