专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:US-2010312013-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; YEE NATHAN K; SONG JINHUA J; REEVES JONATHAN T 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.
专利号:US-7244753-B2 优先权日:2002-07-29 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-9365494-B2 优先权日:2008-12-18 标 题 :Process for synthesis of amino-methyl tetralin derivatives 发明人:DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN 权利人:DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN; ROCHE PALO ALTO LLC 摘要:Methods for producing a compound of formula k1 or k2 n nby reducing a dihydronapthalene amide compound of formula in n nwith hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2n nRu(Z) 2 (L)  j1;n nRu(E)(E′)(L)(D)  j2;n nwherein m, n, Ar, Y, R 1 E, E′, D, Z and L are as defined herein.
专利号:US-6825185-B2 优先权日:2000-12-21 标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D 权利人:NITROMED INC 摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
参考标题:Synthesis And Biological Activity Of Substituted 2,4-Diaminopyrimidines That Inhibit Bacillus Anthracis 作者:Baskar Nammalwar,Richard A. Bunce,K. Darrell Berlin,Christina R. Bourne,Philip C. Bourne,Esther W. Barrow,William W. Barrow |发布日期:2012.8 摘要:The Lowest Mics With Values Of 0.5 μg/ml And 0.375-1.5 μg/ml, Respectively. It Is Likely That The S Isomers Of 1 Will Bind The Substrate-Binding Pocket Of Dihydrofolate Reductase (Dhfr) As In B. Anthracis Was Found For (S)-1A. The Final Step In The Convergent Synthesis Of Target Systems 1 From (+/-)-1-(1-Substituted-2(1H)-Phthalazinyl)-2-Propen-1-Ones 6 With 2,4-Diamino-5-(5-Iodo-3,4-Dimethoxybenzyl)Pyrimidine
合成参考文献
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