专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide 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 nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
专利号:US-5852198-A 优先权日:1996-04-03 标题 :Wittig reagents and method for preparing α,β-unsaturated phosphonates 发明人:XU YIBO; FLAVIN MICHAEL T; XU ZE-QI 权利人:MEDICHEM RES INC 摘要:Wittig-type reagents and methods of preparation and use thereof for preparing alpha , beta -unsaturated phosphonate esters from aldehydes and ketones are disclosed. The Wittig-type reagents have the following formulae: I II wherein X represents triflate, halide, BF4, SbF6, or ClO4; R1 represents alkyl, aryl or arylalkyl; and R2 represents alkyl, aryl or arylalkyl, provided that R1 and R2 not represent phenyl at the same time. The Wittig reagent diethyl phosphono-methylidenetriphenylphosphorane (1b) has been successfully synthesized for the first time via its phosphonium triflate salt (4a), by treating diethyl phosphonomethyltriflate with triphenylphosphine according to the disclosed method. The procedure has been applied to the synthesis of other new Wittig-type reagents such as phosphoranes and phosphonium salts. The new Wittig reagents thus synthesized were treated with various aldehydes and an activated ketone, affording the corresponding alpha , beta -unsaturated phosphonates, saturated phosphonates or phosphoric acids. Triphenylphosphorane 1b and triphenylphosphonium 4a led to both cis and trans isomers with the latter being predominant, while trans isomers were almost exclusively formed when tributyl reagents (1c and 4d) were used.
专利号:US-6320040-B1 优先权日:1990-07-27 标题:4-desmethyl nucleoside analogs and oligomers thereof 发明人:COOK PHILLIP DAN; TENG KELLY 权利人:ISIS PHARMACEUTICALS INC 摘要:Tetrahydrofuranyl compounds are provided that are functionalized to include pendant conjugate groups, and which are useful in diagnosis assays and as research reagents. Novel intermediates for the synthesis of the compounds are also provided.
专利号:US-4536355-A 优先权日:1982-10-08 标题 :Phenoxyphenylaminoalkylphosphinates useful in weed control 发明人:LEE SHY-FUH; HENRICK CLIVE A 权利人:ZOECON CORP 摘要:Novel phenoxyphenoxyalkyl-, phenoxyphenylthioalkyl- or phenoxyphenylsulfonylalkyl-substituted phosphinates and phosphonates, related compounds, synthesis thereof, intermediates therefor, and the use of said novel compounds for the control of weeds.
专利号:US-4456464-A 优先权日:1982-05-19 标题 :Phenoxy- and pyridyloxy-phenoxyalkyl phosphinates and related sulfur compounds for weed control 发明人:LEE SHY-FUH; HENRICK CLIVE A 权利人:ZOECON CORP 摘要:Novel phenoxyphenoxyalkyl-, phenoxyphenylthioalkyl- or phenoxyphenylsulfonylalkyl-substituted phosphinates and phosphonates, related compounds, synthesis thereof, intermediates therefor, and the use of said novel compounds for the control of weeds.