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-5021550-A 优先权日:1986-10-07 标 题 :Method for preventing deletion sequences in solid phase synthesis 发明人:ZEIGER ALLEN R 权利人:UNIV JEFFERSON 摘要:Improved methods for solid-state synthesis of polymers, especially polypeptides and polynucleotides, are provided. In accordance with a preferred embodiment, selectively activatable and reactive bonding moieties are covalently bonded to solid supports for polynucleotide and polypeptide syntheses. Products of failed reactions and some side products are caused to react with the selectively activatable and reactive bonding moiety to cause divalent bonding of unwanted products to the solid support. Upon cleavage of the initial situs of covalent bonding to the solid support, desired products are free to be collected while unwanted products remain covalently bonded to the support. Ease of purification of such polymers is a principal object of the present invention. The methods of the invention are amenable to automation and digital control and novel solid supports, activatable, reactive bonding moieties and other compositions are presented. The expression of polynucleotides prepared in accordance with preferred embodiments produces novel polypeptides.
专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:WO-9411388-A1 优先权日:1992-11-06 标题:Support for the synthesis of modular polymers
专利号:US-5310894-A 优先权日:1990-09-11 标题 :Solid phase polynucleotide syntheses 发明人:ZEIGER ALLEN R 权利人:UNIV JEFFERSON 摘要:Methods for solid-state synthesis of polymers, especially polypeptides and polynucleotides, are provided. In accordance with a preferred embodiment, selectively activatable and reactive bonding moieties are covalently bonded to solid supports for polynucleotide and polypeptide syntheses. Products of failed reactions and some side products are caused to react with the selectively activatable and reactive bonding moiety to cause divalent bonding of unwanted products to the solid support. Upon cleavage of the initial situs of covalent bonding to the solid support, desired products are free to be collected while unwanted products remain covalently bonded to the support. Ease of purification of such polymers is a principal object of the present invention. The methods of the invention are amenable to automation and digital control and novel solid supports, activatable, reactive bonding moieties and other compositions are presented. The expression of polynucleotides prepared in accordance with preferred embodiments produces novel polypeptides.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.