📜多索茶碱杂质01置于sodium Tetrahydroborate体系中,用 甲醇 作为反应溶剂,化学反应 2.0H,以60%的收率获得产物乙羟茶碱 参考文献:El Ashry,El Sayed H.; Rashed,Nagwa; Awad,Laila F.,Journal Of Chemical Research,Miniprint,2001,# 4,P. 440-450 标题:El Ashry,El Sayed H.; Rashed,Nagwa; Awad,Laila F.,Journal Of Chemical Research,Miniprint,2001,# 4,P. 440-450
专利信息
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, 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 pyruvate compound 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 pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-2004005342-A1 优先权日:2002-02-07 标题 :Topical administration of ascorbic acid to reinforce the cohesion of the dermo-epidermal junction 发明人:BERNERD FRANCOISE 权利人:OREAL 摘要:The present invention relates to the pharmaceutical or cosmetic use of a composition comprising, in a pharmaceutically or cosmetically acceptable medium, ascorbic acid or an analogue thereof to reinforce the cohesion of the dermo-epidermal junction. n The invention also relates to the pharmaceutical or cosmetic use of a composition comprising, in a pharmaceutically or cosmetically acceptable medium, ascorbic acid or an analogue thereof to increase the synthesis of tenascin and/or collagen VII. n The invention also relates to the use of ascorbic acid or of an analogue thereof to reinforce the cohesion of the dermo-epidermal junction of reconstructed skins.
专利号:US-5905091-A 优先权日:1996-07-03 标 题 :Enhancement of skin pigmentation by prostaglandins 发明人:FULLER BRYAN B 权利人:UNIV OKLAHOMA 摘要:A composition comprising a carrier and prostaglandin effective in stimulating synthesis of melanin in a human melanocyte thereby enhancing pigmentation of the human skin and optionally comprising a lysosomotropic agent, a phosphodiesterase inhibitor, and/or methylxanthines, and a method of use of the composition. Use of this composition promotes tanning of the human skin and increases photoprotection from ultraviolet radiation.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:US-2024208898-A1 优先权日:2021-03-25 标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents 发明人:KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T 权利人:DANA FARBER CANCER INST INC 摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.
1: Lücker PW, Wetzelsberger K, Erking W, Donike M. [Metabolism and pharmacokinetics of etofylline clofibrate, new antilipemic]. Arzneimittelforschung. 1980;30(11b):2045-53. German. Epub 2006 Nov 15. German. German. German. German.
合成参考文献
摘要:Arzneimittel-Forschung. Drug Research., 30(2023), 1980 [] 摘要:Arzneimittel-Forschung. Drug Research., 8(190), 1958 [] 摘要:Arzneimittel-Forschung. Drug Research., 4(649), 1954 [] 摘要:Merkus FW, Zuidema J. Theophylline and hydroxyethyltheophylline are different drugs. Int J Clin Pharmacol Ther Toxicol. 1980;18(2):97. 参考文献:10.1007/bf00449686 摘要:Kollöffel WJ, Driessen FGWHM, Goldhoorn PB. Rectal administration of paracetamol: a comparison of a solution and suppositories in adult volunteers. International Journal of Clinical Pharmacy. 1996 Jan;18(1):26–9. doi: 10.1007/bf00449686.