专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
专利号:US-8153615-B2 优先权日:2005-06-10 标 题:Synthesis of glycerolipid carbamates and dicarbamates and their use as an antitumor compounds 发明人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 权利人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 摘要:The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.
专利号:US-9867899-B2 优先权日:2010-05-24 标题 :Reinforced adhesive complex coacervates and methods of making and using thereof 发明人:STEWART RUSSELL J 权利人:UNIV UTAH RES FOUND 摘要:Described herein is the synthesis of reinforced adhesive complex coacervates and their use thereof. The reinforced adhesive complex coacervates are composed of (a) at least one polycation, (b) at least one polyanion, and (c) a reinforcing component. The adhesive complex coacervates described herein can be subsequently cured to produce strong, cohesive adhesives. The reinforced adhesive complex coacervates have several desirable features when compared to conventional adhesives. The reinforced adhesive complex coacervates are effective in wet or underwater applications. The reinforced adhesive complex coacervates described herein, being phase separated from water, can be applied underwater without dissolving or dispersing into the water. The reinforced adhesive complex coacervates have numerous biological applications as bioadhesives and bioactive delivery devices. In particular, the reinforced adhesive complex coacervates described herein are particularly useful in underwater applications and situations where water is present such as, for example, wet tissues in physiological conditions.
专利号:EP-1414822-B1 优先权日:2001-06-26 标题:Improved synthesis of branched acyclic nucleosides 发明人:JANSEN GERT 权利人:MEDIVIR AB 摘要:A method for the preparation of acyclic nucleosides such as valomaciclovir stearate comprising the acid hydrolysis of an intermediate of the formula II: where X is a leaving group or an optionally protected guanine moiety, R1 is a hydroxy protecting group or a -C(=O)C1-C22 alkyl ester group; R2 and R3 are independently lower alkyl or benzyl, or R2 and R3 taken together are -CH2CH2- or -CH2CH2CH2- or -CH2CH2CH2CH2-; to the corresponding aldehyde of the formula III: and the reduction of the aldehyde to the corresponding alcohol of the formula IV: by the addition of a borohydride or borane aldehyde reducing agent, characterised in that the borohydride or borane aldehyde reducing agent is introduced under acid conditions.
专利号:US-2014220082-A1 优先权日:2011-06-28 标 题:Adhesive complex coacervates and methods of making and using thereof 发明人:STEWART RUSSELL J 权利人:STEWART RUSSELL J; UNIV UTAH RES FOUND 摘要:Described herein is the synthesis of adhesive complex coacervates and their use thereof. The adhesive complex coacervates are produced by reacting (a) at least one poly anion comprising a plurality of activated ester groups, and (b) at least one polycation comprising a plurality of nucleophilic groups, wherein the nucleophilic groups react with the activated ester groups to produce a new oovalent bond between the polycation and the polyanion. The adhesive complex coacervates described herein have low interfacial tension with water and wettable substrates. When applied to a wet substrate they spread over the interface rather than beading up. The adhesive complex coacervates have numerous biological applications as bioadhesives and drug delivery devices. In particular, the adhesive complex coacervates described herein are particularly useful in wet or underwater applications and situations where water is present such as, for example, physiological conditions.
专利号:WO-9713503-A1 优先权日:1995-10-13 标 题:Synthesis of drug nanoparticles by spray drying 发明人:SELVARAJ ULAGARAJ; MESSING GARY L 权利人:PENN STATE RES FOUND; SELVARAJ ULAGARAJ; MESSING GARY L 摘要:The present invention relates to a method for synthesizing nanoparticles comprising combining an agent and a matrix to form a composite mixture, and spray drying the composite mixture, wherein the nanoparticles are less than about 5000 nm. Suitable agents that can be formulated into nanoparticle in the context of the present invention include therapeutic and diagnostic agents, cosmetic, dye, photographic, food, pesticide agents, among others.
[参考文献]: Elisabetta Bertol, Et Al. Fatty Acid Ethyl Esters In Hair: Correlation With Self-Reported Ethanol Intake In 160 Subjects And Influence Of Estroprogestin Therapy. Drug Test Anal. 2014 Sep;6(9):930-5. [参考文献]: Enbo Xu, Et Al. Characterization Of Volatile Flavor Compounds In Chinese Rice Wine Fermented From Enzymatic Extruded Rice. J Food Sci. 2015 Jul;80(7):C1476-89. [参考文献]: Friedrich Martin Wurst, Et Al. Concentration Of Fatty Acid Ethyl Esters In Hair Of Alcoholics: Comparison To Other Biological State Markers And Self Reported-Ethanol Intake. Alcohol Alcohol. 2004 Jan-Feb;39(1):33-8. [参考文献]: J P Verhave, Et Al. The Dual Role Of Macrophages In The Sporozoite-Induced Malaria Infection. A Hypothesis. Int J Nucl Med Biol. 1980;7(2):149-56. [参考文献]: Julia Klein, Et Al. Neonatal Hair Analysis As A Biomarker For In Utero Alcohol Exposure. N Engl J Med. 2002 Dec 19;347(25):2086.
合成参考文献
摘要:Witt, D., Science of Synthesis Knowledge Updates, (2011) 3, 306. 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 参考文献:10.1016/s0379-0738(01)00456-x 摘要:Pragst F, Auwaerter V, Sporkert F, Spiegel K. Analysis of fatty acid ethyl esters in hair as possible markers of chronically elevated alcohol consumption by headspace solid-phase microextraction (HS-SPME) and gas chromatography-mass spectrometry (GC-MS). Forensic Sci Int. 2001 Sep 15;121(1-2):76–88. doi: 10.1016/s0379-0738(01)00456-x. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 2004. Toxicity, Repellency of Phytotoxicity of 979 Chemicals to Birds, Mammals and Plants. Research Report No. 04-01. National Wildlife Research Center, Fort Collins, Colorado. 118 pp. 摘要:de Figueiredo, R. M., Science of Synthesis: Knowledge Updates, (2024) 2, 271.