专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-7432031-B2 优先权日:2005-03-22 标 题:Toner for electrostatic charge developing, production method thereof, developer for electrostatic charge developing using the same, and image forming method 发明人:MIZUTANI NORIYUKI; MAEHATA HIDEO; HAMANO HIROKAZU; TANAKA HIROYUKI; KITAGAWA SOICHIRO; IGUCHI MOEGI 权利人:FUJI XEROX CO LTD 摘要:A toner for electrostatic charge developing prepared by a production method including aggregating one or more kind of particles in a raw material dispersion including the particles to form aggregated particles, and coalescing the aggregated particles by heating. At least one kind of the particles is resin particles including an amorphous polyester resin synthesized by copolymerizing one or more polyvalent carboxylic acids and two or more polyhydric alcohols; at least one of the polyvalent carboxylic acids is polyvalent carboxylic acid having a sulfonic acid group; two of the polyhydric alcohols are an ethylene oxide adduct of bisphenol A and a propylene oxide adduct of bisphenol A; and the following equation is satisfied:n n10/90≦ BPA ( EO )/ BPA ( PO )≦90/10.n n In the equation, BPA(EO) represents a total mole amount of the ethylene oxide adduct of bisphenol A used in synthesis of the amorphous polyester resin, and BPA(PO) represents a total mole amount of the propylene oxide adduct of bisphenol A used in synthesis of the amorphous polyester resin.
专利号:US-2001024798-A1 优先权日:1998-06-11 标题:Biomimetic combinatorial synthesis 发明人:SHAIR MATTHEW D; LINDSLEY CRAIG W; PELISH HENRY E; SHEEHAN SCOTT M; GOESS BRIAN C; LAYTON MARK E; CHAN LAWRENCE K; CHEN CHUO; WESTWOOD NICHOLAS J 摘要:The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can then be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo [n. 3.1 ] ring systems, medium ring systems, and fused ring systems. In addition to compounds, libraries and methods for their production, the present invention also provides pharmaceutical compositions and methods and kits for determining one or more biological activities of the library members.
专利号:US-4810390-A 优先权日:1986-10-10 标 题:Separation and purification of pigment suspensions and suspensions of pigment intermediates by a membrane separation process 发明人:FLIERL KLAUS; PFENNINGER HEINZ; MARFURT HANS-RUDOLF 权利人:CIBA GEIGY CORP 摘要:Process for separation and purifying pigment suspensions and suspensions of pigment intermediates in a liquid by means of a membrane separation process, whereby the suspension to be treated is uniformly fed to and circulated through a microfiltration unit containing at least one semi-permeable membrane and the separated liquid flows off through the membrane as permeate which process comprises replacing the permeate gradually by a washing liquid that differs from the first liquid such that the total amount of washing liquid fed into the system is 1 to 15 times the total volume of the initial suspension, and separating the resultant suspension from the liquid by means of conventional filtration or drying apparatus. The process is particularly suitable for processing fine pigment suspensions often obtained in pigment synthesis.
专利号:CN-111715289-B 优先权日:2020-05-09 标题:A method and application of in-situ synthesis of FeOOH/Fe3O4/cellulose composite material
专利号:WO-2024097977-A1 优先权日:2022-11-04 标题:Silk nanoparticle synthesis: tuning size, dispersity, and surface chemistry for drug delivery 发明人:SHAIDANI SAWNAZ; FALCUCCI THOMAS; FOSTER OLIVIA; SAHOO JUGAL KISHORE; HASTURK ONUR; KAPLAN DAVID L; JACOBUS CHARLOTTE S 权利人:TUFTS COLLEGE 摘要:Methods disclosed herein relate to generating silk nanoparticles with a low polydispersity index (PDI). Methods include adding a silk solution dropwise into a volatile solvent that is miscible with water, thereby forming a precipitate-bearing solution and applying shear forces to the precipitate-bearing solution for a length of time sufficient to achieve evaporation of at least 95% of the volatile solvent, thereby producing a population of silk fibroin nanoparticles in water having a polydispersity index (PDI) of 0.35 or less, including but not limited to, a PDI of 0.330 or less, 0.325 or less, 0.315 or less, 0.310 or less, 0.30 or less, 0.275 or less, 0.250 or less, 0.225 or less, or 0.200 or less. Parameters related to silk fibroin molecular weight, silk fibroin concentration, shear force application, and temperature may all be modified to achieve silk nanoparticles of a particular size exhibiting particular PDIs.
摘要:Gosselin, R.E., H.C. Hodge, R.P. Smith, and M.N. Gleason. Clinical Toxicology of Commercial Products. 4th ed. Baltimore: Williams and Wilkins, 1976., p. VI-184 摘要:IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans. Geneva: World Health Organization, International Agency for Research on Cancer, 1972-PRESENT. (Multivolume work).