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-2023097824-A1 优先权日:2020-05-08 标 题:Semi-synthesis and use of racemic hematoxylin 发明人:DURRANT EDWARD E; HEINDL DIETER; HUBER FLORIAN MAURITIUS ERASUMU; KLEIN ERIC; KOSMEDER II JEROME W; VOSS EDGAR 权利人:VENTANA MED SYST INC; ROCHE DIAGNOSTICS OPERATIONS INC 摘要:A racemic hematoxylin formulation is disclosed that includes one or both of a stabilizer compound and an antioxidant. The disclosed composition exhibits sufficient stability to be utilized in an automated staining process. Methods of using and making the stabilized composition also are disclosed.
专利号:US-10772990-B2 优先权日:2014-04-01 标题 :Tissue filler compositions and methods of use 发明人:NIKOLIS ANDREAS; HERBERT LISE 权利人:KLOX TECH INC 摘要:The present disclosure relates to methods for stimulating collagen synthesis, cosmetic enhancement of soft tissue and/or inhibiting or treating scarring comprising administering a composition to an area to be treated within a soft tissue, wherein the composition comprises a tissue filler medium and a fluorophore; and illuminating the area with light having a wavelength which can be absorbed by the fluorophore.
专利号:US-2003186237-A1 优先权日:2001-02-14 标题:Methods and compositions of amplifying RNA 发明人:GINSBERG STEPHEN D; CHE SHAOLI 权利人:BAYLOR COLLEGE MEDICINE 摘要:The present invention pertains to a method that will increase the efficiency of second strand cDNA synthesis through a mechanism of “terminal continuationâ€? before further RNA amplification by RNA transcription using, for example, a bacteriophage promoter. In a specific embodiment, a transcription promoter is attached to the 5′ region of cDNA through the same mechanism of “terminal continuationâ€?. Genetic signals are subsequently amplified in a linear manner through RNA transcription. In specific embodiments, the orientation of the transcribed RNA is either sense or antisense, depending on the desired downstream application. In other embodiments, the present invention pertains to methods for extraction and amplification of RNA, particularly mRNA, from histologically stained tissues and cells.
专利号:WO-2021224361-A2 优先权日:2020-05-08 标题 :Semi-synthesis and use of racemic hematoxylin
专利号:CN-115612114-A 优先权日:2021-07-14 标 题:Method and application of copolymer film and its enzymatic self-assembly synthesis
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