专利号:EP-2465936-A1 优先权日:2010-12-20 标题 :Enzymatic synthesis of statins and intermediates thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermdiate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or interemediate thereof.
专利号:US-8853132-B2 优先权日:2008-11-27 标题 :Directed synthesis of oligophosphoramidate stereoisomers 发明人:HEINDL DIETER; KESSLER DIRK; ROESLER ANGELIKA; SEIDEL CHRISTOPH; THUER WILMA 权利人:ROCHE DIAGNOSTICS OPERATIONS 摘要:The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.
专利号:US-2021369846-A1 优先权日:2018-10-26 标 题 :New Ammonium Salts Of Fluorinated Organic Acids, Method Of Their Synthesis and Application 发明人:STEFANEK AGATA; CIACH TOMASZ; LECZYCKAWILK KATARZYNA; CZARNOCKA-SNIADALA SYLWIA; GRAFSTEIN JOANNA; DRESLER MAGDALENA; NOWAK ALEKSANDRA; WGLINKSKI JAKUB 权利人:NANOSANGUIS 摘要:The exemplary arrangements relate to ammonium salts of partially fluorinated organic acids. The exemplary arrangements also relate to methods of synthesis of the ammonium salts of partially fluorinated organic acids. The exemplary arrangements also relate to methods of use of the ammonium salts of partially fluorinated organic acids to produce stabilizing emulsions of the oil-in-water and/or water-in-oil type. The exemplary arrangements also relate to methods of use and applications of the ammonium salts of partially fluorinated organic acids, for example use as stabilizing agents in blood substitute preparations.
专利号:US-2014370563-A1 优先权日:2011-08-26 标 题 :Compositions and methods for the relief of inhibition of aldehyde decarbonylase 发明人:SHANKLIN JOHN; ANDRE CARL 权利人:SHANKLIN JOHN; ANDRE CARL; BROOKHAVEN SCIENCE ASS LLC 摘要:The present invention is related to compositions and methods for enhanced synthesis of hydrocarbons, particularly, but not limited to, alkanes. The invention, in one embodiment, utilizes the co-expression of a hydrogen peroxide metabolizing enzyme in the presence of an aldehyde decarbonylase enzyme to relieve hydrogen peroxide inhibition of the aldehyde decarbonylase enzyme by hydrogen peroxide. In a preferred embodiment a catalase-aldehyde decarbonylase expression construct and fusion peptide is used. The present invention also relates to microorganisms engineered to express said enzymes and to produce hydrocarbon molecules.
专利号:US-8314132-B2 优先权日:2008-04-30 标题:5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone and the intermediates for production thereof 发明人:MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA 权利人:MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA; BIOTECHNOLOGIJOS INST 摘要:Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).
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.
参考文献:10.1186/1757-2215-3-1 摘要:Lane D, Matte I, Rancourt C, Piché A. The prosurvival activity of ascites against TRAIL is associated with a shorter disease-free interval in patients with ovarian cancer. Journal of Ovarian Research. 2010 Jan 18;3(1):1. doi: 10.1186/1757-2215-3-1. 参考文献:10.1007/s10529-011-0694-5 摘要:Mori K, Nakajima M, Kojima K, Murakami K, Ferri S, Sode K. Screening of Aspergillus-derived FAD-glucose dehydrogenases from fungal genome database. Biotechnol Lett. 2011 Nov;33(11):2255–63. doi: 10.1007/s10529-011-0694-5.