专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:US-7091334-B2 优先权日:1997-07-25 标题 :Method for large-scale production of di(uridine 5′)-tetraphosphate and salts thereof 发明人:YERXA BENJAMIN R; PENDERGAST WILLIAM 权利人:INSPIRE PHARMACEUTICALS INC 摘要:The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P 1 ,P 4 -di(uridine 5′)-tetraphosphate, and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P 1 ,P 4 -di(uridine 5′)-tetraphosphate (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. n nwherein:n X is Na, NH 4 or H, provided that all X groups are not H.
专利号:US-6319908-B1 优先权日:1996-07-03 标题 :Method for large-scale production of di(uridine 5′-tetraphosphate) and salts thereof 发明人:YERXA BENJAMIN R; PENDERGAST WILLIAM 权利人:INSPIRE PHARMACEUTICALS INC 摘要:The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P 1 ,P 4 -di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P 1 ,P 4 -di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture, n wherein: n X is Na, NH 4 or H, provided that all X groups are not H.
专利号:US-2023407357-A1 优先权日:2022-05-20 标 题 :Biomanufacturing of oligosaccharides and derivatives from simple sugar 发明人:HOEPKER ALEXANDER CHRIS; CORGIE STEPHANE CEDRIC; SAVINO KEITH 权利人:ZYMTRONIX CATALYTIC SYSTEMS INC 摘要:The invention provides methods for glycosylation and preparation of compounds. The compounds include galactosylated, sialylated, fucosylated, and N-acetylglucosaminylated compounds from simple animal-derived, plant-derived, or microbe-derived oligosaccharides and sugars. In certain embodiments, the invention provides trinucleotide-free enzymatic production of oligosaccharides starting from simple sugars that include plant-based sugars. The invention also provides the enzymatic production of fucosylated oligosaccharides and fucosylated antibody-glycan conjugates from common sugars. The production may be a cell-free, one-pot synthesis using enzymes, and in some embodiments, immobilized enzymes. The synthesis is a highly customizable and highly efficient cell-free manufacturing process. In some embodiments, lactose derivatives and human milk oligosaccharides (HMOs) are produced.
专利号:US-7939510-B2 优先权日:1997-07-25 标 题:Di(uridine 5′-)tetraphosphate and salts thereof 发明人:YERXA BENJAMIN R; BROWN EDWARD G 权利人:INSPIRE PHARMACEUTICALS INC 摘要:The present invention are directed to P 1 ,P 4 -di(uridine 5′-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P 1 ,P 4 -di(uridine 5′-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P 1 ,P 4 -di(uridine 5′-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.
专利号:US-6548658-B2 优先权日:1997-07-25 标 题:Di-(uridine 5′)-tetraphosphate and salts thereof 发明人:YERXA BENJAMIN R 权利人:INSPIRE PHARMACEUTICALS INC 摘要:The present invention provides methods for the synthesis of a pharmaceutically useful dinucleotide, P1, P4-di(uridine 5')-tetraphosphate, and demonstrates the applicability to the production of large quantities. The methods of the present invention substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less. The tetrasodium, ammonium, lithium and potassium salts of P1, P4-di(uridine 5')-tetraphosphate prepared by these methods are stable, soluble, nontoxic, of high purity and easy to handle during manufacture.
参考标题:Method For Large-Scale Production Of Di(Uridine 5')-Tetraphosphate And Salts Thereof 摘要:The Present Invention Provides Methods For The Synthesis Of A Pharmaceutically Useful Dinucleotide, P 1 , P 4 -Di(Uridine 5′)-Tetraphosphate, And Demonstrates The Applicability To The Production Of Large Quantities. The Methods Of The Present Invention Substantially Reduce The Time Required To Synthesize Diuridine Tetraphosphate, For Example, To Three Days Or Less. The Tetrasodium, Ammonium, Lithium And Potassium Salts Of P 1 , P 4 -Di(Uridine 5′)-Tetraphosphate Prepared By These Methods Are Stable, Soluble, Nontoxic, Of High Purity And Easy To Handle During Manufacture.
合成参考文献
参考文献:10.1038/s41592-022-01597-x 摘要:Ino D, Tanaka Y, Hibino H, Nishiyama M. A fluorescent sensor for real-time measurement of extracellular oxytocin dynamics in the brain. Nature Methods. 2022 Sep 22;19(10):1286–94. doi: 10.1038/s41592-022-01597-x.