Method for large-scale production of di(uridine...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/10 (2006.01) A61K 31/7072 (2006.01) A61K 31/7084 (2006.01) A61P 11/00 (2006.01) A61P 15/00 (2006.01) A61P 27/04 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2295515

The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-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 diurindine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5'-tetraphosphate) formula (I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. In formula I, X is Na, NH4 or H, provided that all X groups are not H.

La présente invention concerne de nouveaux procédés de synthèse du dinucléotide thérapeutique, P<1>,P<4>-di(uridine 5'-tétraphosphate), et met en relief leur possibilité d'application en vue d'une production à grande échelle. Les procédés de la présente invention réduisent sensiblement la période de temps nécessaire à la synthèse de diuridine tétraphosphate, de préférence à trois jours ou moins. Les nouveaux sels de tétrammonium et de tétrasodium de P<1>,P<4>-di(uridine 5'-tétraphosphate) de formule (I) préparés suivant ces procédés sont stables, solubles, non toxiques et faciles à manipuler durant la production. Dans la formule I, X représente Na, NH4 ou H, à condition que tous les groupes X ne représentent pas H.

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