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    • 8. 发明授权
    • Di(uridine 5′-)tetraphosphate and salts thereof
    • 二(尿苷5' - )四磷酸及其盐
    • US07939510B2
    • 2011-05-10
    • US12430684
    • 2009-04-27
    • Benjamin R. YerxaEdward G. Brown
    • Benjamin R. YerxaEdward G. Brown
    • A61K31/70
    • A61K31/7048A61K31/7068A61K31/7072A61K31/7076C07H19/10C07H19/20C07H21/00Y10S514/851
    • The present invention are directed to P1,P4-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 P1,P4-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 P1,P4-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.
    • 本发明涉及P1,P4-二(尿苷5'-)四磷酸盐,四碱金属盐如四钠,四锂,四钾及其混合四碱金属阳离子。 P1,P4-二(尿苷5' - )四磷酸的四碱金属盐是水溶性的,无毒的,在制造过程中易于处理。 这些四价一价碱金属盐比单 - ,二 - 或三 - 酸盐更耐水解,因此,它们提供了改进的稳定性和更长的储存期限。 本发明还提供了合成P1,P4-二(尿苷5' - )四磷酸及其药学上可接受的盐的方法,并且证明了对大量生产的适用性。 所述方法基本上减少了合成二脯氨酸四磷酸酯所需的时间,例如为3天或更短。
    • 9. 发明授权
    • Di(uridine 5′-)tetraphosphate and salts thereof
    • 二(尿苷5' - )四磷酸及其盐
    • US07528119B2
    • 2009-05-05
    • US11486497
    • 2006-07-14
    • Benjamin R. YerxaEdward G. Brown
    • Benjamin R. YerxaEdward G. Brown
    • A61K31/70
    • A61K31/7048A61K31/7068A61K31/7072A61K31/7076C07H19/10C07H19/20C07H21/00Y10S514/851
    • The present invention are directed to P1,P4-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 P1,P4-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 P1,P4-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.
    • 本发明涉及P1,P4-二(尿苷5'-)四磷酸盐,四碱金属盐如四钠,四锂,四钾及其混合四碱金属阳离子。 P1,P4-二(尿苷5' - )四磷酸的四碱金属盐是水溶性的,无毒的,在制造过程中易于处理。 这些四价一价碱金属盐比单 - ,二 - 或三 - 酸盐更耐水解,因此,它们提供了改进的稳定性和更长的储存期限。 本发明还提供了合成P1,P4-二(尿苷5' - )四磷酸及其药学上可接受的盐的方法,并且证明了对大量生产的适用性。 所述方法基本上减少了合成二脯氨酸四磷酸酯所需的时间,例如为3天或更短。
    • 10. 发明申请
    • DI(URIDINE 5'-)TETRAPHOSPHATE AND SALTS THEREOF
    • DI(尿苷5' - )四磷酸酯及其盐
    • US20090326050A1
    • 2009-12-31
    • US12430684
    • 2009-04-27
    • Benjamin R. YerxaEdward G. Brown
    • Benjamin R. YerxaEdward G. Brown
    • A61K31/711A61P27/02
    • A61K31/7048A61K31/7068A61K31/7072A61K31/7076C07H19/10C07H19/20C07H21/00Y10S514/851
    • The present invention are directed to P1,P4-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 P1,P4-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 P1,P4-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.
    • 本发明涉及P1,P4-二(尿苷5'-)四磷酸盐,四碱金属盐如四钠,四锂,四钾及其混合四碱金属阳离子。 P1,P4-二(尿苷5' - )四磷酸的四碱金属盐是水溶性的,无毒的,在制造过程中易于处理。 这些四价一价碱金属盐比单 - ,二 - 或三 - 酸盐更耐水解,因此,它们提供了改进的稳定性和更长的储存期限。 本发明还提供了合成P1,P4-二(尿苷5' - )四磷酸及其药学上可接受的盐的方法,并且证明了对大量生产的适用性。 所述方法基本上减少了合成二脯氨酸四磷酸酯所需的时间,例如为3天或更短。