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DK2552930T3 - Krystallinsk (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin- 1-(2h)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphoryl)amino)propanoat - Google Patents

Krystallinsk (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin- 1-(2h)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphoryl)amino)propanoat Download PDF

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DK2552930T3
DK2552930T3 DK11714465.9T DK11714465T DK2552930T3 DK 2552930 T3 DK2552930 T3 DK 2552930T3 DK 11714465 T DK11714465 T DK 11714465T DK 2552930 T3 DK2552930 T3 DK 2552930T3
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phenoxy
mixture
crystalline
isopropyl
fluoro
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DK11714465.9T
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Suguna Rachakonda
Byoung-Kwon Chun
Bruce S Ross
Michael Joseph Sofia
Ganapati Reddy Pamulapati
Hai-Ren Zhang
Peiyuan Wang
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Gilead Pharmasset Llc
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Priority claimed from US12/783,680 external-priority patent/US8642756B2/en
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Claims (19)

  1. KRYSTALLINSK (S)-ISOPROPYL 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1 -(2H)-YL)-4-FLUOR-3-HYDROXY -4-METHYLTETRAHYDROFURAN-2-YL)METHOXY)(PHENOXY)PHOSPHORYL)AMINO)PROPANOAT
    1. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat repræsenteret af formlen SP-4:
    Sp-4 der har XRPD 20-reflektioner (°) ved omkring: 6,1, 8,2, 10,4, 12,7, 17,2, 17,7, 18,0, 18,8, 19,4, 19,8,20,1,20,8,21,8 og 23,3.
  2. 2. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1, der har XRPD 20-reflektioner (°) ved omkring: 6,08, 8,2, 10,38, 10,85, 12,17, 12,7, 13,73, 14,1, 15,91, 16,83, 17,17, 17,66, 17,95, 18,79, 19,1, 19,41, 19,8, 20,11, 20,82, 21,81, 22,03, 23,03, 23,26, 23,64, 23,89 og 24,73 med intensiteter (%) på henholdsvis 66,7, 62,1, 29,8, 10,4, 12,0, 66,4, 14,9, 13,8, 3,1, 8,7, 19,7, 56,2, 37,7, 59,0, 14,3, 37,2, 46,0, 68,8, 100,0, 36,8, 7,4, 14,2, 21,6, 6,3, 7,0 og 3,3.
  3. 3. Farmaceutisk sammensætning, der omfatter krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2 og et farmaceutisk acceptabelt medium.
  4. 4. Farmaceutisk sammensætning ifølge krav 3, hvilken sammensætning endvidere omfatter et andet antiviralt middel.
  5. 5. Farmaceutisk sammensætning ifølge krav 4, hvor det andet antivirale middel er en HCV NS3-proteaseinhibitor.
  6. 6. Farmaceutisk sammensætning ifølge krav 4, hvor det andet antivirale middel er en HCV NS5A-inhibitor.
  7. 7. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofiiran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2 til anvendelse som et medikament.
  8. 8. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofiiran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2 til anvendelse i behandling af en hepatitis C-virusinfektion.
  9. 9. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)- 4-fluor-3-hydroxy-4-methyltetrahydrofiiran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat til anvendelse ifølge krav 8 til anvendelse i kombination med et andet antiviralt middel.
  10. 10. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)- 4-fluor-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(pbenoxy)pbospboryl)amino)propanoat til anvendelse ifølge krav 9, hvor det andet antivirale middel er en HCV NS3-proteaseinhibitor.
  11. 11. Krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)- 4-fluor-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat til anvendelse ifølge krav 9, hvor det andet antivirale middel er en HCV NS5A-inhibitor.
  12. 12. Medikament, der omfatter krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4-fLuor-3-hydroxy-4-methyltetrahydrofiiran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2.
  13. 13. Medikament ifølge krav 12, hvilket medikament endvidere omfatter et andet antiviralt middel.
  14. 14. Medikament ifølge krav 13, hvor det andet antivirale middel er en HCV NS3-proteaseinhibitor.
  15. 15. Medikament ifølge krav 13, hvor det andet antivirale middel er en HCV NS5A-inhibitor.
  16. 16. Anvendelse af en krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4- dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2 i fremstillingen af et medikament til behandling af en hepatitis C-virusinfektion.
  17. 17. Anvendelse af en krystallinsk (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4- dihydropyrimidin-l(2H)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphoryl)amino)propanoat ifølge krav 1 eller 2 og et andet antiviralt middel til fremstilling af et medikament til behandling af en hepatitis C virusinfection.
  18. 18. Anvendelse ifølge krav 17, hvor det andet antivirale middel er en HCV NS3-proteaseinhibitor.
  19. 19. Anvendelse ifølge krav 17, hvor det andet antivirale middel er en HCV NS5A-inhibitor.
DK11714465.9T 2010-03-31 2011-03-31 Krystallinsk (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin- 1-(2h)-yl)-4-fluor-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphoryl)amino)propanoat DK2552930T3 (da)

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US31951310P 2010-03-31 2010-03-31
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US12/783,680 US8642756B2 (en) 2009-05-20 2010-05-20 Nucleoside phosphoramidates
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