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HK1178171A1 - Crystalline (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-1-(2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate - Google Patents

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

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Publication number
HK1178171A1
HK1178171A1 HK13105092.1A HK13105092A HK1178171A1 HK 1178171 A1 HK1178171 A1 HK 1178171A1 HK 13105092 A HK13105092 A HK 13105092A HK 1178171 A1 HK1178171 A1 HK 1178171A1
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Hong Kong
Prior art keywords
phenoxy
mixture
isopropyl
crystalline
fluoro
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HK13105092.1A
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English (en)
French (fr)
Chinese (zh)
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HK1178171B (en
Inventor
Bruce S. Ross
Michael Joseph Sofia
Ganapati Reddy Pamulapati
Suguna Rachakonda
Hai-Ren Zhang
Byoung-Kwon Chun
Peiyuan Wang
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Gilead Pharmasset Llc
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Priority claimed from US12/783,680 external-priority patent/US8642756B2/en
Application filed by Gilead Pharmasset Llc filed Critical Gilead Pharmasset Llc
Publication of HK1178171A1 publication Critical patent/HK1178171A1/en
Publication of HK1178171B publication Critical patent/HK1178171B/en

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Claims (19)

  1. Kristallines (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, dargestellt durch die Formel SP-4: das XRPD 2θ-Reflexionen (°) bei etwa: 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 und 23,3 aufweist.
  2. Kristallines (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 nach Anspruch 1, das XRPD 2θ-Reflexionenen (°) bei etwa: 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 und 24,73 mit Intensitäten (%) von 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 bzw. 3,3 aufweist.
  3. Pharmazeutische Zusammensetzung umfassend kristallines (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 nach Anspruch 1 oder 2 und ein pharmazeutisch akzeptables Medium.
  4. Pharmazeutische Zusammensetzung nach Anspruch 3, ferner ein anderes antivirales Mittel umfassend.
  5. Pharmazeutische Zusammensetzung nach Anspruch 4, wobei das andere antivirale Mittel ein HCV NS3-Proteaseinhibitor ist.
  6. Pharmazeutische Zusammensetzung nach Anspruch 4, wobei das andere antivirale Mittel ein HCV NS5A-Inhibitor ist.
  7. Kristallines (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 nach Anspruch 1 oder 2 zur Verwendung als Medikament.
  8. Kristallines (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 nach Anspruch 1 oder 2 zur Verwendung bei der Behandlung einer Hepatitis C-Virusinfektion.
  9. Kristallines (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 zur Verwendung nach Anspruch 8 zur Verwendung in Kombination mit einem anderen antiviralen Mittel.
  10. Kristallines (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 zur Verwendung nach Anspruch 9, wobei das andere antivirale Mittel ein HCV NS3-Proteaseinhibitor ist.
  11. Kristallines (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 zur Verwendung nach Anspruch 9, wobei das andere antivirale Mittel ein HCV NS5A-Inhibitor ist.
  12. Medikament umfassend kristallines (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 nach Anspruch 1 oder 2.
  13. Medikament nach Anspruch 12, ferner ein anderes antivirales Mittel umfassend.
  14. Medikament nach Anspruch 13, wobei das andere antivirale Mittel ein HCV NS3-Proteaseinbibitor ist.
  15. Medikament nach Anspruch 13, wobei das andere antivirale Mittel ein HCV NS5A-Inbibitor ist.
  16. Verwendung eines kristallinen (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)propanoats nach Anspruch 1 oder 2 bei der Herstellung eines Medikaments zur Behandlung einer Hepatitis C-Virusinfektion.
  17. Verwendung eines kristallinen (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)propanoats nach Anspruch 1 oder 2 und eines anderen antiviralen Mittels bei der Herstellung eines Medikaments zur Behandlung einer Hepatitis C-Virusinfektion.
  18. Verwendung nach Anspruch 17, wobei das andere antivirale Mittel ein HCV NS3-Proteaseinhibitor ist.
  19. Verwendung nach Anspruch 17, wobei das andere antivirale Mittel ein HCV NS5A-Inhibitor ist.
HK13105092.1A 2010-03-31 2011-03-31 Crystalline (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-1-(2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate HK1178171B (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US31954810P 2010-03-31 2010-03-31
US31951310P 2010-03-31 2010-03-31
US319548P 2010-03-31
US319513P 2010-03-31
US783680 2010-05-20
US12/783,680 US8642756B2 (en) 2009-05-20 2010-05-20 Nucleoside phosphoramidates
PCT/US2011/030725 WO2011123645A2 (en) 2010-03-31 2011-03-31 Nucleoside phosphoramidates

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