IP Library Granted Patent US 9,284,342
Granted Patent B2
US 9,284,342 · App. 13/925,078 · Granted Mar 15, 2016

Nucleoside phosphoramidates

Inventors: Bruce S. Ross (El Granada, CA); Michael Joseph Sofia (Doylestown, PA); Ganapati Reddy Pamulapati (San Ramon, CA); Suguna Rachakonda (Twinsburg, OH); Hai-Ren Zhang (San Jose, CA); Byoung-Kwon Chun (Robbinsville, NJ); Peiyuan Wang (Totowa, NJ)
Assignee: Gilead Pharmasset LLC
C07H19/10A61K31/7072A61K45/06C07F9/2479C07H19/06C07H23/00
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Quick Facts
Patent No.
US 9,284,342
App. No.
13/925,078
Granted
Mar 15, 2016
Kind
B2
Abstract

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

Claims (16)

1. A crystalline compound represented by the formula (S P -4):

having XRPD 2θ-reflections (°) at about: 6.1 and 12.7.

2. A pharmaceutical composition comprising the crystalline compound according to claim 1 and a pharmaceutically acceptable medium.

3. A method of treating a hepatitis C virus infection in a human comprising administering to the human an effective amount of the crystalline compound according to claim 1 .

4. The method according to claim 3 further comprising administering to the human another antiviral agent.

5. A process for preparing the crystalline compound according to claim 1 comprising:

exposing a second crystalline compound represented by the formula (S P -4):

having an XRPD diffraction pattern substantially as shown in FIG. 3 or FIG. 4 to atmospheric humidity to provide a first composition.

6. The process according to claim 5 further comprising:

grinding the first composition into a powder; and

allowing the powder to stand in an open vessel.

7. A process for preparing the crystalline compound according to claim 1 comprising:

suspending a second crystalline compound represented by the formula (S P -4):

having an XRPD diffraction pattern substantially as shown in FIG. 3 or FIG. 4 in water to provide a suspension.

8. The process according to claim 7 further comprising heating the suspension.

9. The process according to claim 8 further comprising cooling the suspension.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2022
From: GILEAD PHARMASSET LLC
To: GILEAD SCIENCES, INC.
Reel/Frame 060218/0316 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2013
From: ROSS, BRUCE S.; SOFIA, MICHAEL JOSEPH; PAMULAPATI, GANAPATI REDDY; RACHAKONDA, SUGUNA; ZHANG, HAI-REN; CHUN, BYOUNG-KWON; WANG, PEIYUAN
To: PHARMASSET, INC.
Reel/Frame 030838/0240 →
CHANGE OF NAME Recorded Jul 19, 2013
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 030838/0329 →
Continuity (7)
Continuation 13076552 · Mar 31, 2011
Continuation In Part 12783680 · May 20, 2010
Provisional Application 61319513 · Mar 31, 2010
Provisional Application 61319548 · Mar 31, 2010
Provisional Application 61179923 · May 20, 2009
Provisional Application 61319513 · Mar 31, 2010
Related Publication 20130288997A1 · Oct 31, 2013