IP Library Granted Patent US 8,735,569
Granted Patent B2
US 8,735,569 · App. 13/936,448 · Granted May 27, 2014

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
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Quick Facts
Patent No.
US 8,735,569
App. No.
13/936,448
Granted
May 27, 2014
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 (26)

1. A compound represented by the following structure:

2. A compound represented by the following structure:

3. The compound according to claim 1 , wherein the compound is crystalline.

4. A process for preparing the compound according to claim 3 , which comprises:

crystallizing a compound represented by the following structure:

from a second composition comprising

a) a first composition;

b) pentafluorophenol;

c) a non-nucleophilic base; and

d) a liquid composition;

wherein the first composition comprises the compound represented by the following structure:

and the compound represented by the following structure:

5. A process for preparing a compound represented by the following structure (S P -4):

which comprises:

crystallizing a compound represented by the following structure:

from a second composition comprising

a) a first composition;

b) pentafluorophenol;

c) a non-nucleophilic base; and

d) a liquid composition;

wherein the first composition comprises the compound represented by the following structure:

and the compound represented by the following structure:

6. A process for preparing a compound represented by the following structure (S P -4):

which comprises:

contacting the compound of claim 1 with a product obtained by reacting a compound represented by the following structure:

with a t-butylmagnesium halide.

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, PEIYAN
To: PHARMASSET, INC.
Reel/Frame 030838/0396 →
CHANGE OF NAME Recorded Jul 19, 2013
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 030838/0456 →
Continuity (6)
Division 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
Related Publication 20130310551A1 · Nov 21, 2013