IP Library Granted Patent US 9,637,512
Granted Patent B2
US 9,637,512 · App. 14/152,243 · Granted May 2, 2017

Nucleoside phosphoramidates

Inventors: Byoung-Kwon Chun (Robbinsville, NJ); Ganapati Reddy Pamulapati (San Ramon, CA); Suguna Rachakonda (Twinsburg, OH); Bruce Ross (El Granada, CA); Michael Joseph Sofia (Doylestown, PA); Peiyuan Wang (Totowa, NJ); Hai-Ren Zhang (San Jose, CA)
Assignee: Gilead Pharmasset LLC
C07H19/10A61K31/7072A61K31/716A61K45/00C07F9/24C07F9/242C07F9/65586C07H1/00C07H17/02
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Quick Facts
Patent No.
US 9,637,512
App. No.
14/152,243
Granted
May 2, 2017
Kind
B2
Abstract

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 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 (10)

1. A diastereoselective process for preparing (Sp-4):

comprising:

i) reacting compound C:

wherein LG′ is p-nitrophenoxide, 2,4-dinitrophenoxide or pentafluorophenoxide with a basic reagent and compound 3:

wherein Z is hydrogen, to obtain Sp-4; or

ii) reacting compound C with a basic reagent and compound 3, wherein Z is a protecting group, and deprotecting to obtain S P -4.

2. The process of claim 1 , wherein Z is hydrogen.

3. The process of claim 1 , wherein no chromatography is performed.

4. The process of claim 1 , wherein LG′ is p-nitrophenoxide.

5. The process of claim 1 , wherein LG′ is pentafluorophenoxide.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2022
From: GILEAD PHARMASSET LLC
To: GILEAD SCIENCES, INC.
Reel/Frame 060218/0501 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 16, 2014
From: ROSS, BRUCE; SOFIA, MICHAEL JOSEPH; PAMULAPATI, GANAPATI REDDY; RACHAKONDA, SUGUNA; ZHANG, HAI-REN; CHUN, BYOUNG-KWON; WANG, PEIYUAN
To: PHARMASSET, INC.
Reel/Frame 031981/0028 →
CHANGE OF NAME Recorded Jan 16, 2014
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 032040/0508 →
Continuity (5)
Continuation 13732725 · Jan 2, 2013
Division 12783680 · May 20, 2010
Provisional Application 61319513 · Mar 31, 2010
Provisional Application 61179923 · May 20, 2009
Related Publication 20140121366A1 · May 1, 2014