IP Library Granted Patent US 9,206,217
Granted Patent B2
US 9,206,217 · App. 13/732,725 · Granted Dec 8, 2015

Nucleoside phosphoramidates

Inventors: Bruce 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
C07H19/10A61K31/7072A61K31/716A61K45/00C07F9/24C07F9/242C07F9/65586C07H17/02
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Quick Facts
Patent No.
US 9,206,217
App. No.
13/732,725
Granted
Dec 8, 2015
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 (18)

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

wherein the compound is monoclinic crystalline (S P -4) having unit cell parameters:

i) a˜12.88 Å, b˜6.17 Å, c˜17.73 Å, and β˜92.05°;

ii) a˜20.09 Å, b˜6.10 Å, c˜23.01 Å, and β˜112.29°;

iii) a˜12.83 Å, b˜6.15 Å, c˜17.63 Å, and β−91.75°; or

iv) a˜12.93 Å, b˜6.18 Å, c˜18.01 Å, and β˜96.40°.

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

wherein the compound is monoclinic crystalline having XRPD 2θ-reflections (°) at about:

i) 5.2, 7.5, 9.6, 16.7, 18.3, and 22.2;

ii) 5.0, 7.3, 9.4, and 18.1;

iii) 4.9, 6.9, 9.8, 19.8, 20.6, 24.7, and 26.1;

iv) 6.9, 9.8, 19.7, 20.6, and 24.6;

v) 5.0, 6.8, 19.9, 20.6, 20.9, and 24.9; or

vi) 5.2, 6.6, 7.1, 15.7, 19.1, and 25.0.

3. The compound of claim 2 having XRPD 2θ-reflections (°) at about:

i) 5.2, 7.5, 9.6, 16.7, 18.3, and 22.2; or

ii) 5.0, 7.3, 9.4, and 18.1.

4. A composition comprising the compound according to any one of claim 1 , 2 or 3 and a pharmaceutically acceptable medium.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2022
From: GILEAD PHARMASSET LLC
To: GILEAD SCIENCES, INC.
Reel/Frame 060218/0501 →
CHANGE OF NAME Recorded Jan 15, 2013
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 029635/0086 →
ASSIGNMENT OF ASSIGNORS INTEREST Recorded Jan 15, 2013
From: ROSS, BRUCE; SOFIA, MICHAEL JOSEPH; PAMULAPATI, GANAPATI REDDY; RACHAKONDA, SUGUNA; ZHANG, HAI-REN; CHUN, BYOUNG-KWON; WANG, PEIYUAN
To: PHARMASSET, INC.
Reel/Frame 029635/0090 →
Continuity (4)
Division 12783680 · May 20, 2010
Provisional Application 61319513 · Mar 31, 2010
Provisional Application 61179923 · May 20, 2009
Related Publication 20130165401A1 · Jun 27, 2013