IP Library Granted Patent US 10,100,076
Granted Patent B2
US 10,100,076 · App. 13/908,098 · Granted Oct 16, 2018

Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation

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Quick Facts
Patent No.
US 10,100,076
App. No.
13/908,098
Granted
Oct 16, 2018
Kind
B2
Abstract

The disclosed invention is a composition for and a method of seating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. This invention also provides an effective process to quantify the viral load, and in particular BVDV, HCV or West Nile Virus load, in a host, using real-time polymerase chain reaction (“RT-PCR”). Additionally, the invention discloses probe molecules that can fluoresce proportionally to the amount of virus present in a sample.

Claims (86)

1. A method of treating a viral infection or abnormal cellular proliferation in a human exhibiting the viral infection or abnormal cellular proliferation, wherein the viral infection is not caused by Human Immunodeficiency Virus, comprising administering to the human an effective amount of a compound of the general formula (I-b)

or its β-L enantiomer or its pharmaceutically acceptable salt thereof, wherein:

D is hydrogen;

W 2 is N; and

wherein the compound of formula (I-b) is selected from one of the following:

X 1

X 2

W 1

R 2

R 2 ′

R 3

R 3 ′

OH

NH 2

N

H

OH

H

OH

OH

NH 2

CH

F

H

H

OH

NH-cyclohexyl

H

CH

H

H

H

H

NH 2

NH 2

N

H

OH

H

OH

NH 2

NH 2

CH

H

OH

H

OH

Cl

H

CH

F

H

H

H

Cl

I

CH

H

O—Ac

H

O—Ac

Cl

H

CH

H

OH

H

OH

Cl

H

CH

H

OH

H

H

NH 2

H

CH

H

OH

H

F.

2. The method of claim 1 wherein the viral infection is Flaviviridae.

3. The method of claim 1 wherein the viral infection is Orthomyxoviridae.

4. The method of claim 1 wherein the viral infection is Paramyxoviridae.

5. The method of claim 1 wherein the compound is selected from the group consisting of

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2022
From: GILEAD PHARMASSET LLC
To: GILEAD SCIENCES, INC.
Reel/Frame 059479/0024 →
CHANGE OF NAME Recorded Sep 2, 2014
From: PHARMASSET, LTD.
To: PHARMASSET, INC.
Reel/Frame 033677/0156 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2013
From: WATANABE, KYOICHI A.; STUYVER, LIEVEN
To: PHARMASSET LTD.
Reel/Frame 030840/0046 →
CHANGE OF NAME Recorded Jul 19, 2013
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 030843/0272 →
Cited By (1)
US 12,551,497