US 8,946,244 B2 · 2′-fluoro-6′methylene carbocyclic nucleosides and methods of treating viral infections

Abstract

The present invention relates to 2′-Fluoro-6′-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Hepatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.

Claims41

Dependent claims

A nucleoside compound according to the structure:

Where B is
Wherein R is H, F, Cl, Br, I, C1-C4 alkyl, —C≡N, —C≡C—Ra,
X is H, C1-C4 alkyl (preferably, CH3), F, Cl, Br or I;
Ra is H;
R1 and R1a are each independently, H, an acyl group, a C1-C20 alkyl or ether group, an amino acid residue (D or L), a phosphate, diphosphate, triphosphate, phosphodiester or phosphoamidate group or together R1 and R1a form a carbodiester or phosphodiester group with the oxygen atoms to which they are bonded;
R2 is H, an acyl group, a C1-C20 alkyl or ether group or an amino acid residue (D or L);
Or a pharmaceutically acceptable salt or;
enantiomer thereof.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/510,090Filed 16 Nov 2010 · us provisional application

Priority

16 Nov 2009

Published

US 2013/0005677 A13 Jan 2013

Granted

3 Feb 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification14 codes

C07D 473/34
Nitrogen atom: attached in position 6, e.g. adenine
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61P 1/16
Drugs for disorders of the alimentary tract or the digestive system: for liver or gallbladder disorders, e.g. hepatoprotective agents,…
A61P 31/12
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antivirals

2′-fluoro-6′methylene carbocyclic nucleosides and methods of treating viral infections

Life of this patent

2′-fluoro-6′methylene carbocyclic nucleosides and methods of treating viral infections

Life of this patent

Abstract

Claims41