Gilead Sciences Patent Grants

HCV genotype 4 replicons

Granted: November 18, 2014
Patent Number: 8889849
Replicons of genotype 4 hepatitis C virus (HCV) are provided. These replicons contains adaptive mutations giving rise to the HCV's capability to replicate in vitro. Methods of preparing genotype 4 replicons and methods of using these replicons to screen antiviral agents are also provided.

HCV genotype 3 replicons

Granted: November 18, 2014
Patent Number: 8889848
Replicons of genotype 3 of hepatitis C virus (HCV) are provided. These replicons contains adaptive mutations giving rise to the HCV's capability to replicate in vitro. Methods of preparing genotype 3 replicons and methods of using these replicons to screen antiviral agents are also provided.

Inhibitors of viruses

Granted: November 11, 2014
Patent Number: 8884030
Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Method of treating diabetes

Granted: November 11, 2014
Patent Number: 8883750
Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.

Process and intermediates for preparing integrase inhibitors

Granted: November 4, 2014
Patent Number: 8877931
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

1?-substituted pyrimidine N-nucleoside analogs for antiviral treatment

Granted: November 4, 2014
Patent Number: 8877733
Provided are compounds of Formula I: nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.

Antiviral phosphonate analogs

Granted: October 28, 2014
Patent Number: 8871785
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Method and composition for pharmaceutical product

Granted: October 28, 2014
Patent Number: 8871271
This invention is directed to a composition comprising dry granulated tenofovir DF and emtricitabine, and a method for making same. Dry granulation was unexpectedly found to be important in preparing a tenofovir DF containing composition suitable for inclusion in a combination dosage form containing emtricitabine, efavirenz and tenofovir DF.

Substituted heterocyclic compounds as ion channel modulators

Granted: October 21, 2014
Patent Number: 8865739
The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Methods and intermediates for preparing pharmaceutical agents

Granted: October 7, 2014
Patent Number: 8853210
The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.

1?-substituted carba-nucleoside analogs for antiviral treatment

Granted: October 7, 2014
Patent Number: 8853171
Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Solid forms of an antiviral compound

Granted: September 23, 2014
Patent Number: 8841340
Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

Inhibitors of human immunodeficiency virus replication

Granted: September 23, 2014
Patent Number: 8841331
Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections

Granted: September 23, 2014
Patent Number: 8841286
A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a…

Method of treating diabetes

Granted: September 2, 2014
Patent Number: 8822473
Methods are provided for lowering plasma level of HbA1c in a diabetic, pre-diabetic, or non-diabetic patient suffering from at least one cardiovascular disease and slowing or delaying the development of or worsening of hyperglycemia in a diabetic, pre-diabetic, or non-diabetic patient.

Heterocyclic flaviviridae virus inhibitors

Granted: August 26, 2014
Patent Number: 8815858
The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.

Antiviral compounds

Granted: August 19, 2014
Patent Number: 8809266
The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Modulators of toll-like receptors

Granted: August 19, 2014
Patent Number: 8809527
Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Pyrazolo[1,5-A]pyrimidines for antiviral treatment

Granted: August 19, 2014
Patent Number: 8809330
The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Antiviral compounds

Granted: August 19, 2014
Patent Number: 8809267
The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.