Gilead Sciences Patent Applications

SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

Granted: April 25, 2013
Application Number: 20130102632
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.

FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

Granted: April 18, 2013
Application Number: 20130096122
The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.

ANTIVIRAL COMPOUNDS

Granted: April 11, 2013
Application Number: 20130090302
The invention is related to phosphorus substituted anti-viral inhibitory 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.

PHOSPHONATE ANALOGS OF HIV INHIBITOR COMPOUNDS

Granted: April 11, 2013
Application Number: 20130090299
The invention is related to phosphorus substituted anti-viral inhibitory 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: March 21, 2013
Application Number: 20130071354
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.

TENOFOVIR ALAFENAMIDE HEMIFUMARATE

Granted: March 14, 2013
Application Number: 20130065856
A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).

INHIBITORS OF FLAVIVIRIDAE VIRUSES

Granted: February 28, 2013
Application Number: 20130052161
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 (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.

HCV GENOTYPE 3 REPLICONS

Granted: February 28, 2013
Application Number: 20130052633
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.

ANTIVIRAL COMPOUNDS

Granted: February 28, 2013
Application Number: 20130053577
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.

1'-SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT

Granted: February 7, 2013
Application Number: 20130034521
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.

APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS

Granted: February 7, 2013
Application Number: 20130035339
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the…

MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES

Granted: January 24, 2013
Application Number: 20130022573
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.

BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS

Granted: January 17, 2013
Application Number: 20130018050
This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.

BI-FUNCTIONAL QUINOLINE ANALOGS

Granted: January 10, 2013
Application Number: 20130012504
Provided are compounds of Formula I: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS

Granted: January 10, 2013
Application Number: 20130012521
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the…

COMPOUNDS FOR THE TREATMENT OF ADDICTION

Granted: January 3, 2013
Application Number: 20130005689
Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a…

ALKANOYLAMINO BENZAMIDE ANILINE HDAC INHIBITOR COMPOUNDS

Granted: November 29, 2012
Application Number: 20120301426
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

ANTIVIRAL COMPOUNDS

Granted: October 18, 2012
Application Number: 20120264711
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.

1'-SUBSTITUTED PYRIMIDINE N-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT

Granted: October 18, 2012
Application Number: 20120263678
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.

PROCESS FOR PREPARATION OF HIV PROTEASE INHBITORS

Granted: October 11, 2012
Application Number: 20120258935
A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed