Gilead Sciences Patent Applications

APOPTOSIS SIGNAL-REGULATING KINASE INHIBITOR

Granted: August 14, 2014
Application Number: 20140228412
The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.

THERAPEUTIC COMPOUNDS

Granted: August 7, 2014
Application Number: 20140221421
Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

THERAPEUTIC COMPOUNDS

Granted: August 7, 2014
Application Number: 20140221417
Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

VIRAL INHIBITORS

Granted: August 7, 2014
Application Number: 20140221382
Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.

THERAPEUTIC COMPOUNDS

Granted: August 7, 2014
Application Number: 20140221347
Compounds of formula I: or pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

THERAPEUTIC COMPOUNDS

Granted: August 7, 2014
Application Number: 20140221346
Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY

Granted: July 31, 2014
Application Number: 20140213556
The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants…

PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS

Granted: July 31, 2014
Application Number: 20140213539
Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

AMORPHOUS SOLID SALTS

Granted: July 3, 2014
Application Number: 20140187771
The invention provides an amorphous solid of a compound of formula (I) or of a salt thereof as well as compositions comprising the amorphous solids, and methods for making and using the amorphous solids.

TENOFOVIR ALAFENAMIDE HEMIFUMARATE

Granted: July 3, 2014
Application Number: 20140187773
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).

APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS

Granted: June 26, 2014
Application Number: 20140179663
The present invention relates to compounds of Formula (I): Wherein variables 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, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary…

COMPOUNDS FOR THE TREATMENT OF HIV

Granted: May 22, 2014
Application Number: 20140142085
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

Granted: May 15, 2014
Application Number: 20140135317
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

DRY POWDER FOSFOMYCIN/TOBRAMYCIN FORMULATION FOR INHALATION

Granted: May 15, 2014
Application Number: 20140134253
The present invention provides an inhaled dry powder formulation containing a combination of fosfomycin salt and tobramycin-leucine compound particles. The use of such formulation for the treatment of patients who have Chronic Obstructive Pulmonary Disease (COPD) and who are experiencing or at risk of experiencing acute exacerbation, as well as patients who have other bacterial infections of the respiratory tract, particularly the lower respiratory tract, and methods for treating the…

METHODS FOR PREPARING ANTI-VIRAL NUCLEOTIDE ANALOGS

Granted: May 8, 2014
Application Number: 20140128602
Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS

Granted: May 8, 2014
Application Number: 20140128389
The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.

THERAPEUTIC AND DIAGNOSTIC METHODS RELATED TO LYSYL OXIDASE-LIKE 2 (LOXL2)

Granted: May 1, 2014
Application Number: 20140120102
Provided are therapeutic, diagnostic, and prognostic methods for disease, including diseases associated with fibrosis and cancer using agents that bind to, inhibit, and/or detect lysyl oxidase-like 2 (LOXL2), and agents, compositions, kits, assay systems, and devices for use with such methods.

ANTIVIRAL COMPOUNDS

Granted: April 24, 2014
Application Number: 20140112885
The disclosure 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 PHARMACOKINETIC PROPERTIES OF THERAPEUTICS

Granted: April 17, 2014
Application Number: 20140105859
The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.

SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

Granted: April 17, 2014
Application Number: 20140107155
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.