Gilead Sciences Patent Applications

SOLID FORMS OF AN ASK1 INHIBITOR

Granted: September 29, 2016
Application Number: 20160280683
Crystalline forms of 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

Processes for preparing ASK1 inhibitors

Granted: August 25, 2016
Application Number: 20160244430
The present disclosure provides processes for the preparation of a compound of formula: which exhibits 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. The disclosure also provides compounds that are synthetic intermediates.

TANK-BINDING KINASE INHIBITOR COMPOUNDS

Granted: April 7, 2016
Application Number: 20160096827
Compounds having the following formula (I) and methods of their use and preparation are disclosed:

BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS

Granted: March 17, 2016
Application Number: 20160075695
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1, R1b, R2a, R2b, R3, R4a, R4b, and R5 are described herein.

MODULATORS OF PHARMACOKINETIC PROPERTIES OF THERAPEUTICS

Granted: March 10, 2016
Application Number: 20160067360
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.

TANK-BINDING KINASE INHIBITOR COMPOUNDS

Granted: December 3, 2015
Application Number: 20150344473
Compounds having the following formula (I) and methods of their use and preparation are disclosed:

CRYSTALLINE FORMS OF AN ANTIVIRAL COMPOUND

Granted: June 25, 2015
Application Number: 20150175625
Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of…

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Granted: June 25, 2015
Application Number: 20150175626
The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

TABLETS FOR COMBINATION THERAPY

Granted: June 4, 2015
Application Number: 20150150810
The invention provides solid dose forms (e.g. tablets) comprising a compound of Formula I, a compound of Formula II, a compound of Formula III and a salt of Formula IV.

COMBINATION THERAPY FOR TREATING PULMONARY HYPERTENSION

Granted: May 7, 2015
Application Number: 20150125546
Method of treating and/or preventing pulmonary arterial hypertension comprising administering effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and riociguat or a pharmaceutically acceptable salt thereof.

COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY

Granted: April 23, 2015
Application Number: 20150111855
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…

COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY

Granted: April 23, 2015
Application Number: 20150111856
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…

NAPHTHALENE ACETIC ACID DERIVATIVES AGAINST HIV INFECTION

Granted: April 23, 2015
Application Number: 20150111891
The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

COMBINATION THERAPY COMPRISING TENOFOVIR ALAFENAMIDE HEMIFUMARATE AND COBICISTAT FOR USE IN THE TREATMENT OF VIRAL INFECTIONS

Granted: April 16, 2015
Application Number: 20150105350
The use of the hemifumarate form of {9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine} (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir, and the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and darunavir, are disclosed.

ANTIVIRAL COMPOUNDS

Granted: March 19, 2015
Application Number: 20150080569
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.

PROCESS FOR PREPARING DRONEDARONE AND SALTS THEREOF

Granted: March 5, 2015
Application Number: 20150065734
The present disclosure relates to processes for preparing dronedarone or pharmaceutically acceptable salts thereof.

SPRAY DRIED FORMULATIONS

Granted: February 12, 2015
Application Number: 20150045366
The invention provides a spray dried formulation of Compound I: or a salt thereof as well as compositions comprising the spray dried formulations, and methods for making and using the spray dried formulations.

PHARMACEUTICAL COMPOSITIONS OF RANOLAZINE AND DRONEDARONE

Granted: February 5, 2015
Application Number: 20150037410
The present disclosure relates to a solid composition comprising ranolazine and a spray-dried phosphoric acid salt of dronedarone in a bilayer tablet.

COMPOUND AND METHODS FOR TREATING LONG QT SYNDROME

Granted: February 5, 2015
Application Number: 20150038489
Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blocker

METHODS OF MYOCARDIAL PERFUSION IMAGING

Granted: January 22, 2015
Application Number: 20150023867
The present invention provides a method of myocardial perfusion imaging using reduced doses of (1-{9-[(4S,2R,3R,5R)3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide.