Gilead Sciences Patent Grants

Therapeutic compounds

Granted: October 17, 2017
Patent Number: 9789089
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.

Processes and intermediates for preparing anti-HIV agents

Granted: October 10, 2017
Patent Number: 9783567
The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.

Salts of HIV inhibitor compounds

Granted: October 10, 2017
Patent Number: 9783568
The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to process and intermediates useful for preparing such salts.

Co-crystals, salts and solid forms of tenofovir alafenamide

Granted: October 3, 2017
Patent Number: 9777028
The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds.

Processes for preparing ASK1 inhibitors

Granted: September 26, 2017
Patent Number: 9771328
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.

Phosphatidylinositol 3-kinase inhibitors

Granted: September 19, 2017
Patent Number: 9765060
The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these…

Apoptosis signal-regulating kinase inhibitor

Granted: September 5, 2017
Patent Number: 9750730
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.

Hydroxy containing FXR (NR1H4) modulating compounds

Granted: September 5, 2017
Patent Number: 9751874
The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

Compositions and methods for combination antiviral therapy

Granted: August 29, 2017
Patent Number: 9744181
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…

Solid forms of a toll-like receptor modulator

Granted: August 22, 2017
Patent Number: 9738646
The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.

Quinazoline compounds

Granted: August 15, 2017
Patent Number: 9730936
Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.

Substituted 2,3,4,5,7,9,13,13a-octahydropyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]OXAZEPINES and methods for treating viral infections

Granted: August 15, 2017
Patent Number: 9732092
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Methods for treating virus infections

Granted: August 8, 2017
Patent Number: 9724360
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

Combination methods for treating cancers

Granted: July 18, 2017
Patent Number: 9707236
Disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I: or a pharmaceutically acceptable salt thereof; in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof. The subject may be very high risk or high risk for the cancer and may not respond to either agent administered as a sole therapy. The subject who has the cancer…

Sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2, 1-b][1, 3]oxazepin-8-olate

Granted: July 18, 2017
Patent Number: 9708342
The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3] oxazepin-8-olate Form I and the therapeutic uses thereof.

Polycyclic-carbamoylpyridone compounds and their pharmaceutical use

Granted: July 11, 2017
Patent Number: 9700554
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Fused pyrimidine compounds

Granted: July 11, 2017
Patent Number: 9701677
Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.

Pyrrolo[1,2-][1,2,4]triazines useful for treating respiratory syncitial virus infections

Granted: July 11, 2017
Patent Number: 9701682
Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.

Fused heterocyclic compounds as ion channel modulators

Granted: July 4, 2017
Patent Number: 9695192
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 Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Methods for treating cancers

Granted: June 27, 2017
Patent Number: 9687492
Disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I: or a pharmaceutically acceptable salt thereof. The subject may be very high risk or high risk for the cancer. The subject who has the cancer may also be refractory to at least one chemotherapy treatment, or is in relapse after treatment with chemotherapy, or both. The cancer may be a…