Gilead Sciences Patent Grants

FXR (NR1H4) binding and activity modulating compounds

Granted: November 26, 2019
Patent Number: 10485795
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.

Phosphatidylinositol 3-kinase inhibitors

Granted: November 19, 2019
Patent Number: 10479770
The present application provides the compounds of formula I or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein t, R1, R2, R3, R4, and R6 are as described herein.

Macrocyclic inhibitors of flaviviridae viruses

Granted: November 12, 2019
Patent Number: 10472392
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 virus infections, particularly hepatitis C infections.

Substituted dipyrido[1,2-a:1?,2?-d]pyrazines for treating viral infections

Granted: October 29, 2019
Patent Number: 10456395
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 L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Compounds for the treatment of hepatitis B virus infection

Granted: October 15, 2019
Patent Number: 10442804
The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

FXR (NR1H4) modulating compounds

Granted: September 24, 2019
Patent Number: 10421730
The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure 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.

Process methods for phosphatidylinositol 3-kinase inhibitors

Granted: September 17, 2019
Patent Number: 10414737
A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

Crystalline forms of darunavir

Granted: September 10, 2019
Patent Number: 10407438
The present invention relates to novel crystalline forms of darunavir, the pharmaceutical formulations, and the therapeutic uses thereof in treating viral infections.

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: August 20, 2019
Patent Number: 10385067
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, pharmaceutical formulations, and uses thereof for treating or prophylactically preventing an HIV infection.

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

Granted: August 13, 2019
Patent Number: 10377761
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.

Inhibitors of bruton'S tyrosine kinase

Granted: August 6, 2019
Patent Number: 10370381
Provided are forms of 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, compositions thereof, methods for their preparation, and methods for their use.

Compounds for the treatment of HIV

Granted: August 6, 2019
Patent Number: 10370358
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.

Toll like receptor modulator compounds

Granted: August 6, 2019
Patent Number: 10370342
This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

Substituted imidazo[1,2-a]pyrazines as Syk inhibitors

Granted: July 9, 2019
Patent Number: 10342794
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods…

Pyrrolo[1,2-b]pyridazine derivatives

Granted: July 2, 2019
Patent Number: 10336762
Provided is a compound of Formula (I) wherein the variable groups are defined herein.

FXR (NR1H4) modulating compounds

Granted: June 25, 2019
Patent Number: 10329286
The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure 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.

Substituted pyrrolizine compounds and uses thereof

Granted: June 25, 2019
Patent Number: 10328053
This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.

Inhibitors of Bruton's tyrosine kinase

Granted: June 11, 2019
Patent Number: 10314844
Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.

Tank-binding kinase inhibitor compounds

Granted: June 11, 2019
Patent Number: 10316049
Compounds having the following formula (I) and methods of their use and preparation are disclosed:

COT modulators and methods of use thereof

Granted: June 11, 2019
Patent Number: 10316017
The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.