Gilead Sciences Patent Grants

Processes for preparing toll-like receptor modulator compounds

Granted: March 29, 2022
Patent Number: 11286257
The present disclosure provides methods for preparing (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol or a salt thereof and related key intermediates.

Processes for preparing ACC inhibitors and solid forms thereof

Granted: March 22, 2022
Patent Number: 11279710
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: which exhibits Acetyl-CoA carboxylase (“ACC”) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

Therapeutic compounds

Granted: March 8, 2022
Patent Number: 11267801
The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.

Solid forms of an HIV capsid inhibitor

Granted: March 8, 2022
Patent Number: 11267799
The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae…

Compositions comprising an RNA polymerase inhibitor and cyclodextrin for treating viral infections

Granted: March 8, 2022
Patent Number: 11266681
The present disclosure provides a composition comprising Compound 1, or a pharmaceutically acceptable salt thereof, cyclodextrin, and, optionally, pH adjusting agents.

Methods for treating virus infections

Granted: March 8, 2022
Patent Number: 11266666
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.

Choline salt forms of an HIV capsid inhibitor

Granted: March 8, 2022
Patent Number: 11266638
The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3- (trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection…

Processes for preparing ASK1 inhibitors

Granted: March 1, 2022
Patent Number: 11261161
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.

Methods of treating feline coronavirus infections

Granted: March 1, 2022
Patent Number: 11260070
Provided are methods of treating feline Coronavirus infections using carbanucleoside compounds having a 1?-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl) substituent, or a pharmaceutically acceptable salt thereof. An exemplary compound is (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile.

Metabolites of bictegravir

Granted: February 22, 2022
Patent Number: 11253524
The present invention provides metabolites of the antiviral drug bictegravir, including compositions and salts thereof, which are useful in the prevention and/or treatment of HIV as well as analytical methods related to the administration of bictegravir.

FXR (NR1H4) modulating compounds

Granted: February 15, 2022
Patent Number: 11247986
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.

PD-1/PD-L1 inhibitors

Granted: February 1, 2022
Patent Number: 11236085
Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

Therapeutic heterocyclic compounds

Granted: January 25, 2022
Patent Number: 11229638
Compounds having the following Formula I and/or Formula II and methods of their use and preparation are disclosed:

FXR (NR1H4) modulating compounds

Granted: January 18, 2022
Patent Number: 11225473
The present disclosure relates generally to compounds that bind to 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.

Compounds for inhibition of alpha 4 beta 7 integrin

Granted: January 18, 2022
Patent Number: 11224600
The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Substituted pyrido[1,2-a]pyrrolo[1,2-d]pyrazines for treating viral infections

Granted: January 4, 2022
Patent Number: 11213523
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.

Substituted 6-azabenzimidazole compounds

Granted: December 21, 2021
Patent Number: 11203591
The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

Crystalline forms of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide

Granted: December 21, 2021
Patent Number: 11202780
The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium…

Therapeutic heterocyclic compounds

Granted: November 30, 2021
Patent Number: 11186579
Compounds having the following Formula (I), or a pharmaceutically acceptable salt or pharmaceutically acceptable tautomer thereof, and methods of their use and preparation are disclosed:

Imidazopyrimidine derivatives

Granted: November 23, 2021
Patent Number: 11179397
The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating cancers.