Gilead Sciences Patent Grants

Phosphatidylinositol 3-kinase inhibitors

Granted: February 26, 2019
Patent Number: 10214519
The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R1, R2, R3, R4, R5, R6 and R7 are as described herein.

Quinazoline compounds

Granted: February 19, 2019
Patent Number: 10206926
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.

Solid forms of a toll-like receptor modulator

Granted: February 12, 2019
Patent Number: 10202384
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.

Therapeutic compounds

Granted: February 12, 2019
Patent Number: 10202353
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, in particular infection caused by the HIV virus.

Processes and intermediates for preparing anti-HIV agents

Granted: February 5, 2019
Patent Number: 10196419
The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.

Inhibitors of histone demethylases

Granted: January 29, 2019
Patent Number: 10189787
The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form

Thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-D]pyrimidines useful for treating respiratory syncitial virus infections

Granted: January 15, 2019
Patent Number: 10179794
Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds.

Compounds and methods for antiviral treatment

Granted: January 8, 2019
Patent Number: 10174038
Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Modulators of toll-like receptors

Granted: January 8, 2019
Patent Number: 10172860
Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Co-crystals, salts and solid forms of tenofovir alafenamide

Granted: December 18, 2018
Patent Number: 10155781
The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds.

Substituted pteridines useful for the treatment and prevention of viral infections

Granted: December 4, 2018
Patent Number: 10144736
The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

SYK inhibitors

Granted: October 30, 2018
Patent Number: 10111882
The application provides methods of treating or reducing thrombocytopenia, leukopenia, anemia, or neutropenia in a patient in need thereof, comprising the step of administering an effective amount of a compound selected from Compounds 1-6, disclosed herein.

Fused heterocyclic compounds as CaM kinase inhibitors

Granted: October 16, 2018
Patent Number: 10100058
The present disclosure relates to compounds that are CaM Kinase inhibitors and to their use in the treatment of various disease states, including atrial fibrillation and myocardial infarction. In particular embodiments, the general structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, R5, R6, R9 and R10 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Compounds for the treatment of hepatitis B virus infection

Granted: October 16, 2018
Patent Number: 10100052
The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

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: October 16, 2018
Patent Number: 10098886
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…

Phosphatidylinositol 3-kinase inhibitors

Granted: October 9, 2018
Patent Number: 10092563
The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A?, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or…

Combination methods for treating cancers

Granted: September 25, 2018
Patent Number: 10080756
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…

Tank-binding kinase inhibitor compounds

Granted: September 11, 2018
Patent Number: 10072001
Compounds having the following formula (I) and methods of their use and preparation are disclosed:

Therapeutic compounds

Granted: September 11, 2018
Patent Number: 10071985
The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

Methods and compounds for treating Paramyxoviridae virus infections

Granted: September 4, 2018
Patent Number: 10065958
Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.