Gilead Sciences Patent Grants

Aerosolized fosfomycin/aminoglycoside combination for the treatment of bacterial respiratory infections

Granted: January 29, 2013
Patent Number: 8361444
A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation…

Inhibitors of human immunodeficiency virus replication

Granted: January 15, 2013
Patent Number: 8354429
Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Oxindolyl inhibitor compounds

Granted: January 1, 2013
Patent Number: 8344018
A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. (Formula should be inserted here) Formula (I)

Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections

Granted: December 25, 2012
Patent Number: 8338435
This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C.

Inhibitors of human immunodeficiency virus replication

Granted: December 25, 2012
Patent Number: 8338441
Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Modulators of toll-like receptor 7

Granted: December 25, 2012
Patent Number: 8338593
The present application provides for a compound of Formula (I) or (II): 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 that include the administration of such compounds with at least one additional active agent.

Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment

Granted: December 11, 2012
Patent Number: 8329727
The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral…

Antiviral compounds

Granted: December 11, 2012
Patent Number: 8329926
The invention is related to phosphorus substituted anti-viral inhibitory 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 and intermediates for preparing integrase inhibitors

Granted: December 4, 2012
Patent Number: 8324244
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Aadenosine receptor antagonists

Granted: December 4, 2012
Patent Number: 8324224
Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Nucleoside analogs for antiviral treatment

Granted: December 4, 2012
Patent Number: 8324179
The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically acceptable salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).

1?substituted carba-nucleoside analogs for antiviral treatment

Granted: November 27, 2012
Patent Number: 8318682
Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 1? position of the nucleoside sugar is substituted with a cyano group. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Phosphonate analogs of HIV inhibitor compounds

Granted: November 27, 2012
Patent Number: 8318701
The invention is related to phosphorus substituted anti-viral inhibitory 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.

Method of treating diabetes

Granted: November 20, 2012
Patent Number: 8314104
Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.

Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds

Granted: October 9, 2012
Patent Number: 8283357
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Antiviral compounds

Granted: October 9, 2012
Patent Number: 8283442
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.

N-pyrazole A2A receptor agonists

Granted: October 2, 2012
Patent Number: 8278435
The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart.

Antiviral compounds

Granted: September 25, 2012
Patent Number: 8273341
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.

Anti-proliferative compounds, compositions, and methods of use thereof

Granted: September 18, 2012
Patent Number: 8268802
Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ?O, —O(RX), ?S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with…

Process for preparing an A2A-adenosine receptor agonist and its polymorphs

Granted: September 18, 2012
Patent Number: 8268988
Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.