Gilead Sciences Patent Grants

Viral inhibitors

Granted: September 11, 2012
Patent Number: 8263612
Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.

Alkanoylamino benzamide aniline HDAC inhibitor compounds

Granted: September 4, 2012
Patent Number: 8258316
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.

Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C

Granted: July 31, 2012
Patent Number: 8232278
Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.

Cycloalkylidene and heterocycloalkylidene inhibitor compounds

Granted: June 12, 2012
Patent Number: 8198299
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.

Method of decreasing hepatotoxic side effects using Aadenosine receptor antagonists

Granted: May 29, 2012
Patent Number: 8188099
The invention is related to a method of decreasing hepatotoxic side effects using an A2B adenosine receptor antagonist and utility in the treatment of liver damage caused by undergoing hepatotoxic treatment, such as chemotherapy or radiation. The invention also relates to pharmaceutical compositions for use in the method.

Myocardial perfusion imaging method

Granted: May 22, 2012
Patent Number: 8183226
The present disclosure provides 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 in a variety of applications including myocardial perfusion imaging and coronary vasodilation methods.

Antiviral compounds

Granted: May 15, 2012
Patent Number: 8178491
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.

Process for preparation of HIV protease inhibitors

Granted: May 8, 2012
Patent Number: 8173623
A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.

Nucleoside analogues containing phosphonate or phosphonamide groups

Granted: April 24, 2012
Patent Number: 8163718
Novel compounds having structure (1) wherein Z, is N or CH to form a purine, Y, R1, R2? and R2 are defined in the specification, are provided for use in the treatment of tumors and the prophylaxis or treatment of viral infections.

ALDH-2 inhibitors in the treatment of addiction

Granted: April 17, 2012
Patent Number: 8158810
Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

Process and intermediates for preparing integrase inhibitors

Granted: April 10, 2012
Patent Number: 8153801
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Modulators of pharmacokinetic properties of therapeutics

Granted: April 3, 2012
Patent Number: 8148374
The present application provides for a compound of Formula IV, 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 and include the administration of such compounds with at least one additional therapeutic agent.

3, 4-dihydroquinoxalin-2(1H)-ones for use as stearoyl CoA desaturase inhibitors

Granted: April 3, 2012
Patent Number: 8148376
The present invention discloses 3,4-dihydroquinoxalin-2(1H)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.

Prodrugs of Aadenosine receptor antagonists

Granted: March 27, 2012
Patent Number: 8143249
Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted phenyl; X is hydrogen or methyl; and Y is —C(O)R, in which R is optionally substituted aryl or optionally substituted heteroaryl or a pharmaceutically acceptable salt thereof, and their use in treating mammals for various disease states.

Pyrido(3,2-d)pyrimidines useful for treating viral infections

Granted: March 27, 2012
Patent Number: 8143394
2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a patient in a therapeutically effective amount.

Myocardial perfusion imaging methods and compositions

Granted: March 13, 2012
Patent Number: 8133879
The present disclosure provides 2-adenosine N-pyrazole compounds of structural formula shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds in a variety of applications including myocardial perfusion imaging methods.

Imidazolyl pyrimidine inhibitor compounds

Granted: March 13, 2012
Patent Number: 8134000
A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Fused heterocyclyc inhibitor compounds

Granted: February 28, 2012
Patent Number: 8124764
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Use of Aadenosine receptor agonists

Granted: January 31, 2012
Patent Number: 8106029
Myocardial imaging methods are provided that are accomplished by administering doses of a pharmaceutical composition comprising one or more adenosine A2A receptor agonists, in particular regadenoson, useful for, among other indications, myocardial imaging and coronary vasodilation, in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.

Crystalline pyridazine compound

Granted: January 31, 2012
Patent Number: 8106054
A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.