Process and intermediates for preparing integrase inhibitors
Granted: August 5, 2014
Patent Number:
8796459
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
Viral inhibitors
Granted: July 15, 2014
Patent Number:
8779141
The present invention relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula:
Inhibitors of flaviviridae viruses
Granted: July 1, 2014
Patent Number:
8765722
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 Flaviviridae virus infections, particularly hepatitis C infections.
Synthesis of an antiviral compound
Granted: June 24, 2014
Patent Number:
8759544
The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
Inhibitors of cytochrome P450
Granted: June 24, 2014
Patent Number:
8759379
The present application provides for a compound of Formula I, 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.
Fused heterocyclic compounds as ion channel modulators
Granted: June 17, 2014
Patent Number:
8754103
The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Method of treating atrial fibrillation
Granted: June 17, 2014
Patent Number:
8754087
The present invention relates to a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising coadministration of a synergistically therapeutic amount of dronedarone or a pharmaceutically acceptable salt or salts thereof and a synergistically therapeutic amount of ranolazine or a pharmaceutically acceptable salt or salts thereof. Also provided are methods for modulating ventricular and atrial rhythm and rate. This invention also relates to…
Tenofovir alafenamide hemifumarate
Granted: June 17, 2014
Patent Number:
8754065
A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
Inhibitors of flaviviridae viruses
Granted: June 3, 2014
Patent Number:
8741946
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 Flaviviridae virus infections (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.
Apoptosis signal-regulating kinase inhibitor
Granted: June 3, 2014
Patent Number:
8742126
The present invention relates to a compound of formula (I): The compound has 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.
Pyrido(3,2-d)pyrimidines useful for treating viral infections
Granted: May 20, 2014
Patent Number:
8729089
Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.
Viral inhibitors
Granted: May 13, 2014
Patent Number:
8722677
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.
Substituted heterocyclic compounds
Granted: May 6, 2014
Patent Number:
8716319
The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
Compositions and methods for combination antiviral therapy
Granted: May 6, 2014
Patent Number:
8716264
The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants…
Inhibitors of human immunodeficiency virus replication
Granted: April 29, 2014
Patent Number:
8710230
Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
Fused heterocyclic compounds as ion channel modulators
Granted: April 22, 2014
Patent Number:
8703759
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Fused heterocyclic compounds as ion channel modulators
Granted: April 15, 2014
Patent Number:
8697863
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Antiviral compounds
Granted: April 15, 2014
Patent Number:
8697861
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.
Tenofovir alafenamide hemifumarate
Granted: April 15, 2014
Patent Number:
8697675
A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
4,6-di- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections
Granted: March 18, 2014
Patent Number:
8673929
This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl,…
