HCV genotype 6 replicons
Granted: May 31, 2016
Patent Number:
9353423
Replicons of genotype 6 hepatitis C virus (HCV) are provided. These replicons contain adaptive mutations giving rise to the HCV's capability to replicate in vitro. Methods of preparing genotype 6 replicons and methods of using these replicons to screen antiviral agents are also provided.
Methods for preparing anti-viral nucleotide analogs
Granted: May 24, 2016
Patent Number:
9346841
Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
Methods and intermediates for preparing pharmaceutical agents
Granted: May 24, 2016
Patent Number:
9346796
Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections
Granted: May 24, 2016
Patent Number:
9345663
A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a…
Apoptosis signal-regulating kinase inhibitor
Granted: May 10, 2016
Patent Number:
9333197
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.
7-deazapurine nucleosides for therapeutic uses
Granted: April 26, 2016
Patent Number:
9321800
The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.
Inhibitors of viruses
Granted: April 26, 2016
Patent Number:
9321753
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.
Tenofovir alafenamide hemifumarate
Granted: March 29, 2016
Patent Number:
9296769
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 hepatitis C virus
Granted: March 29, 2016
Patent Number:
9296782
Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.
Processes and intermediates for preparing anti-HIV agents
Granted: March 29, 2016
Patent Number:
9296779
The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
2-quinolinyl-acetic acid derivatives as HIV antiviral compounds
Granted: March 29, 2016
Patent Number:
9296758
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides 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 the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
Granted: March 22, 2016
Patent Number:
9290505
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods…
Myocardial perfusion imaging methods and compositions
Granted: March 22, 2016
Patent Number:
9289446
A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A2a receptor agonist, at least one liquid carrier, and at least one co-solvent.
Naphthalene acetic acid derivatives against HIV infection
Granted: March 15, 2016
Patent Number:
9284323
The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
Method for treating a pulmonary hypertension condition
Granted: March 15, 2016
Patent Number:
9283223
A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
Pyrazolo[1,5-A]pyrimidines as antiviral agents
Granted: March 8, 2016
Patent Number:
9278975
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
Solid forms of an ion channel modulator
Granted: March 1, 2016
Patent Number:
9273038
Crystalline solid forms of the selective late sodium current inhibitor 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
Granted: February 16, 2016
Patent Number:
9259426
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR?R?, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single…
Apoptosis signal-regulating kinase inhibitor
Granted: February 9, 2016
Patent Number:
9254284
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.
Benzimidazolone derivatives as bromodomain inhibitors
Granted: February 9, 2016
Patent Number:
9255089
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
