Quinoline derivatives as bromodomain inhibitors
Granted: August 18, 2015
Patent Number:
9108953
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 R1, R2, R3, R4, R7, W, X, and Z are as described herein.
Naphth-2-ylacetic acid derivatives to treat AIDS
Granted: August 11, 2015
Patent Number:
9102614
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).
Therapeutic compounds
Granted: August 4, 2015
Patent Number:
9096586
Compounds of formula I?: or salts thereof are provided. 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 are also provided.
Macrocyclic inhibitors of flaviviridae viruses
Granted: July 28, 2015
Patent Number:
9090653
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 virus infections, particularly hepatitis C infections.
Methods for the preparation of diasteromerically pure phosphoramidate prodrugs
Granted: July 28, 2015
Patent Number:
9090642
Provided are methods and intermediates for preparing diastereomerically pure phosphoramidate prodrugs of nucleosides of Formulas Ia and Ib: The compounds of Formula Ia and Ib are useful for the treatment Hepatitis C infections.
Process for preparing an A2A-adenosine receptor agonist and its polymorphs
Granted: July 21, 2015
Patent Number:
9085601
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.
Fused heterocyclic compounds as ion channel modulators
Granted: July 14, 2015
Patent Number:
9079901
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.
Antiviral compounds
Granted: July 14, 2015
Patent Number:
9079887
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.
Apoptosis signal-regulating kinase inhibitors
Granted: June 30, 2015
Patent Number:
9067933
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the…
Macrocyclic inhibitors of viruses
Granted: June 23, 2015
Patent Number:
9062092
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 virus infections, particularly hepatitis C infections.
Method of treating atrial fibrillation
Granted: June 16, 2015
Patent Number:
9056108
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…
Therapeutic compounds
Granted: June 9, 2015
Patent Number:
9050344
Compounds of formula I: or pharmaceutically acceptable 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 including an infection caused by the HIV virus.
N-pyrazole Areceptor agonists
Granted: June 2, 2015
Patent Number:
9045519
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 compound to stimulate mammalian coronary vasodilatation for imaging the heart.
Synthesis of an antiviral compound
Granted: June 2, 2015
Patent Number:
9045462
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.
Substituted heterocyclic compounds
Granted: June 2, 2015
Patent Number:
9045428
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.
Methods for preparing anti-viral nucleotide analogs
Granted: May 12, 2015
Patent Number:
9029534
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.
Pyridine derivatives useful as kinase inhibitors
Granted: May 12, 2015
Patent Number:
9029386
Derivatives of pyridine of the formula wherein one of Y and A is CR and the other is N are kinase inhibitors useful in treating conditions associated with excess kinase activity.
Unitary pharmaceutical dosage form
Granted: April 28, 2015
Patent Number:
9018192
In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.
Therapeutic compounds
Granted: April 21, 2015
Patent Number:
9012441
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 including an infection caused by the HIV virus.
Benzothiazole compounds and their pharmaceutical use
Granted: April 14, 2015
Patent Number:
9006229
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.
