Method of preventing and treating airway remodeling and pulmonary inflammation using Aadenosine receptor antagonists
Granted: June 18, 2013
Patent Number:
8466129
The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.
Inhibitors of human immunodeficiency virus replication
Granted: June 11, 2013
Patent Number:
8461180
Compounds of formula (I): wherein c, X, Y, R2, R4 and R5 are defined herein, are useful as inhibitors of HIV replication.
2'-fluoro substituted carba-nucleoside analogs for antiviral treatment
Granted: June 4, 2013
Patent Number:
8455451
Provided are select imidazo[1,2-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substituents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
Bi-functional pyrazolopyridine compounds
Granted: May 28, 2013
Patent Number:
8450490
This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.
Process and intermediates for preparing integrase inhibitors
Granted: May 14, 2013
Patent Number:
8440831
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
Apoptosis signal-regulating kinase inhibitors
Granted: May 14, 2013
Patent Number:
8440665
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 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, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD,…
Method and compositions for treating hematological malignancies
Granted: May 7, 2013
Patent Number:
8435969
A compound of formula 1 and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.
Process for preparation of HIV protease inhibitors
Granted: April 30, 2013
Patent Number:
8431745
A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
Alkanoylamino benzamide aniline HDAC inhibitor compounds
Granted: April 30, 2013
Patent Number:
8431610
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: April 16, 2013
Patent Number:
8420597
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.
1?-substituted-carba-nucleoside prodrugs for antiviral treatment
Granted: April 9, 2013
Patent Number:
8415308
Provided are prodrugs of pyrrolo[1,2-f][1,2,4]triazin-7-yl nucleoside phosphates wherein the 1? position of the nucleoside sugar is substituted with CN. The compounds, compositions, and methods provided are useful for the treatment Hepatitis C infections.
Aerosolized fosfomycin/aminoglycoside combination for the treatment of bacterial respiratory infections
Granted: April 2, 2013
Patent Number:
8409549
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…
Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections
Granted: March 19, 2013
Patent Number:
8399496
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…
Bi-functional quinoline analogs
Granted: March 12, 2013
Patent Number:
8394829
Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.
Fused heterocyclic compounds as ion channel modulators
Granted: March 5, 2013
Patent Number:
8389500
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 (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
Modulators of pharmacokinetic properties of therapeutics
Granted: February 26, 2013
Patent Number:
8383655
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.
Apoptosis signal-regulating kinase inhibitors
Granted: February 19, 2013
Patent Number:
8378108
The present invention relates to compounds of Formula (I): where in 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…
Inhibitors of human immunodeficiency virus replication
Granted: February 19, 2013
Patent Number:
8377960
Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
Bi-functional pyrazolopyridine compounds
Granted: February 5, 2013
Patent Number:
8367829
This invention provides compounds of the formula: wherein X is wherein R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.
Modulators of toll-like receptors
Granted: February 5, 2013
Patent Number:
8367670
Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
