Process for preparing an A-adenosine receptor agonist and its polymorphs
Granted: January 31, 2012
Patent Number:
8106183
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.
Antiviral compounds
Granted: January 3, 2012
Patent Number:
8088368
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.
Anti-proliferative compounds, compositions, and methods of use thereof
Granted: January 3, 2012
Patent Number:
8088754
Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ?O, —O(RX), ?S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); and pharmaceutically acceptable salts thereof.
Modulators of pharmacokinetic properties of therapeutics
Granted: January 3, 2012
Patent Number:
8088770
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.
Cycloalkylidene and heterocycloalkylidene inhibitor compounds
Granted: January 3, 2012
Patent Number:
8088771
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.
Triazolopyridinone derivatives for use as stearoyl CoA desaturase inhibitors
Granted: January 3, 2012
Patent Number:
8088792
The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: 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, metabolic syndrome and the like.
Methods of coronary imaging
Granted: December 6, 2011
Patent Number:
8071566
The present invention provides methods of myocardial perfusion imaging and increasing coronary blood flow of a mammal that are accomplished by administering doses of a compound that is a selective partial A2A receptor agonist with a short duration of action, in particular regadenoson, useful for, among other indications, myocardial imaging and coronary vasodilation, and determining areas of insufficient blood flow.
Modulators of pharmacokinetic properties of therapeutics
Granted: November 29, 2011
Patent Number:
8067449
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.
Antiviral phosphonate analogs
Granted: September 20, 2011
Patent Number:
8022083
The invention is related to phosphorus substituted compounds with antiviral activity, 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.
Carba-nucleoside analogs for antiviral treatment
Granted: September 6, 2011
Patent Number:
8012942
Provided are thieno[3,4-d]pyrimidin-7-yl and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.
Carba-nucleoside analogs for antiviral treatment
Granted: September 6, 2011
Patent Number:
8012941
Provided are imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
1?-substituted carba-nucleoside analogs for antiviral treatment
Granted: August 30, 2011
Patent Number:
8008264
Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
Integrase inhibitors
Granted: August 30, 2011
Patent Number:
8008287
Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
Method for improvement of tolerance for therapeutically effective agents delivered by inhalation
Granted: August 23, 2011
Patent Number:
8003081
A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such…
Targeted delivery of lidocaine and other local anesthetics and a method for treatment of cough, asthma and tussive attacks
Granted: August 16, 2011
Patent Number:
7998463
An anti-tussive nebulized solution for targeted delivery of lidocaine into conducting and central airways. A method for treatment of cough and tussive attacks or episodes using said lidocaine solution. A nebulized lidocaine solution administered in daily dose from about 10 mg to 80 mg of lidocaine dissolved in a saline and nebulized into an aerosol having a mass median aerodynamic diameter 3 ?m to 10 ?m and a geometric standard deviation less than 1.7 using an electronic nebulizer.
Antiviral compounds
Granted: August 16, 2011
Patent Number:
7998950
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.
2'-fluoro substituted carba-nucleoside analogs for antiviral treatment
Granted: July 5, 2011
Patent Number:
7973013
Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-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 substitutents. 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…
Inhaled aztreonam lysine for the treatment of deficits in health-related quality-of-life in lung diseases
Granted: July 5, 2011
Patent Number:
7973029
Provided is a method of treating the health-related quality-of-life (HRQOL) symptoms of a lung disease, comprising the administration of an inhalable aerosol of aztreonam lysine. The method is suitable for the short term and sustainable long term treatment of HRQOL symptoms.
Modulators of toll-like receptor 7
Granted: June 28, 2011
Patent Number:
7968544
The present application includes a compound of Formula I or II: 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 that include the administration of such compounds with at least one additional active agent.
High affinity nucleic acid ligands of complement system proteins
Granted: June 21, 2011
Patent Number:
7964572
Methods are described for the identification and preparation of high-affinity Nucleic Acid Ligands to Complement System Proteins. Methods are described for the identification and preparation of high affinity Nucleic Acid Ligands to Complement System Proteins C1q, C3 and C5. Included in the invention are specific RNA ligands to C1q, C3 and C5 identified by the SELEX method.
