Non-homogeneous systems for the resolution of enantiomeric mixtures
Granted: February 9, 2010
Patent Number:
7659106
The present invention relates to a process for the biocatalyst-mediated enantioselective conversion of enantiomeric mixtures of hydrophobic esters using a biphasic solvent system. More particularly, the present invention relates to the enzyme-mediated enantioselective synthesis of anti-viral compounds, such as 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC) and its analogues, in a non-homogenous reaction system.
Imidazo 4,5-c pyridine compounds and methods of antiviral treatment
Granted: January 19, 2010
Patent Number:
7648998
The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening ofcompounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral…
Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds
Granted: January 19, 2010
Patent Number:
7649015
Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
Therapeutic phosphonate compounds
Granted: January 12, 2010
Patent Number:
7645747
The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.
Antiviral compounds
Granted: January 5, 2010
Patent Number:
7642339
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.
Isolated hOAT polynucleotide
Granted: September 15, 2009
Patent Number:
7589186
This invention is concerned with human organic anion transporter (“hOAT”). Isolated nucleic acid encoding hOAT is provided, along with isolated hOAT polypeptide. hOAT nucleic acid and/or hOAT polypeptide are employed in transgenic animals, recombinant cells, replicable vectors and analytical procedures for identifying hOAT agonists or antagonists, assays for identifying hOAT alleles and/or isotypes, screening tests for nephrotoxic or neurologically active compounds, and determination…
Nucleobase phosphonate analogs for antiviral treatment
Granted: August 25, 2009
Patent Number:
7579332
The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the virus. The compounds of the invention may be useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-l or HIV-2) or human T-cell leukemia virus (HTLV-1 or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or…
ABCA1 elevating compounds
Granted: August 25, 2009
Patent Number:
7579504
The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
Combination therapy to treat hepatitis B virus
Granted: August 11, 2009
Patent Number:
7572800
The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a…
Substituted heterocyclic compounds
Granted: July 28, 2009
Patent Number:
7566717
Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.
Anti-proliferative compounds, compositions, and methods of use thereof
Granted: June 30, 2009
Patent Number:
7553825
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)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted…
Polymorphic and other crystalline forms of cis-FTC
Granted: June 9, 2009
Patent Number:
7544692
Solid phases of (?)-cis-FTC, which are designated herein as amorphous (?)-FTC and Forms II and III (?)-cis-FTC) are provided that can be distinguished from Form I (?)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal…
1,4-dihydropyridine compounds, pharmaceutical compositions, and methods for the treatment of cardiovascular disease
Granted: February 3, 2009
Patent Number:
7485653
The present invention provides certain substituted 1,4-dihydropyridine compounds, including pure enantiomeric forms and pharmaceutical formulations thereof. These compounds provide for elevation of ?-MyHC protein levels and ?-MyHC mRNA levels, and most frequently these same compounds provide simultaneous lowering of ?-MyHC protein levels and ?-MyHC mRNA levels. Thus, these compounds may be used alone or in conjunction with other drugs to treat heart failure.
Phosphonate compounds having immuno-modulatory activity
Granted: December 30, 2008
Patent Number:
7470724
The invention is related to phosphonate substituted compounds having immuno-modulatory 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.
Non nucleoside reverse transcriptase inhibitors
Granted: December 9, 2008
Patent Number:
7462608
Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.
Aza-quinolinol phosphonate integrase inhibitor compounds
Granted: December 9, 2008
Patent Number:
7462721
Aza-quinolinol phosphonate compounds and methods for inhibition of HIV-integrase are disclosed. Ar is aryl or heteroaryl connecting R6 to L. L is a bond or a linker connecting a ring atom of Ar to N. The ring atoms, X1-X5 may be N, substituted nitrogen, or substituted carbon, and form rings. The compounds include at least one phosphonate group covalently attached at any site.
Targeted delivery of lidocaine and other local anesthetics and a method for treatment of cough and tussive attacks
Granted: November 18, 2008
Patent Number:
7452523
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.
Method for improvement of tolerance for therapeutically effective agents delivered by inhalation
Granted: November 18, 2008
Patent Number:
7452524
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…
Anti-cancer phosphonate analogs
Granted: November 18, 2008
Patent Number:
7452901
The invention is related to phosphorus substituted anti-cancer 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.
Nucleotide analogs
Granted: October 21, 2008
Patent Number:
7439350
Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
