Gilead Sciences Patent Applications

Antiviral compounds

Granted: February 19, 2009
Application Number: 20090047252
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.

COMPOSITIONS AND METHODS FOR COMBINATION ANTIVIRAL THERAPY

Granted: February 5, 2009
Application Number: 20090036408
The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants…

Crystalline pyridazine compound

Granted: February 5, 2009
Application Number: 20090036460
A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.

Cicletanine and PKC inhibitors in the treatment of pulmonary and cardiac disorders

Granted: December 18, 2008
Application Number: 20080312241
Embodiments of the present invention are related to novel therapeutic drugs, drug combinations, and associated methods for treating or preventing pulmonary disease, including pulmonary hypertension, pulmonary fibrosis, asthma and COPD, and heart failure, together with other pulmonary and cardiovascular diseases and their complications. More particularly, aspects of the present invention are related to the use of cicletanine and ruboxistaurin as monotherapies or in combination with other…

Delivering Iron to an Animal

Granted: September 4, 2008
Application Number: 20080213345
The invention provides a method for delivery iron to an animal. This invention further provides a method for treating iron deficiency in an animal.

Platelet Derived Growth Factor (PDGF) Nucleic Acid Ligand Complexes

Granted: August 28, 2008
Application Number: 20080207883
This invention discloses a method for preparing a complex comprised of a PDGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a PDGF Nucleic Acid Ligand by SELEX methodology and associating the PDGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further discloses Complexes comprising one or more PDGF Nucleic Acid Ligands in association with a Non-Immunogenic,…

PYRIDO(3,2-d)PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS

Granted: July 31, 2008
Application Number: 20080182870
Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.

Phosphonate Derivatives of Mycophenolic Acid

Granted: July 17, 2008
Application Number: 20080171724
Phosphorus substituted mycophenolate oxime derivatives with anti-cancer, anti-viral, anti-inflammatory anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as…

Pyrimidyl Phosphonate Antiviral Compounds and Methods of Use

Granted: June 26, 2008
Application Number: 20080153783
Pyrimidine I and pyrimidinone II phosphonate compounds and methods for viral inhibition are disclosed. The compounds include at least one phosphonate group covalently attached at any site.

PROCESS AND INTERMEDIATES FOR PREPARING INTEGRASE INHIBITORS

Granted: May 29, 2008
Application Number: 20080125594
The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

Antiviral phosphinate compounds

Granted: March 6, 2008
Application Number: 20080057031
The invention is related to anti-viral phosphinate 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.

Topical Antiviral Formulations

Granted: February 14, 2008
Application Number: 20080035155
The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (N(t)RTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

Use of Adefovir or Tenofovir for Inhibiting Mmtv-Like Viruses Involved in Breast Cancer and Primary Biliary Cirrhosis

Granted: December 6, 2007
Application Number: 20070281911
The active metabolites of adefovir and tenofovir (PMEApp and PMPApp) are active against the MMTV RT. They are 25-fold more potent than 3TCppp, suggesting that tenofovir and adefovir may be effective at inhibiting the MMTV-like retroviruses, which may be the etiological agents involved in PBC and breast cancer.

Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases

Granted: November 29, 2007
Application Number: 20070276050
This invention is directed to methods for identifying apoptosis signal-regulated kinase 1 (“ASK1”) inhibitors useful for preventing and/or treating cardiovascular disease. This invention also relates to methods for preventing and/or treating cardiovascular disease in an animal by administering to the animal an ASK1 inhibitor.

SYSTEMATIC EVOLUTION OF LIGANDS BY EXPONENTIAL ENRICHMENT: BLENDED SELEX

Granted: June 14, 2007
Application Number: 20070134715
A method is described for generating blended nucleic acid ligands containing non-nucleic acid functional units. Specifically, a SELEX identified RNA ligand to the integrin gpIIbIIIa is conjugated to the peptide Gly-Arg-Gly-Asp-Thr-Pro (SEQ ID NO:1). This blended RNA ligand inhibits the biological activity of gpIIbIIIa with high specificity. Also described is a single-stranded DNA ligand to elastase coupled to N-methoxysuccinyl-Ala-Ala-Pro-Val-chloromethyl ketone (SEQ ID NO:2). This…

Methods and compositions for treatment of tumors using nucleic acid ligands to platelet-derived growth factor

Granted: January 25, 2007
Application Number: 20070021327
A method is provided for treating solid tumors comprising administering a composition comprising a PDGF aptamer and a cytotoxic agent. In a preferred embodiment the PDGF aptamer is identified using the SELEX process for the Systematic Evolution of Ligands by Exponential enrichment. A method is also provided for reducing the interstitial fluid pressure (IFP) of a solid tumor comprising administering a PDGF aptamer. Finally, a method is provided for increasing the uptake of cytotoxic…

Nucleic acid ligands to integrins

Granted: January 11, 2007
Application Number: 20070010473
Methods are described for the isolation of nucleic acid ligands to integrins using the SELEX process. SELEX is an acronym for Systematic Evolution of Ligands by EXponential enrichment. The nucleic acid ligands of the present invention are useful as therapeutic and diagnostic agents.

High affinity oligonucleotide ligands to growth factors

Granted: October 12, 2006
Application Number: 20060229273
Methods are described for the identification and preparation of high-affinity nucleic acid ligands to TGF?, PDGF and hKGF. Included in the invention are specific RNA and ssDNA ligands to TGF?1 and PDGF identified by the SELEX method. Also included in the invention are specific RNA ligands to hKGF identified by the SELEX method. Further included are RNA ligands that inhibit the interaction of TGF?1 and hKGF with their receptors and DNA ligands that inhibit the interaction of PDGF with its…

Bivalent binding molecules of 7 transmembrane G protein-coupled receptors

Granted: July 6, 2006
Application Number: 20060147987
Described herein are methods for identifying and preparing bivalent binding molecules to 7 transmembrane G protein-coupled receptors. The methods disclosed herein are based on the SELEX method for generating high affinity nucleic acid ligands. SELEX is an acronym for Systematic Evolution of Ligands by EXponential enrichment. The methods of this invention combine two or more binding domains to two or more different epitopes of the same 7 transmembrane G protein-coupled receptor. These…

Nucleic acid ligands which bind to hepatocyte growth factor/scatter factor (HGF/SF) or its receptor c-met

Granted: July 6, 2006
Application Number: 20060148748
The invention provides nucleic acid ligands to hepatocyte growth factor/scatter factor (HGF) and its receptor c-met. The nucleic acid ligands of the instant invention are isolated using the SELEX method. SELEX is an acronym for Systematic Evolution of Ligands by EXponential enrichment. The nucleic acid ligands of the invention are useful as diagnostic and therapeutic agents for diseases in which elevated HGF and c-met activity are causative factors.