Gilead Sciences Patent Applications

Non nucleoside reverse transcriptase inhibitors

Granted: June 15, 2006
Application Number: 20060128692
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.

Tenascin-C nucleic acid ligands

Granted: May 18, 2006
Application Number: 20060105378
Methods are described for the identification and preparation of nucleic acid ligands to tenascin-C. Included in the invention are specific RNA ligands to tenascin-C identified by the SELEX method. Further included in the invention are methods for detecting the presence of a disease condition in a biological tissue in which tenascin-C is expressed.

Systematic evolution of ligands by exponential enrichment: Chemi-SELEX

Granted: April 27, 2006
Application Number: 20060088877
This application provides methods for identifying nucleic acid ligands capable of covalently interacting with targets of interest. The nucleic acids can be associated with various functional units. The method also allows for the identification of nucleic acids that have facilitating activities as measured by their ability to facilitate formation of a covalent bond between the nucleic acid, including its associated functional unit, and its target.

High affinity TGFbeta nucleic acid ligands and inhibitors

Granted: April 20, 2006
Application Number: 20060084797
Methods are described for the identification and preparation of high-affinity nucleic acid ligands to TGF?2. Included in the invention are specific RNA ligands to TGF?2 identified by the SELEX method. Also included are RNA ligands that inhibit the interaction of TGF?2 with its receptor.

High affinity nucleic acid ligands of complement system proteins

Granted: April 13, 2006
Application Number: 20060079477
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.

Nucleic acid ligands to the prostate specific membrane antigen

Granted: July 21, 2005
Application Number: 20050158780
Methods are provided for generating nucleic acid ligands of Prostate Specific Membrane Antigen (PSMA). The methods of the invention use the SELEX method for the isolation of nucleic acid ligands. The invention also includes nucleic acid ligands to PSMA, and methods and compositions for the treatment and diagnosis of disease using the nucleic acid ligands.

Platelet derived growth factor (PDGF) nucleic acid ligand complexes

Granted: February 24, 2005
Application Number: 20050042273
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,…

High affinity RNA ligands of basic fibroblast growth factor

Granted: February 24, 2005
Application Number: 20050043265
Methods are described for the identification and preparation of nucleic acid ligand solutions to basic fibroblast growth factor (bFGF). Included in the invention are nucleic acid ligands to bFGF which are inhibitors of bFGF and 2?-amino-modified RNA ligands to bFGF.

Methods of producing nucleic acid ligands

Granted: December 2, 2004
Application Number: 20040241731
The present invention includes methods for the identification and production of improved nucleic acid ligands based on the SELEX process. Also included are nucleic acid ligands to the HIV-RT protein identified according to the methods described therein.

High affinity vascular endothelial growth factor(VEGF) receptor nucleic acid ligands and inhibitors

Granted: November 11, 2004
Application Number: 20040224915
Methods are described for the identification and preparation of high-affinity nucleic acid ligands to a VEGF receptor. Included in the invention are specific RNA ligands to a VEGF receptor identified by the SELEX method. Also included are RNA ligands that inhibit the interaction of a VEGF receptor with VEGF.

Compositions and methods for combination antiviral therapy

Granted: November 11, 2004
Application Number: 20040224917
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…

Compositions and methods for combination antiviral therapy

Granted: November 11, 2004
Application Number: 20040224916
The present invention relates to therapeutic combinations of [9-[R-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl]methoxy]propyl]adenine (GS-7340) and (2R,5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, (−)-cis FTC, Emtriva™) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections,…

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

Granted: November 11, 2004
Application Number: 20040224335
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…

Novel polypeptides and coagulation therapy

Granted: October 28, 2004
Application Number: 20040214280
Novel polypeptides (NPs) are provided which are capable of protein C activation without significant fibrinogen clotting activity, and vice versa. NPs having enhanced protein C activating properties in relation to fibrinogen clotting are useful in particular as anticoagulants and in screening for substances that agonize or antagonize this property and in diagnostic procedures to determine the status of patients' activated protein C-mediated anticoagulant pathway. Procoagulant NPs are…

HBV mutations associated with reduced susceptibility to adefovir

Granted: September 30, 2004
Application Number: 20040191763
Applicants have identified 5 mutants associated with hepatitis B virus resistance to adefovir, a nucleotide analogue antiviral drug widely employed in the therapy of hepatitis B. In accord with this invention, reverse transcriptase mutants rtN236T, rtA181V, rtA181T and their corresponding surface antigen mutants sL173F and sL172trunc are provided. The mutant proteins, antibodies thereto and nucleic acids encoding the mutants have diagnostic value in monitoring and adjusting patient…

Vascular endothelial growth factor (VEGF) nucleic acid ligand complexes

Granted: September 30, 2004
Application Number: 20040192632
This invention discloses a method for preparing a complex comprised of a VEGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a VEGF Nucleic Acid Ligand by SELEX methodology and associating the VEGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further discloses Complexes comprising one or more VEGF Nucleic Acid Ligands in association with a Non-Immunogenic,…

HBV mutations associated with reduced susceptibility to adefovir

Granted: September 30, 2004
Application Number: 20040194155
Applicants have identified 5 mutants associated with hepatitis B virus resistance to adefovir, a nucleotide analogue antiviral drug widely employed in the therapy of hepatitis B. In accord with this invention, reverse transcriptase mutants rtN236T, rtA181V, rtA181T and their corresponding surface antigen mutants sL173F and sL172trunc are provided. The mutant proteins, antibodies thereto and nucleic acids encoding the mutants have diagnostic value in monitoring and adjusting patient…

Amphotericin B liposome preparation

Granted: September 9, 2004
Application Number: 20040175417
A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble…

Pre-organized tricyclic integrase inhibitor compounds

Granted: August 26, 2004
Application Number: 20040167124
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. 1

Pre-organized tricyclic integrase inhibitor compounds

Granted: August 12, 2004
Application Number: 20040157804
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. 1