Methods and compositions for treatment of tumors using nucleic acid ligands to platelet-derived growth factor
Granted: November 28, 2006
Patent Number:
7141375
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: August 22, 2006
Patent Number:
7094535
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.
Bivalent binding molecules of 7 transmembrane G protein-coupled receptors
Granted: August 8, 2006
Patent Number:
7087735
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…
Isolated hOAT polypeptide
Granted: July 4, 2006
Patent Number:
7071305
This invention is concerned with human organic anion transporter (“hOAT”). Isolated nucleic acid encoding hOAT is provided, along with ioslated 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…
Polypeptides and coagulation therapy
Granted: June 13, 2006
Patent Number:
7060484
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…
Tenascin-C nucleic acid ligands
Granted: February 28, 2006
Patent Number:
7005260
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.
Non-homogeneous systems for the resolution of enantiomeric mixtures
Granted: December 27, 2005
Patent Number:
6979561
The present invention relates to a process for the biocatalyst-mediated enantioselective conversion of enantiomeric mixtures of hydrophobic esters uing 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-flurocytosin-1-yl)-1,3-oxathiolane (FTC) and its analogues, in a non-homogenous reaction system.
Vascular endothelial growth factor (VEGF) nucleic acid ligand complexes
Granted: November 8, 2005
Patent Number:
6962784
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,…
Process of manufacture of 1,3-oxathiolane nucleosides using titanium trichloride mono-isopropoxide
Granted: September 6, 2005
Patent Number:
6939965
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.
Nucleic acid ligand binding site identification
Granted: August 23, 2005
Patent Number:
6933116
This invention comprises nucleic acid ligand for use as a diagnostic reagent for detecting the presence or absence of a target molecule in a sample, and a diagnostic reagent to measure the amount of a target molecule in a sample. In a preferred embodiment the nucleic acid ligands are identified by the method of the invention referred to as the Systematic Evolution of Ligands by EXponential enrichment (SELEX), wherein a candidate mixture of nucleic acids are iteratively enriched in high…
Nucleic acid ligands to the prostate specific membrane antigen
Granted: August 23, 2005
Patent Number:
6933114
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.
Urea nucleosides as therapeutic and diagnostic agents
Granted: July 5, 2005
Patent Number:
6914138
Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the…
Truncation SELEX method
Granted: February 15, 2005
Patent Number:
6855496
This invention is directed to a method for identifying nucleic acid ligands by the SELEX method wherein the participation of fixed sequences is eliminated or minimized.
Nucleoside modifications by palladium catalyzed methods
Granted: January 25, 2005
Patent Number:
6846918
This invention discloses a method for the preparation of 2?-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the novel pyrimidines and purines that can be prepared according to the method of the invention and oligonucleotides containing said modified pyrimidines and purines.
Amphotericin B liposome preparation
Granted: August 3, 2004
Patent Number:
6770290
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…
High affinity vascular endothelial growth factor (VEGF) receptor nucleic acid ligands and inhibitors
Granted: July 13, 2004
Patent Number:
6762290
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.
High affinity RNA ligands of basic fibroblast growth factor
Granted: July 6, 2004
Patent Number:
6759392
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.
Polymorphic and other crystalline forms cis-FTC
Granted: April 20, 2004
Patent Number:
6723728
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…
Methods of producing nucleic acid ligands
Granted: April 6, 2004
Patent Number:
6716583
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 TGF&bgr; nucleic acid ligands and inhibitors
Granted: March 30, 2004
Patent Number:
6713616
Methods are described for the identification and preparation of high-affinity nucleic acid ligands to TGF&bgr;2. Included in the invention are specific RNA ligands to TGF&bgr;2 identified by the SELEX method. Also included are RNA ligands that inhibit the interaction of TGF&bgr;2 with its receptor.
