Nucleotide analog compositions
Granted: September 17, 2002
Patent Number:
6451340
The invention provides crystalline forms of adefovir dipivoxil and methods to prepare the crystals. The compositions and methods of the present invention have desirable properties for large scale synthesis of crystalline adefovir dipivoxil or for its formulation into therapeutic dosages. Invention compositions include an anhydrous crystal form of adefovir dipivoxil.
Urea nucleosides as therapeutic and diagnostic agents
Granted: August 27, 2002
Patent Number:
6441161
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…
Gene encoding organic anion transporter
Granted: August 13, 2002
Patent Number:
6432631
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…
Vascular endothelial growth factor (VEGF) nucleic acid ligand complexes
Granted: July 30, 2002
Patent Number:
6426335
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,…
High affinity nucleic acid ligands of complement system proteins
Granted: May 28, 2002
Patent Number:
6395888
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.
Transcription-free selex
Granted: May 14, 2002
Patent Number:
6387620
Methods are provided for the production of nucleic acid ligands against target molecules using a procedure known as Transcription-free Systematic Evolution of Ligands by EXponential enrichment (Transcription-free SELEX). The Transcription-free SELEX method assembles nucleic acid ligands from fragments of synthetic nucleic acids by annealing those fragments to a complementary template, and then ligating the fragments together.
2?-fluoropyrimidine anti-calf intestinal phosphatase nucleic acid ligands
Granted: May 14, 2002
Patent Number:
6387635
Methods are described for the identification and preparation of nucleic acid ligands to calf intestinal phosphatase. Included in the invention are specific RNA ligands to calf intestinal phosphatase identified by the SELEX method.
Systematic evolution of ligands by exponential enrichment: tissue SELEX
Granted: April 23, 2002
Patent Number:
6376474
This invention discloses high-affinity oligonucleotide ligands to complex tissue targets, specifically nucleic acid ligands having the ability to bind to complex tissue targets, and the methods for obtaining such ligands. Tissue targets comprise cells, subcellular components, aggregates or cells, collections of cells, and higher ordered structures. Specifically, nucleic acid ligands to red blood cells ghosts, endothelia of the blood brain and CSF-blood barriers, glioblastomas, and…
Piperidine compounds
Granted: April 23, 2002
Patent Number:
6376674
Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and…
Purine nucleoside modifications by palladium catalyzed methods and compounds produced
Granted: March 12, 2002
Patent Number:
6355787
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.
High affinity TGf&bgr; nucleic acid ligands and inhibitors
Granted: February 12, 2002
Patent Number:
6346611
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.
Methods of producing nucleic acid ligands
Granted: February 5, 2002
Patent Number:
6344318
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.
Nucleic acid ligands which bind to hepatocyte growth factor/scatter factor (HGF/SF) or its receptor c-met
Granted: February 5, 2002
Patent Number:
6344321
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.
Tablet
Granted: December 25, 2001
Patent Number:
D452562
Nucleic acid ligands to integrins
Granted: December 18, 2001
Patent Number:
6331394
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.
Nucleic acid ligands
Granted: December 18, 2001
Patent Number:
6331398
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…
Systematic evolution of ligands by exponential enrichment: Chemi-SELEX
Granted: October 9, 2001
Patent Number:
6300074
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.
Method for preparing camptothecin derivatives
Granted: September 4, 2001
Patent Number:
6284891
The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation,
wherein R1 to R6 represent various substituents.
High affinity nucleic acid ligands to lectins
Granted: August 28, 2001
Patent Number:
6280932
This invention discloses high-affinity oligonucleotide ligands to lectins, specifically nucleic acid ligands having the ability to bind to the lectins, wheat germ agglutinin, L-selectin and P-selectin. Also disclosed are the methods for obtaining such ligands.
2?-fluoropyrimidine anti-calf intestinal phosphatase nucleic acid ligands
Granted: August 28, 2001
Patent Number:
6280943
Methods are described for the identification and preparation of nucleic acid ligands to calf intestinal phosphatase. Included in the invention are specific RNA ligands to calf intestinal phosphatase identified by the SELEX method.
