Nucleic acid ligands to integrins
Granted: October 17, 2002
Application Number:
20020150536
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.
Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
Granted: August 29, 2002
Application Number:
20020119443
A novel method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. This method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) 1
Transcription-free SELEX
Granted: August 1, 2002
Application Number:
20020102599
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.
Nucleoside modifications by palladium catalyzed methods
Granted: August 1, 2002
Application Number:
20020103367
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.
Preparation of cyclohexene carboxylate derivatives
Granted: May 16, 2002
Application Number:
20020058823
The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
2'-FLUOROPYRIMIDINE ANTI-CALF INTESTINAL PHOSPHATASE NUCLEIC ACID LIGANDS
Granted: May 9, 2002
Application Number:
20020055113
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.
Nucleotide analog compositions
Granted: April 18, 2002
Application Number:
20020045599
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.
Method for treatment of tumors using nucleic acid ligands to PDGF
Granted: March 21, 2002
Application Number:
20020034506
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…
Liposomal benzoquinazolne thymidylate synthase inhibitor formulations
Granted: March 21, 2002
Application Number:
20020034538
Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to the free drug. The formulations include liposomes comprising at least one phosphatidylcholine, a cholesterol, and a benzoquinazoline thymidylate synthase inhibitor.
Homogeneous detection of a target through nucleic acid ligand-ligand beacon interaction
Granted: December 27, 2001
Application Number:
20010055773
A homogeneous assay that utilizes molecular beacons as the reporter and nucleic acid ligands as the sensor is described. This assay, called the ligand beacon assay, is for the detection of target molecules in a test mixture. The concept of the ligand beacon assay was tested using several proteins to which high affinity and specific nucleic acid ligands are available. The assay specifically detects the molecular target that binds the nucleic acid ligand with high affinity and specificity.…
Method for preparing camptothecin derivatives
Granted: December 13, 2001
Application Number:
20010051724
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, 1
Nucleotide analogs
Granted: November 15, 2001
Application Number:
20010041794
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.
