Antiviral analogs
Granted: October 7, 2008
Patent Number:
7432272
The application relates to 4?-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such compounds, to methods and intermediates useful for preparing such compounds, and to therapeutic methods comprising administering such compounds to animals in need thereof.
Phosphonate analogs of antimetabolites
Granted: October 7, 2008
Patent Number:
7432273
The invention is related to phosphorus substituted antimetabolites, 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.
Anti-inflammatory phosphonate compounds
Granted: October 7, 2008
Patent Number:
7432261
The invention is related to phosphorus substituted anti-inflammatory 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.
Antiviral phosphonate analogs
Granted: September 30, 2008
Patent Number:
7429565
The invention is related to phosphorus substituted compounds with antiviral activity, 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.
Purine nucleoside phosphorylase inhibitory phosphonate compounds
Granted: September 23, 2008
Patent Number:
7427624
The invention is related to phosphorus substituted purine nucleoside phosphorylase inhibitory 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.
Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections
Granted: September 23, 2008
Patent Number:
7427633
A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a…
Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
Granted: September 23, 2008
Patent Number:
7427636
The invention is related to phosphorus substituted IMPDH inhibitory 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.
Kinase inhibitory phosphonate analogs
Granted: August 26, 2008
Patent Number:
7417055
The invention is related to phosphorus substituted kinase inhibitory 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.
Phosphonate analogs for treating metabolic diseases
Granted: August 5, 2008
Patent Number:
7407965
The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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.
Prodrugs of phosphonate nucleotide analogues
Granted: June 24, 2008
Patent Number:
7390791
A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided.
Methods of producing nucleic acid ligands
Granted: May 6, 2008
Patent Number:
7368236
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.
Anti-infective phosphonate analogs
Granted: November 27, 2007
Patent Number:
7300924
The invention is related to phosphorus substituted anti-infective 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.
Methods and compositions for identifying therapeutic compounds with GS-9005 ester hydrolase A
Granted: September 25, 2007
Patent Number:
7273715
By the present invention, enzymes responsible for prodrug activation are identified and utilized for the identification of candidate compounds as prodrugs. The present invention includes methods for identifying a candidate compound as a suitable prodrug as well as methods of screening candidate compounds for suitability as therapeutic agents.
Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
Granted: September 25, 2007
Patent Number:
7273716
By the present invention, enzymes responsible for prodrug activation are identified and utilized for the identification of candidate compounds as prodrugs. The present invention includes methods for identifying a candidate compound as a suitable prodrug as well as methods of screening candidate compounds for suitability as therapeutic agents.
Methods and compositions for identifying therapeutic compounds with GS-9005 ester hydrolase B
Granted: September 25, 2007
Patent Number:
7273717
By the present invention, enzymes responsible for prodrug activation are identified and utilized for the identification of candidate compounds as prodrugs. The present invention includes methods for identifying a candidate compound as a suitable prodrug as well as methods of screening candidate compounds for suitability as therapeutic agents.
Determining non-nucleic acid molecule binding to target by competition with nucleic acid ligands
Granted: August 21, 2007
Patent Number:
7258980
A competitive binding assay is used to determine whether a non-nucleic acid molecule from a library of non-nucleic acid molecules binds to a target. The non-nucleic acid molecule competes with a labeled nucleic acid ligand for binding to the target which may be immobilized. Detecting displacement of labeled nucleic acid ligand from a complex of the labeled nucleic acid ligand and the target determines binding of the non-nucleic acid molecule to the target. The nucleic acid ligand may be…
Pre-organized tricyclic integrase inhibitor compounds
Granted: August 7, 2007
Patent Number:
7253180
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties…
High affinity RNA ligands of basic fibroblast growth factor
Granted: March 27, 2007
Patent Number:
7196069
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.
Systematic evolution of ligands by exponential enrichment: blended SELEX
Granted: February 13, 2007
Patent Number:
7176295
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…
High-affinity oligonucleotide ligands to vascular endothelial growth factor (VEGF)
Granted: December 26, 2006
Patent Number:
7153948
Methods are described for the identification and preparation of nucleic acid ligand ligands to vascular endothelial growth factor (VEGF). Included in the invention are specific RNA ligands to VEGF identified by the SELEX method.
