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Class 536/28.1 - N-glycosides wherein the N is part of a six-membered hetero ring (e.g., diazines, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which are N-glycosides wherein the N of the N-glycoside
No. of patents: 189
Last issue date: 01/31/2012


1          
NumberTitleIssue Date
8106184Nicotinoyl riboside compositions and methods of use
The invention relates to compositions of nicotinoyl ribosides and nicotinamide riboside derivatives and their methods of use. In some embodiments, the invention relates to methods of making nicotinoyl ribosides. In some embodiments, the invention relates to pharmace...
01/31/2012
7786296Silyl linker for solid-phase synthesis of nucleic acid
The purpose of the invention is to develop a silyl linker that can be efficiently introduced on a solid-phase support used for the synthesis of nucleic acid oligomers such as DNA. The present invention relates to a silyl linker for use in the solid-phase synthesis o...
08/31/2010
7592446Synthesis of selenium-derivatized nucleosides, nucleotides, phosphoramidites, triphosphates and nucleic acids
The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucl...
09/22/2009
7432272Antiviral analogs
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 meth...
10/07/2008
7429572Modified fluorinated nucleoside analogues
The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2′R)-2′-deo...
09/30/2008
7405214Nucleoside derivatives and therapeutic use thereof
The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disord...
07/29/2008
7378402Anti-viral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions an...
05/27/2008
7335765Nucleoside and oligonucleotide analogues
A compound of the formula (1): wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or —P(R3)R4, wherein R
02/26/2008
7314923Nucleoside and oligonucleotide analogues
A probe for a gene or a primer for starting amplification comprising an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of the nucleoside units is a structure of the formula (2): ...
01/01/2008
7282581Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to Z...
10/16/2007
7265096Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorde...
09/04/2007
7247621Antiviral phosphonate compounds and methods therefor
Pharmaceutical compositions comprise a nucleotide analog with a phosphonate group at a concentration effective to act as a substrate and/or inhibitor of a viral polymerase, and especially of the HCV RNA dependent RNA polymerase. ...
07/24/2007
7247745Process for preparing 1,5-diaryl-3-substituted pyrazoles
A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III
07/24/2007
7235647Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides
The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically accept...
06/26/2007
7220730Cancer specific radiolabeled conjugates regulated by the cell cycle for the treatment and diagnosis of cancer
Radiolabeled conjugates are disclosed which have a component that is effective to target tumor cells, which cells selectively take up and degrade the conjugate, thereby delivering to the tumor cell nucleus a radioisotope capable of being incorporated into the nuclea...
05/22/2007
7217805Bicyclonucleoside analogues
Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable ...
05/15/2007
7192936Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
2′ and/or 3′ prodrugs of 1′, 2′, 3′ or 4′-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and o...
03/20/2007
7169766Methods and compositions for treating hepatitis C virus
A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided....
01/30/2007
7166718Calix[4]arene-nucleoside and calix[4]oligonucleotide hybrids
The present invention relates to calix[4]arene-nucleoside hybrids containing calix[4]arene moieties and calix[4]arene-oligonucleotide hybrids as a DNA hairpin structure mimics synthesized by using the calix[4]arene-nucleoside as a key building block. Calix[4]arene-n...
01/23/2007
7163929Methods and compositions for treating flaviviruses and pestiviruses
A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug...
01/16/2007
7160999Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers
A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-f...
01/09/2007
7145000Markable compounds for easy synthesis of 3'-[F] fluoro-3'-deoxynucleotides, and method for their production
What is described are compounds wherein R represents Br, I or R1—SO3, where R1 is an unsubstituted or substituted C1–C5-alkyl gr...
12/05/2006
7125983L-nucleic acid derivatives and process for the synthesis thereof
A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been...
10/24/2006
7105661Process for manufacturing morpholino-nucleotides, and use thereof for the analysis of and labelling of nucleic acid sequences
The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae:
09/12/2006
7101861Methods and compositions for treating flaviviruses and pestiviruses
A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug...
09/05/2006
7081526Process for manufacturing morpholino-nucleotides, and use thereof for the analysis of and labelling of nucleic acid sequences
The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae:
07/25/2006
7078518Forms of 5-Azacytidine
The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure...
07/18/2006
7074917Method for purifying 5′ -protected 2′ -deoxypurine nucleosides
A method for efficiently purifying 5′ protected 2′-deoxypurine nucleosides, efficient production of which has previously been difficult. Impurities can be separated by obtaining the 5′ protected 2′-deoxypurine nucleoside as an inclusion crystal including a s...
07/11/2006
7067641Phosphinoamidite carboxylates and analogs thereof in the synthesis of oligonucleotides having reduced internucleotide charge
Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH
06/27/2006
7056894Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases, and uses thereof
The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C...
06/06/2006
7038038Synthesis of 5-azacytidine
The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylat...
05/02/2006
7022680Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases
The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contribut...
04/04/2006
7002006Protection of nucleosides
A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally su...
02/21/2006
6974802Treatment of viral infections using prodrugs of 2′,3-dideoxy,3′-fluoroguanosine
A method of treating HBV or HIV infections comprising administering to an individual an effective amount of the compound of formula IId′: wherein R2 is the residue of an aliphatic ...
12/13/2005
6960568Nucleosides and related processes, pharmaceutical compositions and methods
The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention ...
11/01/2005
6958391Method for purifying 5′-protected 2′-deoxypurine nucleosides
A method for efficiently purifying 5′ protected 2′-deoxypurine nucleosides, efficient production of which has previously been difficult. Impurities can be separated by obtaining the 5′ protected 2′-deoxypurine nucleoside as an inclusion crystal including a s...
10/25/2005
6949639Oligonucleotide labeling reactants and their use
The invention relates to a novel labeling reactant of formula (I) suitable for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support t...
09/27/2005
6949640Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy...
09/27/2005
6933315Derivatives of isoindigo, indigo and indirubin and methods of treating cancer
A compound called NATURA, which is a derivative of Isoindigo is useful in aiding the general health of a patient and specifically is beneficial in preventing or treating cancer. This compound and other related Isoindigo, Indigo and Indirubin derivatives are designed...
08/23/2005
6930097Matrix metalloproteinase and tumor necrosis factor inhibitors
A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryimidine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of TNFα to TNFα-RI. ...
08/16/2005
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