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Class 536/28.53 - Chalcogen bonded directly to the 2- and 4-positions of the diazine ring (e.g., uridine, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 249
Last issue date: 11/02/2010


1              
NumberTitleIssue Date
7825239Antiviral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediat...
11/02/2010
7417034Pharmaceutically active uridine esters
The present invention relates to novel uridine esters of the general formula wherein R represents a carboxylic acid residue, preferably a fatty acid residue and R′ represents hydrogen or a hydroxy group, thei...
08/26/2008
7396826Pharmaceutically active uridine esters
The present invention relates to novel uridine esters of the general formula wherein R represents a carboxylic acid residue, preferably a fatty acid residue and R′ represents hydrogen or a hydroxy group, their u...
07/08/2008
7388094Processing for producing 2′-deoxy-2′-fluorouridine
1-β-D-Arabinofuranosyluracil in 3′,5′-hydroxyl-protected form is reacted with a trifluoromethanesulfonylating agent in the presence of an organic base to convert it into a 2′-triflate form, and then it is reacted with a fluorinating agent containing “a salt...
06/17/2008
7385050Cleavable linker for polynucleotide synthesis
Functionalized supports for polynucleotide synthesis are disclosed. The supports have linker moieties that are stable to conditions used in polynucleotide synthesis, but may be cleaved to release synthesized polynucleotides from the support. Methods of making the fu...
06/10/2008
7271258Methods of synthesizing oligonucleotides using carbonate protecting groups and alpha-effect nucleophile deprotection
The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect nucleophile irreversibly cleave the carbonate protecting groups whil...
09/18/2007
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
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
7119096Uracil reductase inactivators
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 ...
10/10/2006
7105498Acylated uridine and cytidine and uses thereof
The invention relates to compositions comprising acyl derivatives of cytidine and uridine. The invention also relates to methods of treating hepatopathies, diabetes, heart disease, cerebrovascular disorders, Parkinson's disease, infant respiratory distress syndrome ...
09/12/2006
6987180Uridine analogs and techniques for making and using
Uridine analogs and techniques for making and using uridine analogs are disclosed in this invention. These uridine analogs include nucleoside phosphates having a 5-aminouracil group. These nucleotides can be incorporated into a nucleic acid as an unnatural base, as ...
01/17/2006
6946450β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereo...
09/20/2005
6894159Process for the preparation of 2′-fluoro-5-methyl-beta-L-arabino-furanosyluridine
The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-β-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr...
05/17/2005
68848822′-deoxyuridine derivatives and hydrogels formed therewith
A 2′-deoxyuridine derivative of formula I is bioavailable and thermally stable and forms a gel in water at a low concentration; and, can be employed as a drug delivery vehicle: ...
04/26/2005
6875860Method for purifying 5′ -protected thymidines and novel derivatives thereof
This invention provides a method for efficiently purifying 5′-protected thymidines which cannot be efficiently purified by the prior art. Impurities can be separated by obtaining crystals including a carbonyl-containing solvent to provide a highly pure 5′-protec...
04/05/2005
6875752Uridine derivatives as antibiotics
All possible isomeric forms of a compound of the formula where the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts useful as antibiotics. ...
04/05/2005
6870048Process for the preparation of 2'-halo-β-L-arabinofuranosyl nucleosides
The present invention is directed to the process for the preparation of 2′-deoxy-2′-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2′-deoxy-2′-fluoro-β-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and le...
03/22/2005
6864366Process for the preparation of (e)-5-(2-bromovinyl)-2′-deoxyuridine
Process of preparing (E)-5-(2-bromovynyl)-2′-deoxyuridine (Brivudine) characterized in that halogen-free solvent selected form esters or cyclic ethers are used in the bromination step of 5-ethyl-2′-deoxyuridine diacylate. The use of solvents is advantageous in r...
03/08/2005
6858591Antibiotic AA 896 analogs
The invention provides compounds of the Formula 1 wherein the definitions of m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, ...
02/22/2005
6822090Process for the preparation of cytidine derivatives
An efficient method for producing cytidine derivatives that took away the previous drawbacks by efficiently synthesizing cytidine derivatives by utilizing a tertiary amine can be provided. ...
11/23/2004
6727232Nucleoside peptide antibiotics of AA-896
This invention relates to antibiotic compounds AA896 of the formula wherein: R1 is H, aryl, alkyl (C1-C20), —CH2-aryl, —C(O)alkyl(C1-C20), —C...
04/27/2004
6727231Uridine therapy for patients with elevated purine levels
The invention is based on the discovery that patients having elevated purine levels, e.g., individuals diagnosed with pervasive developmental disorders, such as autistic disorder, and/or neuromuscular disorders, can be treated with uridine compositions. ...
04/27/2004
6713623Tetraphosphonate bicyclic trisanhydrides
Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates. ...
03/30/2004
6699978Linker nucleoside, and production and use of the same
The present invention relates to a linker nucleoside, its preparation and use for the covalent bonding of biomolecules to oligonucleotides, in particular p-RNA oligonucleotides....
03/02/2004
6689763Antibiotics AA-896
This invention relates to new antibiotics designated AA-896-A1, AA-896-A2, AA-896-A3, AA-896-A4, AA-896-A5, AA-896-A6, AA-896-B1, AA-896-B2, AA-896-B3, AA-896-B4, AA-896-B5, AA-896-B6, AA-896-B7, AA-896-C1, AA-896-C2, AA-896-C3, AA-896-C4, AA-896-C5, AA-8...
02/10/2004
6646118Solid phase synthesis
The present invention relates to a support system for solid phase synthesis of oligomers, such as oligonucleotides, wherein the starting compound is bound to the support via a disiloxyl linkage. Furthermore, the invention relates to a method for synthesis...
11/11/2003
6642373Activators for oligonucleotide synthesis
The present invention relates to improved methods for the preparation of nucleoside phosphoramidites and oligonucleotides. In one aspect, the methods of the invention are used to prepare phosphitylating reagents using pyridinium salts as activators. In a ...
11/04/2003
6593466Guanidinium functionalized nucleotides and precursors thereof
The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for ...
07/15/2003
6579976Process for producing 2',3'-diethyl substituted nucleoside derivatives
There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing O-thiocarbonyl derivatives of sugar-moiety hydroxyl groups or...
06/17/2003
6566344ଲ-L-2'-deoxy-nucleosides for the treatment of hepatitis B
This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-ଲ-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or ...
05/20/2003
6545134Method for the production of pentopyranosyl nucleosides
Processes for the preparation of 3',4'-cyclic acetals of pentopyranosylnucleosides, in which the pentopyranosyl nucleoside is reacted with an aldehyde, ketone, acetal, or ketal under reduced pressure of less than about 500 mbar....
04/08/2003
6531589Base protecting groups and synthons for oligonucleotide synthesis
The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further provides a nucleoside base protecting group that is stable und...
03/11/2003
6512107Process for the preparation of 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine
The present invention relates to a novel and improved process for preparing 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus an...
01/28/2003
65068882'-O-amino-containing nucleoside analogs and polynucleotides
Novel nucleoside or nucleotide analogs comprising 2'-O-amino residues, processes for their synthesis and incorporation into polynucleotides....
01/14/2003
6504024Propargylethoxyamino nucleotide primer extensions
Propargylethoxyamino nucleosides are disclosed having the structure ##STR1## wherein R1 and R2 are --H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W1 is --H or --OH; W2 i...
01/07/2003
6498149Natural antitumor or antiviral substances and use of the same
The present invention provides substances having an efficacy against tumors and viruses on which the conventional anti-tumor agents and anti-virus agents exhibit only insufficient effects, and having carcinostatic effect and anti-virus effect on various r...
12/24/2002
6482921Uridyl peptide antibiotic (UPA) derivatives, their synthesis and use
The present invention relates to dihydro derivatives of the uridyl peptide antibiotics mureidomycin, pacidimycin and napsamycin which have antibiotic activity against a number of bacterial strains including strains resistant to current therapeutic antibio...
11/19/2002
64479982-Aminopyridine and 2-pyridone C-nucleosides, oligonucleotides comprising, and tests using the same oligonucleotides
The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonuc...
09/10/2002
6429309Solid phase synthesis
The present invention relates to a support system for the solid phase synthesis of oligomers, such as oligonucleotide, wherein the starting compound is bound to the support via a disiloxyl linkage. Furthermore, the invention relates to a method for synthe...
08/06/2002
6414137Selective solvent extraction for the purification of protected nucleosides
A process for the purification of nucleosides, and more particularly to a selective solvent extraction method for purifying protected nucleosides. In the purification process, solid particles of protected nucleosides are selectively washed to remove undes...
07/02/2002
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