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Class 536/28.4 - The N-hetero ring is a 1,3-diazine ring, including hydrogenated (e.g., pyrimidines, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the N-hetero ring is a 1,3-diazine ring
No. of patents: 113
Last issue date: 05/27/2008


1      
NumberTitleIssue Date
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
7345164Production method of 5′-acyloxynucleoside compound
A production method for conveniently producing a 5′-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a 2′,3′,5′-triacyloxynucleoside compound represented by the formula [I] t...
03/18/2008
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
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
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
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
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
7105499Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are pa...
09/12/2006
7078499Nucleotide analogues comprising a reporter moiety and a polymerase enzyme blocking moiety
Nucleotides comprising a reporter moiety and a polymerase enzyme blocking moiety in which the reporter moiety does not also act as a polymerase enzyme blocking moiety are described. Also described are compounds of Formula (I): wherein W is a phosphate group, B is a ...
07/18/2006
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
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
6956028Compositions and methods for treatment of mitochondrial diseases
Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidine nucleotide precursors in amounts sufficient to treat symptoms result...
10/18/2005
6933288Pyranosyl cytosines: pharmaceutical formulations and methods
This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using solid-phase methodology. These hexopyranosyl cytosine derived natural product...
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
6897302Method for synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C)
The invention provides a method of synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C). The method allows for large-scale production of β-L-FD4C in an efficient, cost-effective, and environmentally sound manner. ...
05/24/2005
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
6884880Process for the preparation of 9-β-anomeric nucleoside analogs
A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-β-D- or L-purine nucleoside analog...
04/26/2005
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
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
6846918Nucleoside modifications by palladium catalyzed methods
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 metho...
01/25/2005
6784161Method for the treatment or prevention of flavivirus infections using nucleoside analogues
The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable sa...
08/31/2004
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
6709679Antineoplastic conjugates of transferin, albumin and polyethylene glycol
Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compound...
03/23/2004
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
6680382Process for preparing purine nucleosides
The present invention provides for the preparation ଲ-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and s...
01/20/2004
6635753Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof
There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates,...
10/21/2003
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
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
6376470Polymer conjugates of ara-C and ara-C derivatives
The present invention is directed to polymeric-prodrug transport forms of the formula: ##STR1## wherein: G is a linear or branched, terminally functionalized polymer residue; Y1 is O, S, or NR1 ; M is X or Q; wherein X is an electron with...
04/23/2002
6359124Antisense inhibition of ras gene with chimeric and alternating oligonucleotides
Compositions and methods are provided for the modulation of expression of the human ras gene in both the normal and activated forms. Oligonucleotides are provided that have methylene(methylimino) linkages alternating with phosphorothioate or phosphodieste...
03/19/2002
63312872'-deoxy-2'-fluoro-d-arabinofuranosyl pyrimidine nucleoside
The nucleoside analog 2'-fluoro-5-methyl-1-ଲ-D-arabinofuranosyluracil (FMAU) has been found to have an especially desirable combination of properties for use as an imaging agent, including in particular limited in vivo catabolism. Methods for the pr...
12/18/2001
63200404-desmethyl nucleoside analogs and oligomers thereof
Tetrahydrofuranyl compounds are provided that are functionalized to include pendant conjugate groups, and which are useful in diagnosis assays and as research reagents. Novel intermediates for the synthesis of the compounds are also provided....
11/20/2001
6297222Acyl deoxyribonucleoside derivatives and uses thereof
The invention relates to compositions comprising acyl derivatives of 2'-deoxyribonucleosides. The invention also relates to methods of treating or preventing radiation, mutagen and sunlight-induced biological damage, and methods for improving wound healin...
10/02/2001
6268490Bicyclonucleoside and oligonucleotide analogues
An oligo- or polynucleotide analogue having one or more structures of the general formula ##STR1## where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue ...
07/31/2001
6268183Method of purifying thuringiensin
The invention discloses a two-step process for recovery of thuringiensin, comprising adsorbing the thuringiensin from fermentation broth by calcium silicate, and dissociating the thuringiensin by dibasic sodium phosphate. The resulting thuringiensin can b...
07/31/2001
62655693'-Deoxyribonucleotide derivatives
Disclosed are 3'-deoxyribonucleotide derivatives represented by the following general formula [I]: Q--V--(CH2)n --NH--R [I] wherein Q represents a 3'-deoxyribonucleotide residue, n represents an integer not less than 4, V represents --C....
07/24/2001
6265558Thiol-derivatized nucleosides and oligonucleosides
Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain embodiments, the compounds of the invention further include s...
07/24/2001
6184364High affinity nucleic acid ligands containing modified nucleotides
Nucleic acid ligands containing modified nucleotides are described as are methods for producing such oligonucleotides. Such ligands enrich the chemical diversity of the candidate mixture for the SELEX process. Specific examples are provided of nucleic aci...
02/06/2001
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