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| Number | Title | Issue Date |
| 7378402 | Anti-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 |
| 7345164 | Production 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 |
| 7265096 | Gemcitabine 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 |
| 7247621 | Antiviral 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 |
| 7235647 | Intermediate 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 |
| 7217805 | Bicyclonucleoside 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 |
| 7166718 | Calix[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 |
| 7145000 | Markable 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 |
| 7105499 | Nucleoside 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 |
| 7078499 | Nucleotide 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 |
| 6987180 | Uridine 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 |
| 6960568 | Nucleosides 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 |
| 6956028 | Compositions 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 |
| 6933288 | Pyranosyl 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 |
| 6930097 | Matrix 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 |
| 6897302 | Method 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 |
| 6884882 | 2′-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 |
| 6884880 | Process 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 |
| 6875752 | Uridine 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 |
| 6864366 | Process 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 |
| 6858591 | Antibiotic 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 |
| 6846918 | Nucleoside 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 |
| 6784161 | Method 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 |
| 6727232 | Nucleoside 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 |
| 6709679 | Antineoplastic 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 |
| 6689763 | Antibiotics 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 |
| 6680382 | Process 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 |
| 6635753 | Process 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 |
| 6579976 | Process 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 |
| 6504024 | Propargylethoxyamino 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 |
| 6376470 | Polymer 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 |
| 6359124 | Antisense 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 |
| 6331287 | 2'-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 |
| 6320040 | 4-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 |
| 6297222 | Acyl 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 |
| 6268490 | Bicyclonucleoside 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 |
| 6268183 | Method 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 |
| 6265569 | 3'-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 |
| 6265558 | Thiol-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 |
| 6184364 | High 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 |