Abstract: Deoxyuridine derivatives of Formula (I?); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.

Abstract: The disclosure provides nucleotide analogs and methods of their use. Analogs of the invention comprise a reporter molecule (label) attached via the N4, N6, O4, or O6 position of the nitrogenous base portion of the analog. In a preferred embodiment, nucleotide analogs of the invention comprise a label attached to the nitrogenous base portion of the analog via a cleavable linker at the N4, O4, N6 or O6 position.

Abstract: 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 use as pharmaceutically active agents against a variety of diseases, methods for the preparation of said uridine esters and pharmaceutical compositions containing at least one uridine ester as active ingredient. The present invention relates also to a drug combination comprising free fatty acids and/or fatty acid esters and uridine, deoxyuridine, uridine monophosphate and/or deoxyuridine monophosphate, and to the use of such a drug combination.

Abstract: The present invention is directed to new therapeutic compounds isolated from spider venom and methods of using these new compounds. The compounds are sulfated nucleoside derivatives including ribonucleoside mono- and disulfates derived from guanine, adenosine, and cytidine. Some of these compounds are glycosylated or fucosylated bearing one or more sugar residues.

Abstract: The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with alkyl halide or alkyl sulfonate in the presence of alcohol of Chemistry (FIG. 1) as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

Abstract: 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 use as pharmaceutically active agents against a variety of diseases, methods for the preparation of said uridine esters and pharmaceutical compositions containing at least one uridine ester as active ingredient. The present invention relates also to a drug combination comprising free fatty acids and/or fatty acid esters and uridine, deoxyuridine, uridine monophosphate and/or deoxyuridine monophosphate, and to the use of such a drug combination.

Abstract: 1-?-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 or complex formed by an organic base and hydrofluoric acid” to produce 2?-deoxy-2?-fluorouridine in 3?,5?-hydroxyl-protected form. A deprotecting agent is further caused to act thereon to obtain 2?-deoxy-2?-fluorouridine. The 2?-deoxy-2?-fluorouridine obtained can efficiently be purified by temporarily converting it into a 3?,5?-diacetyl form, recrystallizing the 3?,5?-diacetyl form, and then deacetylating it. Thus, high-purity 2?-deoxy-2?-fluorouridine can be produced.

Abstract: 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 functionalized supports and methods of using are also disclosed.

Abstract: The present invention discloses a 5?-amino-2?-fluoro-2?,5?-dideoxynucleoside derivative represented by the following formula [1]: (wherein R1 represents a nucleic acid base which may have a protecting group; R2 represents a hydrogen atom or a protecting group of an amino group; R3 represents a hydrogen atom or a protecting group of a hydroxyl group); a dideoxynucleoside-insoluble carrier bound substance prepared by binding said dideoxynucleoside derivative to an insoluble carrier, and an oligonucleotide analogue into which said dideoxynucleoside derivative is introduced. The oligonucleotide analogue being introduced with a dideoxynucleoside derivative of the present invention has excellent thermal stability and also high binding affinity when duplex is formed. Also, it is anticipated that it has high resistance to nucleases.

Abstract: The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with ?-effect nucleophiles. The ?-effect nucleophile irreversibly cleave the carbonate protecting groups while simultaneously oxidizing the internucleotide phosphite triester linkage to a phosphodiester linkage. The procedure may be carried out in aqueous solution at neutral to mildly basic pH. The method eliminates the need for separate deprotection and oxidation steps, and, since the use of acid to remove protecting groups is unnecessary, acid-induced depurination is avoided. Fluorescent or other readily detectable carbonate protecting groups can be used, enabling monitoring of individual reaction steps during oligonucleotide synthesis. The invention is particularly useful in the highly parallel, microscale synthesis of oligonucleotides.

Abstract: 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-nucleoside and calix[4]arene-oligonucleotide hybrids of the present invention can effectively recognize DNA or RNA through triplex formation by bonding between calix[4]arene containing cavity and biologically active substance.

Abstract: A novel method has been found to produce 2,2?-anhydro-1-(?-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2?-anhydro-1-(?-L-arabinofuranosyl)thymine. A novel method has been further found to L-2?-deoxyribose derivatives as a useful synthetic intermediate through L-2,2?-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.

Abstract: 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 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.

Abstract: 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 and for enhancement of phospholipid biosynthesis comprising administering the acyl derivatives of the invention to an animal.

Abstract: 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 a substitute for uridine or thymine. The nucleic acid can then be treated with an oxidizing agent and an alkaline solution, which causes cleavage of the nucleic acid at the position of the unnatural base. The nucleoside phosphate analogs can be used in many ways, including measuring chemical interactions between nucleic acids and other compounds, or sequencing nucleic acids. Additional compounds can also be derivitized onto the amino group, allowing other functionalities to be added to the nucleoside phosphate, or to the nucleic acid incorporating the nucleoside phosphate.

Abstract: 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-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

Abstract: The present invention relates to a novel and improved process for preparing 2?-fluoro-5-methyl-?-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:

Abstract: 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:

Abstract: 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?-protected thymidine. Thus, this invention allows 5?-protected thymidines, which cannot be purified in an industrial scale by the prior art, to be easily provided with a high purity in a large scale.

Abstract: 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.

Abstract: The present invention is directed to the process for the preparation of 2?-deoxy-2?-halo-?-L-arabinofuranosyl nucleosides, and in particular, 2?-deoxy-2?-fluoro-?-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.

Abstract: 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 respect of toxicity, discharge costs and environment protection.

Abstract: The invention provides compounds of the Formula 1 wherein the definitions of m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are in the specification. These compounds are useful as antibacterial agents.

Abstract: 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.

Abstract: A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intensity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is (1) a thymine/uracil derivative emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; (2) a cytosine derivative emitting light most intensely when the confronting base is guanine; (3) an adenine derivative emitting light most intensely when the confronting base is cytosine; and, (4) a guanine derivative emitting light most intensely when the confronting base is cytosine or thymine/uracil.

Abstract: The present invention relates to novel compounds according to the to the general formulas I, II, III, IV or V: 1

Abstract: 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-nucleoside and calix[4]arene-oligonucleotide hybrids of the present invention can effectively recognize DNA or RNA through triplex formation by bonding between calix[4]arene containing cavity and biologically active substance.

Abstract: The compounds represented by the formulae (I) wherein X is selected from the group consisting of: O, S, N—R1, and CHR1; Y and Y′ is individually selected from H, OR1, NR1R2, and N3 Z and Z′ is individually selected from II, OR1, and NR1R2 R=II, formula (II), formula (III), or formula (III), R1 and R2 is selected from H, alkyl, acyl, aryl which may be substituted or unsubstituted, R3 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, B is selected from 5 or 6-substituted uracil or cytosine, pseudouracil, N-substituted pseudouracil, 2-thiouracil, 2-thiocytosine, 5- or 6-substituted 2-thiouracil and 2-thiocytosine, 6-azauracil, 5-azacytosine, 8-azapurines, and 7-aza-8-deazapurines. Substitutions may be halosubstituted alkyl, halosubstituted alkenyl, halosubstituted alkynyl, halosubstituted aryl, alkylthio, or NR1R2.

Abstract: 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-Bl, 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-896-D1, AA-896-D2, AA-896-D3 and AA-896-D4 derived from the microorganism Streptomyces spp. LL-AA896 which are useful an anti-bacterial agents.

Abstract: The disclosure concerns a process for the recovery of uridine from molasses by means of chromatographic processes, whereby uridine is enriched to a high yield and high purity and in particular that uracil is separated from uridine.

Abstract: 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.

Abstract: 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(O)NHalkyl(C1-C20), or —C(O)NHaryl; R2 is H, alkyl (C1-C20), —CH2aryl, alkyl (C1-C20) or —C(O)alkyl(C1-C20); R3 is —OH; R2 and R3 may optionally be taken together to form a moiety R4 is alkyl (C1-C20), or aryl; or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Disclosed are compounds, compositions and methods for treating hepatitis C virus infections.

Abstract: 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.

Abstract: 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.

Abstract: 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-896-D1, AA-896-D2, AA-896-D3 and AA-896-D4 derived from the microorganism Streptomyces spp. LL-AA896 which are useful an anti-bacterial agents.

Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4′-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The present invention relates to a new, essentially four-step process for preparing beta-L-2′-deoxy-thymidine starting from L-arabinose. The process according to the invention is particularly important for mass production of beta-L-2′-deoxy-thymidine.

Abstract: 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 of oligonucleotides on a solid support. The support system comprises a stable disiloxyl linkage providing high nucleoside loadings to the support and the method allows convenient non-laborious oligomer synthesis.

Abstract: 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 further aspect, the methods of the invention are used to prepare internucleoside linkages using activators which include at least one pyridinium salt and at least one substituted imidazole. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having 2′-substituents using imidazolium or benzimidazolium salts as an activator. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having bioreversible protecting group that confers enhanced chemical and biophysical properties, without exocyclic amine protection, using imidazolium or benzimidazolium salts as an activator.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: 1

Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.

Abstract: A compound of formula (I) 1

Abstract: 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 TNF&agr; to TNF&agr;-RI.

Abstract: A process for efficiently producing a nucleic acid derivative by condensing a specific nitrogen-containing heterocyclic compound such as a dinitrogen 6-membered heterocyclic compound or a trinitrogen 5-membered heterocyclic compound with a pentose using a less expensive and safe reagent. Namely, a process for producing a nucleic acid derivative by condensing a dinitrogen 6-membered heterocyclic compound or a trinitrogen 5-membered heterocyclic compound with a pentose in the presence of an iron halide.

Abstract: 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 diagnostic, therapeutic and investigative purposes.

Abstract: The invention concerns compounds of formula (I) wherein: R2 is hydrogen, halogen, alkyl, alkenyl or alkynyl, a OH, O-alkyl, OCO-alkyl radical, an O-aryl or OCO-aryl radical; R4 is CH2NH2; CH2NHalkyl, CH2N(alkyl1)(alkyl2), CH2-guanidine, CH2-amidine optionally substituted; R5 represents in particular (a) or (b) or (c) or (d), a CH2N3 radical (e); R8 is hydrogen or alkyl; R9 is alkyl, aryl or heteroaryl, R8 and R9 capable of forming a heterocycle, or R5 represents a CH2alkyl, CH2Oalkyl or CO2alkyl, CH2Salkyl radical; R6 is hydrogen or halogen, OH, Oalkyl, OCOalkyl, S-alkyl or S-aryl; R7 is hydrogen or OH. The compounds of formula (I) exhibit antibiotic properties.

Abstract: 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 allowing halogenated derivatives in the sugar-moiety, in the nucleic acids or in derivatives thereof to react with any one of hypophosphorous acids (including salts thereof) and phosphites (esters) which are inexpensive, non-toxic and safely usable as radical reducing agents in industrial scale, in the presence of a radical reaction initiator. The process of the present invention is an industrially useful and highly safe process for reducing sugar-moiety hydroxyl groups and halogen atoms in nucleic acids or derivatives thereof (including nucleic acid-related compounds) at low costs.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.