Abstract: A method for the size reduction of high-molecular structures, in particular high-molecular nucleic acid structures, in samples wherein the high-molecular structures to be size-reduced are passed through a means provided with at least one porous layer the pore size of which decreases in the direction of the passage of the structures to be size-reduced through the porous layer.

Abstract: A method of treating alginic acid to produce polyguluronic acids.

Abstract: A composition for the protection, treatment and repair and for reducing the inflammation of connective tissue in mammals and a method for the treatment of connective tissue in mammals by the administration of the composition. The composition includes S-Adenosylmethionine (SAM), and a component selected from an aminosugar or salts thereof (e.g., glucosamine) or glycosaminoglycans (e.g., chondroitin salts) or mixtures or fragments thereof. The composition optionally includes manganese which promotes the production of connective tissue matrix. The composition also optionally includes methyl donors or methyl donor cofactors, such as vitamin B12, vitamin B6, folic acid, dimethylglycine or trimethylglycine.

Abstract: Methods of preparing bis-protected guanidino groups of formula (IX) comprising the steps of reacting a compound of formula (VIII) with an amine, wherein R′ is a thiopseudourea protecting group. Guanidino (IX) may then be used to add a guanidino functionality to other compounds, in particular those with a reactive hydroxyl group to give a protected functional group —NH—C(NH)—NH—CO—O—(CR5R6)N—CR3R4—Y—R2.

Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

Abstract: Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.

Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

Abstract: A method for treating HBV infections via administration of 2′, 3′ dideoxynucleoside compounds.

Abstract: Phosphite linked nucleotide sugars, e.g. nucleoside-monophosphite-glycosides, are synthesized using phosphoramiditing agents. The success of the synthetic method is largely independent of the choice of sugar and of nucleotide. The phosphite linked nucleotide sugars are shown to be useful, in the presence of an oxidizing agent, for the production of phosphate linked nucleotide sugars, e.g. nucleoside-monophosphate-glycosides.

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

Abstract: A photoactivatable nucleic acid derivative composition in which one or more photoreactive group(s) are bound to a natural or synthetic nucleic acid. The photoreactive groups can be bound to the nucleic acid before, during or after its formation, and can thereafter be activated in order to attach the nucleic acid to another molecule, e.g., to the surface of a solid support. Also described is a method of preparing such a composition, and a method of using such a composition to attach the nucleic acid to a another molecule, such as that provided by the surface of a substrate used to prepare a nucleic acid chip by photolithographic techniques.

Abstract: Aryl phosphate nucleoside derivatives show potent activity against HIV without undesirable levels of cytotoxic activity. Examples of aryl phosphate nucleoside derivatives include aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

Abstract: The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleotide linkages of oligonucleotides. The invention provides a process to synthesize new sulfur transfer reagents and a process for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage and in solution, and highly efficient in sulfurization.

Abstract: The present invention provides alkylphosphonate dimers and oligonucleotides prepared therefrom. The invention further provides novel methods for the preparation of these alkylphosphonate dimers. Methods for the preparation of substantially diastereomerically pure alkylphosphonate dimers are also provided.

Abstract: Disclosed is a method for quantifying cholesterol in HDL, which does not require complex fragmentation and separation operations, and by which the HDL cholesterol in test samples containing HDL and other lipoproteins such as low density lipoprotein (LDL), very low density lipoprotein (VLDL) and chylomicron (CM) may be quantified selectively, simply and accurately. The method for quantifying cholesterol in high density lipoprotein comprises a first step of erasing cholesterol in lipoproteins other than high density lipoprotein in a test sample, and a second step of adding a surfactant which specifically acts on high density lipoprotein to the product of the first step and enzymatically quantifying cholesterol in high density lipoprotein.

Abstract: The invention provides a method of potentiating the activity of antibacterial agents that act on bacterial cell walls, comprising the step of administering to a subject an antibacterial agent and an aminoglycoside to attain a peak concentration of at least 4 mg/l of aminoglycoside and thereafter maintaining the aminoglycoside at a concentration of up to 4 mg/l for at least 1 hour. Compositions comprising an antibacterial agent and an aminoglycoside for efficacious treatment of bacterial infection are also provided.

Abstract: The present invention embraces methods and compositions which employ antimicrobial compositions which are &agr;-alkylglucosides and esters thereof.

Abstract: Medicinal compositions which can be processed into solutions and are useful in inhibiting rejection reactions against the transplantation of organs or bone marrow, in the maintenance immunotherapy therefor or in treating autoimmune diseases, characterized by containing 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or pharmaceutically acceptable acid-addition salts thereof and cyclodextrins as a stabilizer optionally together with saccharides, if required.

Abstract: The present invention relates to an apparatus for preparing polynucleotides on a solid support in a reactor comprising a column containing an immobilized solid support that is functionalized for polynucleotide synthesis. The solid support can be porous, and can be functionalized with a nucleoside or with a universal synthesis of polynucleotides.

Abstract: The invention provides methods for purifying carbohydrates, including oligosaccharides, nucleotide sugars, and related compounds, by use of ultrafiltration, nanofiltration and/or reverse osmosis. The carbohydrates are purified away from undesired contaminants such as compounds present in reaction mixtures following enzymatic synthesis or degradation of oligosaccharides.