Abstract: Novel chiral compounds that mimic and/or modulate the activity of wild-type nucleic acids are disclosed. In general, the compounds are phosphorothioate oligonucleotides wherein the 5?, and the 3?-terminal internucleoside linkages are chirally Sp and internal internucleoside linkages are chirally Rp.

Abstract: The present invention provides a method of preventing or treating retinal degeneration arising from pathophysiological or physical conditions. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor ligand, in an amount effective to elevate its extracellular concentration to activate retinal glial and neuronal cell surface P2Y receptors and mount a neuroprotective response. Methods of administering including intravitreal bolus and sustained administrations, transscleral delivery, topical, and systemic administrations. The pharmaceutical composition useful in this invention comprises a P2Y purinergic receptor agonist, which include uridine 5?-di-and triphosphate (UDP, UTP) and their analogs, adenosine 5?-diphosphate (ADP) and its analogs, cytidine 5?-di-and triphosphate (CDP, CTP) and their analogs, and dinucleoside polyphosphate compounds.

Abstract: Methods and Intermediates for the Preparation of Oligomers Containing Diastereomerically Enriched Phosphorothioate Linkages are Disclosed.

Abstract: Synthetic processes are provided wherein oligomers are prepared using phosphoramidite compositions. Oligomers having phosphodiester, phosphorothioate, phosphorodithioate covalent linkages are prepared that can include other covalent linkages. Also provided are compositions useful in such processes.

Abstract: Surfaces containing high purity silica (silicon dioxide) exhibit high loading potential for nucleic acids. Formulations containing nucleic acids and materials which mask the electrostatic interactions between the nucleic acids and surfaces are disclosed. By masking the phosphate charges of the nucleic acids, undesired interactions may be minimized or eliminated, thereby allowing the covalent bonding of the nucleic acids to the surface to proceed. The use of such formulations additionally minimizes nonspecific binding of the nucleic acids to the surface. Examples of materials to be included in such formulations include cations, xanthines, hexoses, purines, arginine, lysine, polyarginine, polylysine, and quaternary ammonium salts.

Abstract: Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.

Abstract: Active compound combinations, which have a light protection action, of 4,4′,4″-(1,3,5-triazine-2,4,6-triyltriimino)-trisbenzoic acid tris(2-ethylhexyl ester) and one or more emulsifiers chosen from the group of substances of the general structural formula wherein R1, R2 and R3 independently of one another are chosen from the group which comprises: H and branched and unbranched, saturated and unsaturated fatty acid radicals having 8 to 24 carbon atoms, in which up to three aliphatic hydrogen atoms can be replaced by hydroxyl groups, and n is a number from 2 to 8.

Abstract: A coprecipitant and a nucleic-acid extraction method using the coprecipitant are provided. The coprecipitant has affinity to the nucleic acids, no competitive inhibition to the reverse transcription and no inhibition to the PCR reaction in case of extracting a very small amount of nucleic acids by alcoholic precipitation using isopropyl alcohol or ethanol. Further, the coprecipitant can precipitate with the nucleic acids as a visible white or blue precipitate, thereby to suppress technical errors and enhance the extraction efficiency. A coprecipitant which acts in a process of extracting the nucleic acids by centrifugal separation from biological materials and/or test samples in the same manner as nucleic acids and has ability for precipitating as a visible white or blue precipitate when being separating and concentrating it by alcohol.

Abstract: A subject of the invention is the compounds of formula (I): R1═H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy, R2═H, Hal, R3═H, alkyl, Hal,  Rg and Rh: H, alkyl, aryl heterocycle, R5═H or O-alkyl, R6═alkyl or CH2—O-alkyl, R7═H or alkyl. The compounds of formula (I) have antibiotic properties.

Abstract: The present invention provides a peritoneal dialysis solution that contains heat stable osmotic agents such as D-glucitols, gluconic acids and alkylglycosides produced the reduction, oxidation or glycosylation of icodextrins respectively. As a result, osmotic agents that are stable under autoclaving or heat sterilization conditions are provided which reduces the amount of bioincompatible materials in the sterilized peritoneal dialysis solutions. Methods of preparing the D-glucitols, gluconic acids and alkylglycosides are disclosed.

Abstract: It is the object of the present invention to provide an industrially useful process for the manufacture of polyguluronic acids having degrees of polymerization less than 20 and substantially free of mannuronic acid contamination. Alginate salts of organic bases are quite soluble in aqueous solution, and remain soluble in aqueous solution throughout a hydrolysis reaction in the range of pH values at which the acidic hydrolysis is effected at a reasonably fast rate. Based on this finding, a solution containing 5 wt. % or more of alginic acid prepared by dissolving alginic acid in water by neutralization with an organic base is provided and then hydrolyzed under acidic conditions, followed by selective precipitation of polyguluronic acids under acidic conditions.

Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. wherein: X is Na, NH4 or H, provided that all X groups are not H.

Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.

Abstract: Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.

Abstract: The present invention relates to arsenic sulfide compounds. The present invention also relates to pharmaceutical compositions useful for treating cancer, such as leukemia or lymphoma, which comprises an arsenic sulfide compound. The present invention further relates to methods for treating cancer, such as leukemia or lymphoma, using an arsenic sulfide compound. Finally, the present invention relates to processes for producing arsenic disulfide (As4S4).

Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.

Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. Therapeutic uses of Formula I include treatment of sinusitis, otitis media, dry eye, retinal detachment, nasolacrimal duct obstruction, female infertility and irritation due to vaginal dryness, via increased mucus secretions and hydration of the epithelial surface. wherein: X is Na, NH4 or H, provided that all X groups are not H.

Abstract: This invention is directed to a method of stimulating tear secretion and mucin production in eyes. The method comprises the step of administering to the eyes of a subject a composition comprising a compound of Formula I, II, III, or IV and its pharmaceutically acceptable salts, in an amount effective to stimulate tear fluid secretion. The method of the present invention may be used to increase tear production for any reason, including, but not limited to, treatment of dry eye disease and corneal injury. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

Abstract: The invention provides a novel silicon-containing compound having an oxidation potential of 0.3 to 1.5 V on the basis of a standard hydrogen electrode, wherein at least one alkoxy group is bonded to a silicon atom and at least one aromatic amine group is also bonded to the silicon atom. An organic electroluminescence device having excellent mechanical and electric contact between an electrode and an organic layer is also provided by treating the surface of an anode with using a surface-treating agent comprising the above silicon-containing compound.

Abstract: A subject of the invention is the compounds of formula (I): in which R represents a carboxylic acid remainder containing up to 18 carbon atoms the products of formula (I) can be used to prepare antibiotic products.