Abstract: Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.

Abstract: The present invention relates to the treatment of conditions associated with neuronal activity. Specifically, the invention is drawn to methods and compositions for administering adenosine to inhibit pain syndromes or epilepsy in a patient.

Abstract: The present invention presents novel methods for recovery of phosphoramidites from the waste products of oligonucleotide synthesis. The methods include reacting a trihalophenoxydihalophosphorane with a H-phosphonate in the presence of an amine.

Abstract: A process for preparing alkyl polyglycosides by reacting a fatty alcohol with a saccharide in a glycosidation reaction under acidic condition wherein a water-containing emulsion is drawn off from the reaction includes an improvement wherein the emulsion is demulsified by raising the pH of the water-containing emulsion, preferably to a level above 7, whereupon the demulsified water-containing emulsion is allowed to settle into at least a predominantly fatty alcohol containing first layer and a predominantly water-containing second layer. The fatty alcohol-containing layer can be recycled back to the glycosidation reaction. The pH of the water-containing emulsion can be raised by the addition thereto of caustic, such as sodium hydroxide.

Abstract: A method and composition for inhibiting the spread of a retrovirus such as HIV in a human cell population in which a retrovirus such as HIV is present has been found. The spread of the retrovirus is inhibited by treatment of the cells with a synergistic combination mixture of a dideoxy-ribonucleoside excluding AZT and hydroxycarbamide.

Abstract: A novel process is provided for producing a 5-perfluoroalkyl-5,6-dihydrouracil represented by General Formula (1): ##STR1## (where R.sup.1 and R.sup.2 are independently hydrogen, methyl, or ethyl, and Rf is a perfluoroalkyl of 1 to 10 carbons). The process comprises reacting .alpha.-perfluoroalkylacrylic acid represented by General Formula (2):CH.sub.2 =C(Rf)--COOH (2)with a urea derivative represented by General Formula (3):R.sup.1 NHCONHR.sup.2 (3)in the presence of acetic anhydride with formed acetic acid being removed out of the reaction system during the reaction. The .alpha.-perfluoroalkylacrylic acid may be added successively. A process for producing a 5-perfluoroalkyl-5-bromo-6-hydrouracil by General Formula (4) is also provided: ##STR2## (where R.sup.1, R.sup.2, and Rf are as defined above) wherein the reaction of a 5-perfluoroalkyl-5,6-dihydrouracil produced by the above process with bromine is conducted in water as the solvent.

Abstract: A method for preparing a conjugate, and preferably a protein-polysaccharide conjugate, includes functionalizing a first moiety (e.g., a polysaccharide) with one or more pendant haloacyl groups. Thereafter, the functionalized first moiety is reacted with a second moiety, preferably an unmodified protein or a protein to which no thiol groups have been added, to form a covalently linked conjugate. Various different haloacyl reagents can be used in the invention. For example, the haloacyl reagent can be an active ester, an anhydride, a haloacyl chloride, or a haloacyl acid. Specific haloacyl reagents that can be used in the process of the invention include N-succinimidyl-2,3-dibromopropionate and N-succinimidyl iodoacetate. The invention further relates to the conjugates produced by the method of the invention. These conjugates can be used as immunogens or vaccines.

Abstract: 5',5'-Pyrophosphates of non-naturally occurring nucleosides selected from thymine-3'-azido-2',3'-dideoxy-D-riboside, 5-fluorouracil-2'-deoxy-D-riboside, uracil-3'-azido-2',3'-dideoxy-D-riboside, guanine-2',3'-dideoxy-D-riboside, hypoxanthing-2',3'-dideoxy-D-riboside, cytosine-2',3'-dideoxy-D-riboside, and adenine-2',3'-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutical pharmaceutical compositions or as pro-drugs encapsulated into biological carriers, e.g., transformed erythrocytes, for targeting to specific cell population responsible of the development of the pathological disorders.

Abstract: Disclosed is a rinse solution for rinsing organs and tissues prior to transplantation. The solution comprises, in one liter of solution: from 2 mM to 50 mM glycine; from 0.12 to 1.2 mM adenosine; monosaccharide, sodium, potassium, calcium and magnesium ions; and water for injection sufficient to make a liter of solution; said solution having a pH of about 6.0 to 7.5 and a concentration of potassium of less than 6 MEQ/L. Methods of making and using the solutions are also disclosed.

Abstract: The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.

Abstract: Antimicrobial compounds having the formula as well as pharmaceutically acceptable sats, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: Disclosed are ursodeoxycholic acid derivatives having an increased solubility in water, and methods for producing the derivatives. To produce the derivatives, ursodeoxycholic acid is protected at its carboxyl group with a benzyl group, then reacted with tetrabenzyl-acetic acid-oxyglucoside of the following formula (1), and de-benzylated; or ursodeoxycholic acid is protected at its hydroxyl group with a t-butyldimethylsilyl group, then reacted with tetrabenzyl-2-hydroxyethyloxyglucoside of the following formula (2), and de-t-butyldimethylsilylated and de-benzylated.

Abstract: Described is an apparatus for the contamination-free isolation of nucleic acids from biological fluids and suspensions containing nucleic acids comprising: a reaction compartment for holding an adsorption medium laden with nucleic acids; connected via a channel to a removal compartment; wherein the nucleic acids can be moved by an electrophoresis device from the reaction compartment into the removal compartment and enriched there; and the reaction compartment can be charged via a charging orifice and drained via a draining orifice being located essentially opposite of the charging orifice.

Abstract: The present invention describes methods for linking phosphoramidite nucleosides to a solid support-bound nucleoside. This invention presents novel processes for synthesizing oligonucleotides. Acetonitrile having a water content between 30 ppm and about 1250 ppm is used as the solvent for the washing steps in solid phase oligonucleotide synthesis, or is used as a solvent for the capping reagent or oxidizing reagent. The processes of the present invention are amenable to large-scale, economic oligonucleotide synthesis using the phosphoramidite method.

Abstract: A class of substituted and unsubstituted nucleo-base analogs and related azoles, designated as "phosphazoles," is disclosed, certain preferred embodiments having the basic structure of ##STR1## Also disclosed are methods of making and using the new compounds.

Abstract: A cyclic oligosaccharide or salts thereof comprising glucoses bound cyclically via .alpha.-1,6-linkages and having at least one S-oxo acid group bound, and ana gent for preventing or treating retroviral diseases which comprises said cyclic oligosaccharide or salts thereof as an active ingredient. The novel sulfated cyclic isomaltoligosaccharide inhibits infection of host cells with various retroviruses such as AIDS virus etc. so effectively that it has a significant preventive and therapeutic effect on diseases caused by retroviruses. Accordingly, said oligosaccharide can be utilized as an agent for preventing or treating retroviral diseases in pharmaceutical industry.

Abstract: It was found that normal human stem cells produce a regulated non-processive telomerase activity, while cancer cells produce a processive telomerase activity. Nucleotide analogs, such as 7-deaza-2'-deoxyquanosine-5'-triphosphate (7-deaza-dGTP) were found to be substrates for processive telomerase and incorporated into telomeric sequence. The incorporation of this nucleotide subsequently affected the processivity of telomerase, converting processive telomerase to non-processive telomerase. The incorporation of this nucleotide analogs was also found to inhibit formation of G-quartets by telomeric sequence. Other methods for converting cancer processive telomerase to the more benign non-processive telomerase include partially cleaving the telomerase RNA.

Abstract: Hyaluronic acid, hyaluronate esters and salts thereof are sulfated such that the number of sulfate groups per monomeric unit is in the range of from 0.5 to 3.5. The sulfated derivatives exhibit anticoagulant and cell adhesion reduction properties, and may be used to prepare biomaterials.

Abstract: A method for inhibiting replication of reverse transcriptase dependent virus in plant or animal cells, comprising the step of administering to said cells a compound that depletes the intracellular pool of deoxyribonucleoside phosphate in an amount effective to inhibit replication of said virus. Hydroxyurea is one such suitable compound. Also disclosed is a method for producing incomplete reverse-transcriptase dependent viral DNA, by administering a deoxyribonucleoside phosphate-depleting drug to cells infected with such a virus.

Abstract: The invention discloses new oligodeoxyribonucleotides of animal origin, having a molecular weight comprised between 4000 and 10000 daltons, that can be obtained by fractionation of polydeoxyribonucleotides or otherwise by chemical or enzymatic depolymerization of high molecular weight deoxyribonucleic acids. The new compounds are endowed with a significant anti-ischemic activity.