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: 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: 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: 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: 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.

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 concerns a method and device for the rapid, simultaneous isolation of genomic desoxyribonucleic acid (DNA) and cellular total ribonucleic acid (RNA), free of genomic DNA from various starting materials. The fields of application are molecular biology, biochemistry, gene technology (in particular gene therapy), medicine, biomedical diagnosis, veterinary medicine, food analysis and all related fields. The method proposed is characterized in that materials containing DNA and RNA are lysed in a special buffer, the lysate incubated with a mineral carrier, the carrier with the DNA bound to it separated off and washed with buffer solution, and the DNA subsequently separated from the carrier with a buffer of lower salt concentration. The lysate left after separating off the DNA bound to the carrier is mixed with phenol, chloroform and sodium acetate in defined proportions, the phases allowed to separate, and the total RNA precipitated from the aqueous phase by adding isopropanol.

Abstract: A process for the preparation of 4"-deoxyerythromycins, having the formula: ##STR1## wherein R is H or OH, R.sup.1 is H or loweralkyl, and R.sup.2 is H or CH.sub.3 by treatment of the starting material, 2'-O-acetyl-4"-imidazolylthiocarbamoyl-erythromycin, with a hypophosphite reagent, in a water-miscible protic solvent optionally comprising a phase transfer agent. In a preferred embodiment, the water-miscible solvent is an alcohol and the starting material is reacted with sodium hypophosphite, ACVA and tetra-n-butylammonium hydroxide.

Abstract: 5,5'-Pyrophosphates of non-naturally occurring nucleosides selected from 1-(1-thyminyl)-3-azido-2, 3-dideoxy-D-riboside, 1(5-fluoro-1-uracilyl)-2, 3-dideoxy-D-riboside, 1-(1-uracilyl)-3-azido-2, 3-dideoxy-D-riboside, 1-(9-guaninyl)-2, 3-dideoxy-D-riboside, 1-(9-hypoxanthinyl)-2, 3-dideoxy-D-riboside, 1-(1-cytosinyl)-2, 3-dideoxy-D-riboside, and 1-(9-adeninyl)-2, 3-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutic agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as prodrugs encapsulated within biological carriers, e.g. transformed erythrocytes, for targeting to specific cell populations responsible for the development of the noted pathological disorders.

Abstract: The present invention is directed to a method of synthesizing sulfurized oligonucleotide analogs by reacting an oligonucleotide analog containing a phosphorous(III) linkage with a dithiocarbonic acid diester polysulfide having the formula ##STR1## to produce a sulfurized oligonucleotide analog. The diester polysulfide reagent is useful in solution and solid phase oligonucleotide analog synthesis.

Abstract: The present invention provides a practical method capable of chemically synthesizing a 100-mer or more long-chain oligonucleotide easily and reliably and a novel compound used in said method. The present invention relates to a method for chemical synthesis of an oligonucleotide by the phosphoroamidite method, which comprises preparing a base moiety-unprotected nucleoside phosphoroamidite from a base moiety-unprotected nucleoside by use of an imidazole trifluoromethanesulfonate represented by the following chemical formula, and coupling said base moiety-unprotected nucleotide phosphoroamidite in a predetermined order to chemically synthesize an oligonucleotide consisting of a specific nucleotide sequence, as well as to an imidazole trifluoromethanesulfonate represented by the chemical formula.