Abstract: Methods of modulating the activity of the TAR element of HIV are provided. Oligonucleotides having 6 to 50 bases and at least one 2'-O alkyl modification and selected sequences are disclosed.

Abstract: Replacement of the natural nucleotides with unnatural zwitterionic nucleotides having a cationic moiety tethered to the base (or analog thereof) results in oligodeoxynucleotides with diminished charge but undiminished ability to complex with DNA at low ionic strengths. We have now discovered that DNA can be made fully zwitterionic by introducing tethered cationic moieties to the bases without affecting duplex formation. The resulting oligonucleotides have the further advantages of being nuclease resistant.

Abstract: Antimicrobial compounds having the formula ##STR1## as well as pharmaceutically acceptable salts, 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: The present invention relates to the discovery that certain .beta.-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV), Varciella-Zoster virus (VZV) and Herpes Virus 8 (HV-8). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV, VZV and HV-8 infections in humans.

Abstract: This invention discloses a method for the preparation of 2'-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the novel pyrimidines and purines that can be prepared according to the method of the invention and oligonucleotides containing said modified pyrimidines and purines.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, and phosphorodithioate covalent linkages. Also provided are synthetic intermediates useful in such processes.

Abstract: A method for inhibiting replication of HIV, which comprises subjecting HIV-infected cells to a composition (a) comprising as a primary component a polysaccharide derived from a hot aqueous solvent extract of tubercle bacillus.

Abstract: The object of the present invention is a pharmaceutical composition, which comprises, as active principle, a combination of an adenosinergic agonist and a compound selected from the opiates, benzodiazepines and NMDA antagonists.

Abstract: The present invention relates to a method for treating AIDS, which comprises administering to an HIV-infected patient (a) a composition containing as the primary component a polysaccharide derived from a hot water extract of human-type tubercle bacillus and (b) a nucleoside-type anti-HIV agent. Due to the incorporation of composition (a), the present invention enhances the therapeutic effect of nucleoside-type anti-HIV agents on AIDS.

Abstract: This invention relates to synthetic oligonucleotides that are useful for antisense based therapeutic applications. The synthetic oligonucleotides of this invention have modifications in the sugar phosphate backbone for improved antisense properties.

Abstract: A linker arm for solid support oligonucleotide synthesis, the linker arm comprising formula (1), wherein: X.sup.1 is selected from the group consisting of --O--, --S--, --S(O).sub.2 --, --C(O)-- and --N(R.sup.12)--; R.sup.12 is selected from the group comprising hydrogen, a substituted or unsubstituted C.sub.1 -C.sub.20 alkyl group, a substituted or unsubstituted C.sub.5 -C.sub.30 aryl group and a substituted or unsubstituted C.sub.5 -C.sub.40 alkaryl group, X.sup.3 is --O-- or --N(H)--; R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C.sub.1 -C.sub.20 alkyl group, a substituted or unsubstituted C.sub.5 -C.sub.30 aryl group and a substituted or unsubstituted C.sub.5 -C.sub.40 alkylaryl group; n is 0, 1 or 2; and one of A' and B' is selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C.sub.1 -C.sub.20 alkyl group, a substituted or unsubstituted C.sub.5 -C.

Abstract: The invention provides a cationic polynucleoside chain having multiple nucleosides, the nucleosides being coupled together by positively charged guanidyl linkages.

Abstract: Provided is an artificial nucleic acid which has a double-stranded structure made of two oligonucleotides, where the oligonucleotide has in a sugar-phosphate backbone structure thereof a sugar moiety having a group having a metal-coordinating site, and the two oligonucleotides are bound together through a metal complex structure formed by coordination of the metal-coordinating site to a metal ion. Also provided is a nucleotide useful for synthesizing the artificial nucleic acid.

Abstract: There is described a polycarboxylic acid or a salt thereof obtained by oxidation of a polysaccharide containing an anhydrous glucose as a constituent unit, wherein the carboxyl group content thereof is high and the weight average molecular weight thereof is not less than 2000. This polycarboxylic acid is suitable for use as a builder for detergent because the amount of an alkali required to perform neutralization titration of the polycarboxylic acid is not less than 435 mg in terms of sodium hydroxide and because the chelate force thereof to a polyvalent cation is high.The polycarboxylic acid is produced by oxidizing a polysaccharide with an oxidizing agent in the presence of a transition metal catalyst.

Abstract: The present invention is related to a novel class of decarboxylase enzyme inhibitors consisting of .alpha.-oxiranyl amino acids and derivatives thereof and a method of synthesizing such compounds.

Abstract: The present invention provides a method for the preparation of disaccharides, such as glucosaminyl muramic acids peptides and derivatives. The method includes condensing a protected muramic acid ester with a 1-organothio- or 1-fluoroglucosamine derivative in the presence of a suitable promoter to produce a protected glucosaminyl muramic acid ester. The protected glucosaminyl muramic acid ester may be used to prepare disaccharide peptides, such as N-acetylglucosaminyl-N-acetylmuramyl dipeptides, which have demonstrated immunological activity. Protected muramic acid esters and 1-organothio- or 1-fluoro-glucosamine compounds which may be employed as intermediates in the method are also provided.

Abstract: The present invention relates to methods for substantially enhancing the stereoselective synthesis of .beta.-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.

Abstract: Novel coumarin derivatives comprising a coumarin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivate cross-linking groups when incorporated into polynucleotides as replacements for one or more of the complementary nucleoside bases present in probes used in procedures involving nucleic acid hybridization reactions.

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: Acid resistant Oligomers suitable for oral administration, orally acceptable formulations of such Oligomers and preparation of pharmaceutical formations of such Oligomers are provided.