Abstract: Compositions comprising the nucleotides adenosine diphosphate and adenosine monophosphate, and their use for neutralizing effects of excess incident energy on the human body, particularly effects of ionizing radiation from nuclear or radiological energy sources, are disclosed and claimed.

Abstract: The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.

Abstract: The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compounds according to the present invention show potent inhibition of the replication of the human immunodeficiency virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2,3?-dideoxy-?-ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an “O2 carbonyl”, that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.

Abstract: Disclosed are novel adenosine A3 receptor agonists of Formula I: wherein: R is hydrogen or lower alkyl; R1 is optionally substituted lower alkoxy or optionally substituted cycloalkyloxy; R2 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted trialkylsilyl; and R3 is hydroxymethyl or R4R5NC(Q)—; in which R4 and R5 are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl.

Abstract: The present invention relates to fluorescent cobalamins and uses of these compounds. More particularly, this invention relates to fluorescent cobalamins that comprise a fluorescent, phosphorescent, luminescent or light-producing compound covalently linked to cobalamin. These fluorescent cobalamins can be used to as diagnostic and prognostic markers (a) to distinguish cancer cells and tissues from healthy cells and tissues, including identifying lymph nodes containing cancer cells, and (b) to determine if an individual will respond positively to chemotherapy using cobalamin-therapeutic bioconjugates.

Abstract: There are provided 2-aminopurine derivatives represented by the following general formula (1): where R represents any species selected from the group consisting of hydrogen and acyl groups, X represents any species selected from the group consisting of phosphoramidite and oligonucleotides, Y represents any species selected from the group consisting of dimethyltrityl groups and oligonucleotides, and Z1, Z2, Z3, Z4 and Z5 are the same or different and represent any species selected from the group consisting of hydrogen and hydroxyl, amino, lower alkyl, alkoxy, carboxyl and sulfonic acid groups, provided that Z1, Z2, Z3, Z4 and Z5 are not all hydrogen, as well as gene expression-regulating compositions characterized by comprising the derivatives. By introducing the 2-aminopurine derivatives into oligonucleotides it is possible to achieve crosslinking reaction with high reactivity for target nucleic acids and notably high base sequence specificity.

Abstract: Provided are methods of producing phosphitylated compounds, including 3?-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula I wherein R, R1, and R2 are independently C1-C10 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, C7-C10 aralkyl, C1-C10 heteroalkyl, or C1-C10 heteroaryl, wherein any two adjacent R, R1, and R2 may be connected to form a heterocyclic ring; (2) acid-base complexes derived from a diazabicyclo amine base; and (3) combinations of two or more thereof.

Abstract: The present invention relates to a method of inhibiting cellular and protein attachment to substrates by applying a composition containing an effective amount of adherent N,O-carboxymethylchitosan to a substrate with such that cellular and protein attachment are prevented or greatly reduced.

Abstract: A method for purifying an oligonucleotide that comprises providing an oligonucleotide attached to a substrate, wherein the oligonucleotide contains phosphate protecting groups; contacting the oligonucleotide with a reagent, e.g., an organic amine, that cleaves the phosphate protecting groups from the oligonucleotide without detaching the oligonucleotide from the substrate; isolating the oligonucleotide attached to the substrate from the cleaved phosphate protecting groups; and cleaving the oligonucleotide from the substrate. This method provides crude oligonucleotide mixtures that are easier to purify and from which the desired full-length oligonucleotide product can be isolated in higher yields.

Abstract: Linear cyclodextrin copolymers and linear oxidized cyclodextrin copolymers containing an unoxidized and/or an oxidized cyclodextrin moiety integrated into the polymer backbone are described. Methods of preparing such copolymers are also described. The linear cyclodextrin copolymer and linear oxidized cyclodextrin copolymer of the invention may be used as a delivery vehicle of various therapeutic agents.

Abstract: The invention relates to acyclic chain terminator nucleotide analogs. More particularly, the invention relates to phosphonomethoxyethyl nucleotide analogs and detectably labeled versions thereof, especially fluorescently labeled versions thereof. The invention further relates to the use of chain terminating phosphonomethoxyethyl nucleotide analogs in methods of synthesizing a polynucleotide, labeling a polynucleotide, determining polynucleotide sequence information, and kits therefor.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.

Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one internucleoside 3′-NHP(O)(S−)O-5′ linkage, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive thiophosphoramidate oligonucleotides were found to retain the high RNA binding affinity of the parent oligonucleotide N3′→P5′ phosphoramidates and to exhibit a much higher acid stability.

Abstract: The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include an aminooxy linkage. These oligomers are useful for diagnostic, therapeutic and investigative purposes.

Abstract: The present invention relates to drug delivery devices for moist tissue, in particular mucosal tissue and tissue in the serous cavities, as well as a method of its use. The devices, which contain NOCC, are adherent to the mucosal tissue, allowing localized drug delivery. The devices are particularly useful in vaginal, buccal and ocular devices.

Abstract: A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia.

Abstract: The present invention discloses a method for treating heart rhythm disturbances in a mammal in need thereof by the administration of N6-substituted-5′(N-substituted)carboxamidoadenosines. More particularly, the invention is directed to a method for treatment of heart rhythm disturbances in a mammal that would benefit from the induction of negative dromotropic and/or negative chronotropic actions, comprising the administration to said mammal an effective amount of a compound of the Formula: or a pharmaceutically acceptable salt or ester thereof; wherein R1 is C3-7 secondary alkyl, or C3-8 cycloalkyl; and R2 is C1-4 alkyl or C3-5 cycloalkyl The invention is also directed to novel dosage forms comprising said compounds.

Abstract: This invention presents novel methods for synthesizing phosphorothioate oligonucleotides, using support-bound phosphoramidites. Novel intermediates useful in the methods are also provided.

Abstract: The present invention is a general method for irreversibly inactivating ribonucleases. Ribonucleases are completely inactivated by treating them with a reducing agent and heat. RNA samples contaminated with ribonuclease may be treated with this method to protect them from degradation. The RNA may then be used directly in a variety of enzymatic reactions and molecular biology techniques. This method may also be applied to a variety of molecular biology reagents which may be contaminated with ribonuclease to protect an RNA from being degraded when incubated with the reagent.

Abstract: Sulfofucosylacylglycerol derivatives represented by General Formula (1): where R101 represents an acyl residue of a higher fatty acid and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid. The derivatives represented by General formula (1) are useful as a DNA polymerase inhibitor and an anticancer agent.