Abstract: A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists of the Adenosine A1 receptor.

Abstract: 2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.

Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.

Abstract: The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleoside linkages of oligonucleotides. The invention provides new sulfur transfer reagents and processes for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage and highly efficient in sulfurization.

Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

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 and compositions for treating viral infection in vitro and in vivo using a guanosine-rich oligonucleotide. The oligonucleotides have sufficient guanosine to form a guanosine tetrad. Also provided are oligonucleotides of at least two runs of at least two guanosines. Also provided are guanosine-rich oligonucleotides and methods for treating viral infections in humans, and a method for designing guanosine-rich oligonucleotides having anti-viral activity and integrase inhibition activity.

Abstract: N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.

Abstract: The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]: wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.

Abstract: Guanosine-rich oligonucleotides having sequences that favor the formation under physiological conditions of a stable four-stranded structure containing two stacked guanosine quartets (G4s) are disclosed. These oligonucleotides demonstrate enhanced nuclease resistance, cellular uptake and biological efficacy. Methods and composition for treating viral infection using these guanosine-rich oligonucleotides are also disclosed. Certain embodiments of the new oligonucleotides are 16-17 nucleotides long and contain at least one C-5 propynyl dU substitution. A method for designing anti-viral oligonucleotides is also disclosed.

Abstract: The present invention relates to an improved method for synthesizing nucleosides with a low &agr;:&bgr; anomeric ratio. The method comprises coupling a protected furanosyl halide and an appropriately protected heterocycle in the presence of a nucleophilic polar solvent and a strong base.

Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

Abstract: An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F2 in He or other inert gas.

Abstract: Acyl derivatives of glycosyl-L-ascorbic acids which have a higher oil-solubility than L-ascorbic acid, glycosyl-L-ascorbic acids, and inorganic esters of L-ascorbic acid such as phosphates and sulfates of L-ascorbic acid. When administered to living bodies, the acyl derivatives easily permeate into living tissues to release L-ascorbic acid, resulting in an exertion of the physiological action inherent to L-ascorbic acid. Thus, the derivatives can be arbitrarily used in food products, cosmetics, and pharmaceuticals.

Abstract: The invention relates to an apparatus for isolating nucleic acids from biological fluids and suspensions containing nucleic acids, a reaction compartment 17 for receiving an adsorption medium 100 being connected to a removal compartment 50, and the nucleic acids being able to be moved and enriched from the reaction compartment 17 into the removal compartment 50 by an electrophoresis apparatus 20a, 20b.

Abstract: &agr;-D-pentofuranoside derivatives have the general formula (D), in which R stands for (C1-C4)alkyl that is non-substituted or substituted one or several times by halogen, (C1-C4)alkyl, (C1-C4)alkoxy and/or phenyl, and R1 stands for [(C6-C20)aryl]k−[(C1-C4)alkyl or [(C6-C20)]aryl]k−[(C1-C12)alkyl)(3-k)Si in which k=0 to 3, that are non-substituted or substituted one or several times by halogen, (C1-C4)alkyl, (C1-C4)alkoxy and/or (C6-C20) aryl, or preferably a benzyl that is non-substituted or substituted one or several times by the above substituents. Also disclosed are starting and intermediary compounds, up to furanosides (D) having an analogous structure, processes for preparing said furanosides and their precursors, and their use.

Abstract: The present invention is directed to reduce elevated levels of tumor necrosis factor-alpha (TNF-&agr;) found in a failing heart. The present invention is directed to a composition and method of regulating TNF-&agr; expression in myocardial tissue by treating the myocardial tissue with biological equivalents of endogenous adenosine. A composition and method of using the composition to treat patients with damaged myocardial tissue is provided which increases the cellular availability of adenosine with a resulting decrease of TNF-&agr; levels in the heart. The present invention provides a novel pharmacological intervention program in failing mammalian hearts, and more particularly provides a cardioprotective treatment to patients with congestive heart failure.

Abstract: Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

Abstract: Provided are very highly water soluble, stable, crystalline salts of 2′,3′-dideoxy-2′,3′-didehydrothymidine (“d4T”), 2′,3′-dideoxyinosine (“ddI”), and 2′,3′-dideoxy-2′-fluoroinosine (“F-ddI”). Such salts are useful as intermediates or as antiviral agents.

Abstract: The present invention relates to novel adenosine derivatives having the formula (I): wherein R is a lower alkyl group; R′ is hydrogen or a lower alkyl group; X is a cycloalkyl group, an alkyl group having at least one hydroxy group, an alkyl group having at least one phenyl group, a bicycloalkyl group, a naphthylalkyl group, an acenaphthylenylalkyl group or a group of the formula (II) or (III); Z is hydrogen, a hydroxy group or a lower alkoxy group, Q is hydrogen or a hydroxy group, A is —CH2—, —O—, —S— or shows a direct connection; Y is —(CH2)n— or shows a direct connection; n is an integer of 1 to 3; and the broken line is a double bond or a single bond. and pharmaceutically acceptable salt thereof, which are useful as antihypertensive agents.