Abstract: The present invention reveals a new series of derivatives and analogues of adenine and adenosine, i.e., 3'-adenosine derivatives, which inhibit adenylyl cyclase activity. These newly synthesized compounds include the most potent inhibitors of adenylyl cyclases known. The present invention also discloses a method for measuring the inhibition of adenylyl cyclase activity.

Abstract: Site 1- and site 2-selective derivatives of cAMP have been found to inhibit the growth of a variety of cancer and leukemic cells. The compounds have been found to have a synergistic effect in cancer and leukemic cell growth inhibition when a site 1-selective compound is used in combination with a site 2-selective compound.

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). 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 infections in humans.

Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Methods of treating fungal infections are disclosed. The methods comprise administering a chitin synthesis inhibitor to a mammal in a continuous fashion so that at least a minimum effective concentration is maintained in the mammal's plasma or in a target organ. In a preferred embodiment, the administration is by continuous intravenous infusion and the fungal infection is due to Candida albicans. In another preferred embodiment, the administration is by a sustained release formulation and the fungal infection is due to Candida albicans.

Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.

Abstract: 2',3'-Dideoxy-3'-fluorouridine is purified by treating an aqueous or aqueous methanolic solution with charcoal.

Abstract: 5'-O-Acyl-5-fluorouridines and 5'-O-acyl-5-sluorocytidines are prepared by the direct acylation of the 5'-hydroxyl group with amino acids under Mitsunobu conditions and the amino acyl derivatives are coupled with other amino acids or peptides to provide antibacterial and antifungal derivatives of the nucleosides. For example, 5-fluorouridine is acylated at the 5'-hydroxyl group with an amino protected L-valine and the acylation product is deprotected to provide 5'-O-(L-valinyl)-5-fluorouridine having activity against Gram-positive bacteria including resistant staphylococcus. Preferred peptide derivatives comprise the tripeptides of ornithine and lysine wherein the terminal amino group is substituted by both hydroxy and acetyl. The latter peptides inhibit the growth of C. albicans.

Abstract: Cathepsin G-inhibiting aptamers comprising oligonucleotides selected from the group consisting of the consensus sequences: ##STR1## wherein N represents nucleotides and the figures represent the number of possible nucleotides at that site; said cathepsin G-inhibiting aptamers are suggested as medicament.

Abstract: An improved process for the separation of RNA from a liquid sample of biological origin containing RNA comprises (a) intimately contacting the sample with a two-phase composition wherein the upper phase is predominately phenol and the lower phase is an aqueous solution comprising at least one water-soluble guanidinium salt, a buffer and urea, the water content of the aqueous phase being relatively low, (b) adding a relatively dense water-insoluble solvent and (c) recovering RNA from the resulting aqueous phase.

Abstract: The present invention provides nucleic acid compounds which have a non-nucleic acid structure with ring skeleton to which two functional groups are bound with fixed state and are able to point to substantially the same direction, nucleic acid compounds which can form triple strands with third nucleotide chains, nucleic acid compounds which have improved permeability, and synthetic methods thereof.

Abstract: The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: ##STR2## in which R.sup.a, R.sup.b and R.sup.c are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R.sup.1 and R.sup.2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R.sup.3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3'-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.

Abstract: The invention provides compositions and methods to prevent the appearance of visually detectable precipitate in the composition upon storage of an aqueous solution of the composition containing 5-250 mg/mL of the phosphonate nucleotide analog for at least 6 months at 22.degree. where the composition comprises a phosphonate nucleotide analog and a sufficient amount of a divalent or trivalent metal cation sequestering agent such as about 0.1% w/v EDTA, and/or a sufficiently low concentration of a divalent or trivalent metal cation, e.g., about 3-10 ppm, and/or a sufficient pH in water, e.g., a pH of about 7.0-7.5.

Abstract: The compound 8-chloroadenosine 3',5'-cyclic phosphate and its pharmaceutically acceptable salts are used to treat malignant tumors in afflicted hosts.

Abstract: The present invention provides an inhibitor of monoamine oxidase comprising a modified synthetic flavin adenine dinucleotide compound. Also provided is a method of inhibiting monoamine oxidase enzymatic activity in a cell, comprising the step of contacting said cell with a pharmacologically effective dose of a modified synthetic flavin adenine dinucleotide compound. Further provided is a method of treating a brain pathophysiological state in an individual, comprising administering a therapeutically effective dose of a modified synthetic flavin adenine dinucleotide compound to said individual.

Abstract: Method for production of 2'-O-derivatized uridine and cytosine RNA synthons comprising derivatizing the 2'-hydroxyl group of a partially protected cytosine ribonucleoside to preferentially produce a partially protected 2'-O-derivatized nucleoside, which is then either (1) reacted at the 3'-hydroxyl group to produce a 2'-O-derivatized cytosine RNA synthon, or (2) reacted with a hydroxide source to produce a uridine nucleobase by deamination, thereby producing a partially protected 2'-O-derivatized uridine ribonucleoside which can be reacted at its 3'-hydroxyl group to produce a uridine RNA synthon.

Abstract: The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in those processes.

Abstract: Therapeutically utilizable oligonucleotides of the formulae I and II have been obtained by introduction of terminal 3'--3' and 5'--5' linkages. These compounds are stable to nucleases and suppress the biological function of nucleic acids.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sup.1 is hydrogen, benzyl or a substituted benzyl group;X is hydrogen, a flouro, an amino or a substituted amino group;Y is hydrogen, a methoxy, a methylthio, a benzylthio, a methylethyl, a chloro, an amino or a substituted amino group; andY' is an oxo or a thio group; andZ is hydrogen, a hydroxy, a methoxy, a halogen, an amino or a substituted amino group.The present invention also provides a method of synthesizing a compound having the above-identified structure as well as the intermediate compounds produced according to that method.

Abstract: Methods for inducing immunosuppression in animals which need immunosuppressive treatment involving administration to animals of a therapeutically effective amount of the cyclic AMP agent HE-33 or its nucleoside.