Abstract: Oligonucleotides are provided which are effective in inhibiting the growth, metastasis and/or angiogenesis of tumors, including particularly melanoma and/or lung cancer. Methods are also provided for use of these oligonucleotides in the treatment of diseases.

Abstract: Methods and compositions are provided for infecting cells with virus. Specific embodiments involved stressing the cellular membranes with chemical, electrical or mechanical means, such as by incubating the cells in DOTAP or Transfectam.TM.. Other embodiments involve impregnating carriers with virus for use in research a suitable carrier such as a polymer or nanoparticle.

Abstract: A packaging system for the transportation and storage of materials, including radioactive and other hazardous materials. The system comprises a primary container removably received within a secondary container, and the secondary container being removably received within a tertiary container. The primary container can be centrifuged to minimize unrecoverable material, and in especially radioactive materials, the primary container is the only component that must be considered as radioactive waste.

Abstract: Ribavirin is administered to a patient in a dosage range which is effective to modulate lymphokine expression in activated T cells. In particular, ribavirin is used to suppress Th2-mediated T cell responses and promote Th1-mediated T cell response. Thus, instead of administering ribavirin in its well-recognized role as an anti-viral agent, ribavirin is herein used in the treatment of imbalances in lymphokine expression. Such imbalances may be found to be concomitants of allergic atopic disorders such as allergic asthma and atopic dermatitis, helminth infection and leishmaniasis, and various primary and secondary immunodeficiencies, which may or may not also be associated with viral infection.

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

Abstract: Methods and compositions are provided which increase the cellular uptake of bioactive materials by covalently bonding such compounds to carbohydrate moieties through chemical linkers using other than glycosidic bonds. Numerous carbohydrates, linkers and bioactive materials can be joined in this way to form novel compositions, which are collectively referred to herein as glinkosides. Preferred glinkosides are preferentially taken up by glucose receptor and/or other cellular receptors, and once inside the cells, the glinkosides are cleaved into a sugar, a linker or linker fragments, and a biologically active compound. Various aspects of the invention include processes for synthesizing glinkosides, glinkoside compositions, and methods of treating diseases using glinkosides.

Abstract: A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one of the forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.

Abstract: A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.

Abstract: A process for introducing vitamin B-12 into the bloodstream is disclosed by which vitamin B-12 is absorbed sublingually. The vitamin B-12 is in the form of a micro-lozenge which contains cyanocobalamin or hydroxocobalamin and which is capable of being dissolved in approximately four minutes or less.

Abstract: Certain 9-(.beta.-D-Ribofuranosyl)purine-6-carboxamide and other related compounds are prepared and are useful as antiviral agents.

Abstract: Imidazo[1,2-a]-s-triazines including the base, the nucleoside, derivatives of the nucleoside, and the 5' nucleotide are prepared and are useful as antiviral Agents against RNA viruses.

Abstract: 1-.beta.-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide is prepared by a process wherein a suitably substituted formimidic acid hydrazide is condensed with a blocked derivative of D-ribose and the intermediate is ring closed with a reagent which donates one carbon atom to yield a 3-substituted-1-(blocked .beta.-D-ribofuranosyl)-1,2,4-triazole. Treatment of this intermediate with ammonia and/or removal of the blocking group yields the product.

Abstract: Compounds of the structure ##STR1## wherein Y is O, NH or NAc; X is H, .beta.-D-ribofuranosyl or 2,3,5-tri-O-Ac-.beta.-D-ribofuranosyl and Ac is acetyl; are useful as antimicrobal agent.

Abstract: 9-.beta.-D-Arabinofuranosyl nucleotides of the following structure are disclosed: ##STR1## wherein AP is a 3' or 5' phosphorylated arabinofuranoside or the corresponding 3', 5' cyclic phosphate joined by a glycoside linkage to N.sup.9 of the aglycon component of said nucleotide, and Z is H, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkoxy, or hydroxy.Compounds prepared according to the invention exhibit antiviral activity in vitro, while others are precursors useful in the synthesis of bioactive compounds.

Abstract: 3,5,7-Trisubstituted pyrazolo[1,5-a]pyrimidines are disclosed of the general formula ##STR1## wherein R.sub.1 is CF.sub.3 or C.sub.1 -C.sub.9 alkyl; R.sub.2 is CF.sub.3 or C.sub.1 -C.sub.9 alkyl; and R.sub.3 is halogen. Such compounds are useful as inhibitors of 3',5'-cyclic AMP phosphodiesterase enzyme.

Abstract: Compounds of formula ##STR1## wherein X is --NR.sub.1 R.sub.2, --Cl, --Br or SR; Y is --X, --OH or --NH.sub.2 ; Z is hydrogen or --NH.sub.2 ; and R' is hydrogen or C.sub.1 -C.sub.18 acyl; R being hydrogen, aryl, aralkyl, substituted aryl, substituted aralkyl, or C.sub.1 -C.sub.7 alkyl; and R.sub.1 and R.sub.2 being independently selected from the group consisting of hydrogen, phenyl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.10 branched chain alkyl, C.sub.1 -C.sub.7 unsaturated alkyl or lower alkyl joined to form a 5 or 6-membered heterocyclic ring, with the proviso that when one of R.sub.1 and R.sub.2 are hydrogen, the other is not. The compounds variously exhibit phosphodiesterase inhibition, protein kinase activation, positive inotropic effects, adenyl cyclase inhibition and other biological activities.

Abstract: Ribofuranosyl derivatives of 3-deazaguanine including the 5'-phosphate, 3',5'-cyclic phosphate and 5'-deoxy, useful as antiviral agents and antibacterial agents, are disclosed.

Abstract: N.sup.6 -Carbamoyl and -carbonyl analogs of adenosine 3',5'-cyclic phosphate (cAMP) are prepared and variously demonstrated to exhibit kinase, adrenal steroidogenisis and lipolysis activation superior to cAMP, inhibit phosphodiesterase, and found to increase cardiac output or, in particular cases, to lower blood pressure.

Abstract: 2-Substituted-s-triazolo[1,5a]pyrimidines are disclosed which are useful as inhibitors of phosphodiesterase enzymes or intermediates in the production process. Such compounds are of the following structure: ##STR1## wherein X, R, R.sub.1, R.sub.2 and R.sub.3 are as defined hereinafter.

Abstract: As antiviral agents and intermediates therefor, 3-substituted 1-(.beta.-D-glycosyl)-1,2,4-triazoles, O-acylated analogs thereof, and 5'- and 3',5'-cyclic phosphates of the triazole nucleosides, "glycosyl" being .[.a pentofuranosyl moiety, preferably one whose 2'-oxygen is trans to the triazole aglycon, e.g., xylofuranosyl,.]. ribofuranosyl, .[.2-0-methylribofuranosyl, etc.,.]. the triazole aglycon being 3-substituted with cyano, methylcarboxylate, carboxamidoxime, carboxamido-, thiocarboxamido, or carboxamidine. Preparation of these nucleosides is by silylation of the substituted triazole followed by glycosylation with the appropriate blocked glycosyl halide. Alternatively, acid-catalyzed fusion of the requisite 1,2,4-triazole with an O-acylated pentofuranose yields the nucleosides.