Abstract: A preferred method and dosages for treatment of retrovirus-induced dementia by the administration of 2',3'-dideoxyinosine(ddI) is disclosed.

Abstract: The present invention discloses the use of [R]-3-(2-deoxy-.beta.-D-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo-[ 4,5-d][1,3]diazepin-8-ol, also commonly known as pentostatin, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprised of such compounds, in the prophylactic or affirmative treatment of cerebral and cardiovascular disorders such as cerebral and myocardial ischemia. The invention also discloses the administration of pentostatin along with adenosine in the prophylactic or affirmative treatment of cerebral and cardiovascular disorders.

Abstract: A versatile polymeric support system for the synthesis of oligonucleotides is provided featuring a universal primer which allows chain elongation, in either the 3' or 5' direction, with any currently available DNA or RNA synthesis method, by a process which utilizes oxidatively cleaved primers to facilitate chain elongation and release. The support system is capable of withstanding mildly basic and acidic reaction conditions, while still permitting a convenient and quantitative release, either before or after removal of protecting groups from reactive groups, of synthesized oligonucleotides from a single polymeric support. Removal of the protecting groups before cleavage of the oligomer from the support permits the use of the immobilized oligomer as an affinity hybridization support for both isolating and detecting complementary polynucleic acids.

Abstract: Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons, and P-chiral oligonucleotides and related P-chiral polymers.

Abstract: Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. In preferred embodiments, the reactive portions comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with and without intervening intercalating moieties and act through phosphorodiester hydrolytic bond cleavage. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided which are useful for elaboration of oligonucleotides for such purposes.

Abstract: A novel method for the isolation of high molecular weight DNA from plants, yeast bacteria, and animal cells or tissue employs xanthate forming compounds, such as sodium/potassium ethyl xanthogenate. The procedure does not require deproteination and yields clean DNA that is suitable for both PCR and Southern blotting. It can be utilized on a small scale without homogenizing the tissue. These features also facilitate automated screening of tissue samples, one of the labor-intensive techniques in molecular biology.

Abstract: The present invention relates to a freeze-dried preparation comprising (1) about 5 to about 50 W/W% of a non-volatile acid and/or a salt thereof, (2) about 10 to about 95 W/W% of 4-O-(2-deoxy-2-dimethylamino-4,6-O-ethylidene-.beta.-D-glucopyranosyl)-4'- demethyl-4-epipodophyllotoxin hydrochloride and (3) 0 to about 85 W/W% of at least one sugar as a stabilizer.

Abstract: The object of the present invention is the administration of a substance which contains, as active principle, an adenosine substituted on N.sup.6 of formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 each represents hydrogen or ##STR2## for the treatment of hyperlipemia and/or hypertriglyceridemia.

Abstract: Method for substituting a substitution compound for the hydrogen of a support bound primary hydroxyl group. The support bound primary hydroxyl group is treated in an organic, substantially anhydrous solvent in the presence of a tertiary amine base and the substitution compound.The substitution compound has a positive moiety and a negative moiety. The positive moiety is selected from the group consisting of trityl, pixyl, and derivatives thereof.The reagent is selected from the group consisting of tetraalkylammonium salts, inorganic salts, and mixtures thereof. Each reagent has a cation and an anion moiety.The cation moiety of the reagent is more electropositive than the positive moiety of the substitution compound. This relationship enables the reagent to attract the negative moiety of the substitution compound.

Abstract: Compounds of the formula ##STR1## are disclosed, wherein R.sub.1, represents secondary alkyl; aralkyl; cycloalkyl; heteroaryl substituted alkyl; norbornyl; and substituted secondary alkyl, aralkyl, cycloalkyl, heteroaryl substituted alkyl, norbornyl; and para-substituted phenyl groups; and R.sub.2 and R.sub.3 are hydrogen or pharmacologically acceptable acyl groups. The compounds of the invention are useful as cardiovascular vasodilator or anti-hypertensive agents. The therapeutically useful compounds of the invention as well as similar 5'-N and N-6 substituted adenosine 5'-uronamides are prepared, in accordance with a novel process, from isopropylidene (or otherwise suitably blocked) inosine-5' -uronic acid. Isopropylideneinosine-5' -uronic acid is reacted with a suitable inorganic acid halide, such as thionyl chloride, to yield 6-halogeno-9-[ 2',3' -O-isopropylidene-.beta.-D-ribofuranosyl-5-uronic acid halide] -9H-purine. This intermediate is reacted with an amine of the general formula R.sub.4,R.sub.

Abstract: Novel adenine derivatives whose structures are represented by Formula I, are disclosed, as are methods of using those compounds and others of Formula II to treat monocyte-mediated disorders such as rheumatoid arthritis and multiple sclerosis.

Abstract: Nucleic acid derivatives and pharmaceutical compositions containing such derivatives are produced containing one 4-thiouridylic acid for every 6 to 39 cytidylic acids present, which has a length of from 50 to 10,000 base pairs. Methods of treatment using these nucleic acid derivatives to treat viral infections is also described.

Abstract: The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.

Abstract: A method and compositions are provided for synthesizing polynucleotides wherein the exocyclic amino groups of 5'-O-protected-2'O-alkylsilyl-adenosine phosphoramidite and 5'-O-protected-2'-O-alkylsilylguanosine phosphoramidite monomers are protected with dialkylformamidine. In a preferred embodiment, the ribonucleoside phosphoramidite monomers are activated with ethylthiotetrazole.

Abstract: The present invention is directed to compounds useful as probes for characterizing and studying the adenosine A.sub.2 receptor. The present invention is also directed to methods of treating central nervous system disorders and cardiovascular disorders which include treating hypertension and thrombosis by administering said compounds.

Abstract: The present invention discloses a compound of the formula: ##STR1## where R.sub.1 is hydrogen or the group ##STR2## where R.sub.3 and R.sub.4 are the same or different and are hydrogen, C.sub.1 to C.sub.12 linear or branched alkyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.6 to C.sub.10 aryl unsubstituted or substituted with C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched alkoxy, nitro, amino, amino substituted with at least one C.sub.1 to C.sub.6 linear or branched alkyl or phenyl, C.sub.2 to C.sub.10 aralkyl, C.sub.4 to C.sub.8 heteroaryl wherein said heteroatom is nitrogen, phosphorous, sulfur or oxygen, and R.sub.2 is hydrogen, or taken together with R.sub.5, forms a chemical bond, and R is a monosaccharide radical selected from the group consisting essentially of glucose, fructose, ribose, 2-deoxyribose, mannose, galactose, xylose and arabinose.

Abstract: Disclosed are deoxyfructonucleotides and dideoxyfructonucleotides which may be used as propagators and terminators in DNA extension reactions.

Abstract: A method is provided for the high fidelity, rapid and economical in vitro synthesis of oligonucleotides. Nucleoside H-phosphonates are condensed in seriatim using a dehydrating agent to produce a poly (nucleoside H-phosphonate). The product is oxidized to yield the desired oligonucleotide. A novel reagent is provided for multiple nucleoside additions in single cycles.

Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.

Abstract: A method is provided for making 3' and/or 5' end-capped oligonucleotides so as to render the oligonucleotide resistant to degradation by exonucleases. The exonuclease degradation resistance is provided by incorporating two or more phosphoramidate and phosphorocmonothioate and/or phosphorodithioate linkages at the 5' and/or 3' ends of the oligonucleotide, wherein the number of phosphoramidate linkages is less than a number which would interfere with hybridization to a complementary oligonucleotide strand and/or which would interfere with RNAseH activity when the oligonucleotide is hybridized to RNA.